Call +1 (833) 552-7181 or Contact us Earn $25 in coupons on your first order with Aladdin!
Toggle Nav
My Cart
Search
Advanced Search
Menu
Sign In
྾
main product photo

Recombinant Human PDGFR alpha Protein

Features and benefits
  • Expression System: HEK293
  • Accession #: P16234
  • Protein Tag: C-His
  • Bioactivity: Immobilized recombinant Human PDGF-B at 2.0 μg/mL can bind Recombinant Human PDGFR alpha Protein (rp149974), the EC₅₀ of this effect is 107.6 ng/mL.
  • Endotoxin Concentration: <0.1 EU/μg
Item Number
rp149974
Grouped product items
SKUSizeAvailabilityPrice Qty
rp149974-10μg
10μg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$279.90
rp149974-50μg
50μg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$439.90
rp149974-100μg
100μg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$699.90
rp149974-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$3,999.90
Add to Wish List Compare
Bulk Order  DATASHEET

Animal Free, ≥95% (SDS-PAGE), Active, 293F, C-His tag, 1-524 aa

View related series
Click to view protein information: PDGFRA
Accession#:P16234 Gene ID:5156 PDGFR alpha PDGFRA

Basic Description

Product NameRecombinant Human PDGFR alpha Protein
SynonymsAlpha platelet-derived growth factor receptor | Alpha-type platelet-derived growth factor receptor | CD140 antigen-like family member A | CD140a antigen | EC 2.7.10.1 | PDGFR-2 | PDGFR-alpha | PDGF-R-alpha | Platelet-derived growth factor alpha receptor |
GradeActiBioPure™, Animal Free, Azide Free, Bioactive, Carrier Free
Product Description

Purity
≥95% (SDS-PAGE)
Endotoxin level
＜0.1 EU/μg
Function
Receptor that binds both PDGFA and PDGFB and has a tyrosine-protein kinase activity.

Specifications & PurityActiBioPure™, Bioactive, Animal Free, Carrier Free, Azide Free, ≥95%(SDS-PAGE)
BioactivityImmobilized recombinant Human PDGF-B at 2.0 μg/mL can bind Recombinant Human PDGFR alpha Protein (rp149974), the EC₅₀ of this effect is 107.6 ng/mL.
Endotoxin Concentration<0.1 EU/μg
Expression SystemHEK293
SpeciesHuman
Amino Acids1-524 aa
SequenceMGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYPMSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIYVPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNGTFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNNEVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVKEMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENLTEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDLVDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRDRSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSEHHHHHH
Protein TagC-His
Accession #P16234
Predicted molecular weight59 kDa
SDS-PAGE70 - 95 kDa, under reducing conditions; 65 - 90 kDa, under non-reducing conditions.

Images

Recombinant Human PDGFR alpha Protein (rp149974) - Protein Bioactivity
Immobilized recombinant Human PDGF-B at 2.0 μg/mL can bind Recombinant Human PDGFR alpha Protein (rp149974), the EC50 of this effect is 107.6 ng/mL.

Recombinant Human PDGFR alpha Protein (rp149974) - SDS-PAGE
3 μg/lane of Recombinant Human PDGFR alpha Protein was resolved with SDS-PAGE under reducing (R) and non-reducing (N) conditions and visualized by Coomassie® Blue staining, showing a band at 70 - 95 kDa under reducing condition and 65 -90 kDa under non-reducing condition.

Product Specifications

FormLyophilized
ReconstitutionReconstitute in sterile water to a concentration of 0.1-0.5 mg/ml.
Storage TempStore at -20°C,Avoid repeated freezing and thawing
Shipped InIce chest + Ice pads
Stability And StorageStore at -20~-80℃ for more than 1 year. Upon delivery aliquot. Avoid freeze/thaw cycle.

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Related Documents

 SDS

 Specification Sheet

FAQs and Articles

FAQ
Aladdin® Target Proteins
Categories: Technical articles
Tags:
Cytokines Drug development Target Proteins Drug Targets Receptors Immune Checkpoints Cell Surface Markers Signaling Pathways

References

1. Kraker AJ, Hartl BG, Amar AM, Barvian MR, Showalter HD, Moore CW..  (2000)  Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors..  Biochem Pharmacol,  60  (7): (885-898).  [PMID:10974196] [10.1016/s0006-2952(00)00405-6]
2. Huber K, Brault L, Fedorov O, Gasser C, Filippakopoulos P, Bullock AN, Fabbro D, Trappe J, Schwaller J, Knapp S et al..  (2012)  7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes..  J Med Chem,  55  (1): (403-13).  [PMID:22136433] [10.1021/op500134e]
3. Kubo K, Shimizu T, Ohyama S, Murooka H, Iwai A, Nakamura K, Hasegawa K, Kobayashi Y, Takahashi N, Takahashi K et al..  (2005)  Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas..  J Med Chem,  48  (5): (1359-66).  [PMID:15743179] [10.1021/op500134e]
4. Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S et al..  (2010)  Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant..  J Med Chem,  53  (12): (4701-19).  [PMID:20513156] [10.1021/op500134e]
5. Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Müller A, Baumgartner C, Valent P, Augustin M et al..  (2009)  Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells..  Leukemia,  23  (3): (477-85).  [PMID:19039322] [10.1021/op500134e]
6. Dubreuil P, Letard S, Ciufolini M, Gros L, Humbert M, Castéran N, Borge L, Hajem B, Lermet A, Sippl W et al..  (2009)  Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT..  PLoS ONE,  4  (9): (e7258).  [PMID:19789626] [10.1021/op500134e]
7. Zhou Y, Chen Y, Tong L, Xie H, Wen W, Zhang J, Xi Y, Shen Y, Geng M, Wang Y et al..  (2012)  AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR..  J Cell Mol Med,  16  (10): (2321-30).  [PMID:22304225] [10.1021/op500134e]
8. Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A et al..  (2006)  N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor..  J Med Chem,  49  (22): (6465-88).  [PMID:17064066] [10.1021/op500134e]
9. Klutchko SR, Zhou H, Winters RT, Tran TP, Bridges AJ, Althaus IW, Amato DM, Elliott WL, Ellis PA, Meade MA et al..  (2006)  Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors..  J Med Chem,  49  (4): (1475-85).  [PMID:16480284] [10.1021/op500134e]
10. Oyarzabal J, Zarich N, Albarran MI, Palacios I, Urbano-Cuadrado M, Mateos G, Reymundo I, Rabal O, Salgado A, Corrionero A et al..  (2010)  Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach..  J Med Chem,  53  (18): (6618-28).  [PMID:20722422] [10.1021/op500134e]
11. Heinrich MC, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M.  (2012)  Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors..  Clin Cancer Res,  18  (16): (4375-84).  [PMID:22745105] [10.1021/op500134e]
12. Roberts WG, Whalen PM, Soderstrom E, Moraski G, Lyssikatos JP, Wang HF, Cooper B, Baker DA, Savage D, Dalvie D et al..  (2005)  Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451..  Cancer Res,  65  (3): (957-66).  [PMID:15705896] [10.1021/op500134e]
13. Trudel S, Li ZH, Wei E, Wiesmann M, Chang H, Chen C, Reece D, Heise C, Stewart AK.  (2005)  CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma..  Blood,  105  (7): (2941-8).  [PMID:15598814] [10.1021/op500134e]
14. Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C.  (2009)  Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4)..  J Med Chem,  52  (20): (6433-46).  [PMID:19788238] [10.1021/op500134e]
15. Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K et al..  (2012)  Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent..  J Med Chem,  55  (2): (903-13).  [PMID:22148921] [10.1021/op500134e]
16. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM.  (2009)  Inhibitor hijacking of Akt activation..  Nat Chem Biol,  5  (7): (484-93).  [PMID:19465931] [10.1021/op500134e]
17. Fraser C, Dawson JC, Dowling R, Houston DR, Weiss JT, Munro AF, Muir M, Harrington L, Webster SP, Frame MC et al..  (2016)  Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase..  J Med Chem,  59  (10): (4697-710).  [PMID:27115835] [10.1021/op500134e]
18. Uckun FM, Dibirdik I, Qazi S, Vassilev A, Ma H, Mao C, Benyumov A, Emami KH.  (2007)  Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK)..  Bioorg Med Chem,  15  (2): (800-14).  [PMID:17098432] [10.1021/op500134e]
19. Kim KH, Maderna A, Schnute ME, Hegen M, Mohan S, Miyashiro J, Lin L, Li E, Keegan S, Lussier J et al..  (2011)  Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis..  Bioorg Med Chem Lett,  21  (21): (6258-63).  [PMID:21958547] [10.1021/op500134e]
20. Lam B, Arikawa Y, Cramlett J, Dong Q, de Jong R, Feher V, Grimshaw CE, Farrell PJ, Hoffman ID, Jennings A et al..  (2016)  Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK)..  Bioorg Med Chem Lett,  26  (24): (5947-5950).  [PMID:27839918] [10.1021/op500134e]
21. Huang Z, Li H, Zhang Q, Lu F, Hong M, Zhang Z, Guo X, Zhu Y, Li S, Liu H.  (2017)  Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis..  ACS Med Chem Lett,  8  (11): (1142-1147).  [PMID:29152045] [10.1021/op500134e]
22. Burger MT, Nishiguchi G, Han W, Lan J, Simmons R, Atallah G, Ding Y, Tamez V, Zhang Y, Mathur M et al..  (2015)  Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies..  J Med Chem,  58  (21): (8373-86).  [PMID:26505898] [10.1021/op500134e]
23. Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH et al..  (2012)  Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families..  J Pharmacol Exp Ther,  343  (3): (617-27).  [PMID:22935731] [10.1021/op500134e]
24. Patwardhan PP, Ivy KS, Musi E, de Stanchina E, Schwartz GK.  (2016)  Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma..  Oncotarget,  7  (4): (4093-109).  [PMID:26675259] [10.1021/op500134e]
25. Gucký T, Řezníčková E, Radošová Muchová T, Jorda R, Klejová Z, Malínková V, Berka K, Bazgier V, Ajani H, Lepšík M et al..  (2018)  Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations..  J Med Chem,  61  (9): (3855-3869).  [PMID:29672049] [10.1021/op500134e]
26. Pippione AC, Sainas S, Federico A, Lupino E, Piccinini M, Kubbutat M, Contreras JM, Morice C, Barge A, Ducime A et al..  (2018)  N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK..  Medchemcomm,  9  (6): (963-968).  [PMID:30108985] [10.1039/C8MD00068A]
27. Reich SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B, Ernst JT, Han Q, Goel VK et al..  (2018)  Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition..  J Med Chem,  61  (8): (3516-3540).  [PMID:29526098] [10.1021/op500134e]
28. Zhang H, Xu L, Qin X, Chen X, Cong H, Hu L, Chen L, Miao Z, Zhang W, Cai Z et al..  (2019)  N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships, and in Vivo Efficacy..  J Med Chem,  62  (14): (6665-6681).  [PMID:31095385] [10.1021/op500134e]
29. Wu Y, Wang B, Wang J, Qi S, Zou F, Qi Z, Liu F, Liu Q, Chen C, Hu C et al..  (2019)  Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors..  J Med Chem,  62  (13): (6083-6101).  [PMID:31250638] [10.1021/op500134e]
30. Zhou Y, Shan S, Li ZB, Xin LJ, Pan DS, Yang QJ, Liu YP, Yue XP, Liu XR, Gao JZ et al..  (2017)  CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency..  Cancer Sci,  108  (3): (469-477).  [PMID:28004478] [10.1021/op500134e]
31. Mazzocca A, Napolitano A, Silletta M, Spalato Ceruso M, Santini D, Tonini G, Vincenzi B.  (2019)  New frontiers in the medical management of gastrointestinal stromal tumours..  Ther Adv Med Oncol,  11  (13): (1755-70).  [PMID:31205499] [10.1177/1758835919841946]
32. Ren X, Pan X, Zhang Z, Wang D, Lu X, Li Y, Wen D, Long H, Luo J, Feng Y et al..  (2013)  Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib..  J Med Chem,  56  (3): (879-94).  [PMID:23301703] [10.1021/op500134e]
33. Liao AT, Chien MB, Shenoy N, Mendel DB, McMahon G, Cherrington JM, London CA.  (2002)  Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors..  Blood,  100  (2): (585-93).  [PMID:12091352] [10.1021/op500134e]
34. Yang H, Chennamaneni LR, Ho MWT, Ang SH, Tan ESW, Jeyaraj DA, Yeap YS, Liu B, Ong EH, Joy JK et al..  (2018)  Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia..  J Med Chem,  61  (10): (4348-4369).  [PMID:29683667] [10.1021/op500134e]
35. Seunghee Hong,Jinhee Kim,Sun-Mi Yun,Hyunseung Lee,Yoonsu Park,Soon-Sun Hong,Sungwoo Hong.  (2013-04-23)  Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant..  Journal of medicinal chemistry,  56  ((9)): (3531-3545).  [PMID:23600806]
36. Sung Hee Hwang, Aaron T Wecksler, Guodong Zhang, Christophe Morisseau, Long V Nguyen, Samuel H Fu, Bruce D Hammock,.  (2013-06-04)  Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors..  Bioorganic & medicinal chemistry letters,  23  ((13)): ( 3732-3737 ).  [PMID:23726028]
37. Ajit Dhananjay Jagtap,Pei-Teh Chang,Jia-Rong Liu,Hsiao-Chun Wang,Nagendra B Kondekar,Li-Jiuan Shen,Hsiang-Wen Tseng,Grace Shiahuy Chen,Ji-Wang Chern.  (2014-08-05)  Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia..  European journal of medicinal chemistry,  85  (268-288).  [PMID:25089810]
38. Bing Yu,Li-da Tang,Yi-Liang Li,Shu-Hui Song,Xiao-Liang Ji,Mu-Sen Lin,Chun-Fu Wu.  (2011-12-16)  Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase..  Bioorganic & medicinal chemistry letters,  22  ((1)): (110-114).  [PMID:22169262]
39. Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA..  (2004)  3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding..  J Med Chem,  47  (13): (3367-3380).  [PMID:15189033] [10.1021/jm031145u]
40. Kuo GH, Wang A, Emanuel S, Deangelis A, Zhang R, Connolly PJ, Murray WV, Gruninger RH, Sechler J, Fuentes-Pesquera A, Johnson D, Middleton SA, Jolliffe L, Chen X..  (2005)  Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors..  J Med Chem,  48  (6): (1886-1900).  [PMID:15771433] [10.1021/jm040099a]
41. VanderWel SN, Harvey PJ, McNamara DJ, Repine JT, Keller PR, Quin J, Booth RJ, Elliott WL, Dobrusin EM, Fry DW, Toogood PL..  (2005)  Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4..  J Med Chem,  48  (7): (2371-2387).  [PMID:15801830] [10.1021/jm049355+]
42. Vendôme J, Letard S, Martin F, Svinarchuk F, Dubreuil P, Auclair C, Le Bret M..  (2005)  Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases..  J Med Chem,  48  (20): (6194-6201).  [PMID:16190746] [10.1021/jm050231m]
43. McDermott LA, Higgins B, Simcox M, Luk KC, Nevins T, Kolinsky K, Smith M, Yang H, Li JK, Chen Y, Ke J, Mallalieu N, Egan T, Kolis S, Railkar A, Gerber L, Liu JJ, Konzelmann F, Zhang Z, Flynn T, Morales O, Chen Y..  (2006)  Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis..  Bioorg Med Chem Lett,  16  (7): (1950-1953).  [PMID:16460940] [10.1016/j.bmcl.2005.12.092]
44. Cee VJ, Albrecht BK, Geuns-Meyer S, Hughes P, Bellon S, Bready J, Caenepeel S, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hodous BL, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, McGowan D, Morrison M, Olivieri PR, Patel VF, Polverino A, Powers D, Rose P, Wang L, Zhao H..  (2007)  Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase..  J Med Chem,  50  (4): (627-640).  [PMID:17253679] [10.1021/jm061112p]
45. Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ..  (2007)  1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel..  J Med Chem,  50  (9): (2011-2029).  [PMID:17425296] [10.1021/jm061223o]
46. Weiss MM, Harmange JC, Polverino AJ, Bauer D, Berry L, Berry V, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Whittington DA, Zanon R..  (2008)  Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors..  J Med Chem,  51  (6): (1668-1680).  [PMID:18324759] [10.1021/jm701098w]
47. McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, Lamb J, Archibald H, Raudales R, Tam A, Lee D, Rothenberg SM, Supko JG, Sordella R, Ulkus LE, Iafrate AJ, Maheswaran S, Njauw CN, Tsao H, Drew L, Hanke JH, Ma XJ, Erlander MG, Gray NS, Haber DA, Settleman J..  (2007)  Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling..  Proc Natl Acad Sci U S A,  104  (50): (19936-19941).  [PMID:18077425] [10.1073/pnas.0707498104]
48. Kunz RK, Rumfelt S, Chen N, Zhang D, Tasker AS, Bürli R, Hungate R, Yu V, Nguyen Y, Whittington DA, Meagher KL, Plant M, Tudor Y, Schrag M, Xu Y, Ng GY, Hu E..  (2008)  Discovery of amido-benzisoxazoles as potent c-Kit inhibitors..  Bioorg Med Chem Lett,  18  (18): (5115-5117).  [PMID:18723346] [10.1016/j.bmcl.2008.07.111]
49. Golubovskaya VM, Nyberg C, Zheng M, Kweh F, Magis A, Ostrov D, Cance WG..  (2008)  A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the y397 site of focal adhesion kinase decreases tumor growth..  J Med Chem,  51  (23): (7405-7416).  [PMID:18989950] [10.1021/jm800483v]
50. Cha MY, Lee KO, Kim JW, Lee CG, Song JY, Kim YH, Lee GS, Park SB, Kim MS..  (2009)  Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer..  J Med Chem,  52  (21): (6880-6888).  [PMID:19888761] [10.1021/jm901146p]
51. Antczak C, Veach DR, Ramirez CN, Minchenko MA, Shum D, Calder PA, Frattini MG, Clarkson B, Djaballah H..  (2009)  Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors..  Bioorg Med Chem Lett,  19  (24): (6872-6876).  [PMID:19889540] [10.1016/j.bmcl.2009.10.085]
52. Shomin CD, Meyer SC, Ghosh I..  (2009)  Staurosporine tethered peptide ligands that target cAMP-dependent protein kinase (PKA): optimization and selectivity profiling..  Bioorg Med Chem,  17  (17): (6196-6202).  [PMID:19674907] [10.1016/j.bmc.2009.07.056]
53. Wee XK, Yeo WK, Zhang B, Tan VB, Lim KM, Tay TE, Go ML..  (2009)  Synthesis and evaluation of functionalized isoindigos as antiproliferative agents..  Bioorg Med Chem,  17  (21): (7562-7571).  [PMID:19783149] [10.1016/j.bmc.2009.09.008]
54. Pettus LH, Wurz RP, Xu S, Herberich B, Henkle B, Liu Q, McBride HJ, Mu S, Plant MH, Saris CJ, Sherman L, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS..  (2010)  Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase..  J Med Chem,  53  (7): (2973-2985).  [PMID:20218619] [10.1021/jm100095x]
55. Yu H, Jung Y, Kim H, Lee J, Oh CH, Yoo KH, Sim T, Hah JM..  (2010)  1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives: a novel type II Raf kinase inhibitors..  Bioorg Med Chem Lett,  20  (12): (3805-3808).  [PMID:20466542] [10.1016/j.bmcl.2010.04.039]
56. Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T..  (2010)  A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl..  J Med Chem,  53  (15): (5439-5448).  [PMID:20604564] [10.1021/jm901808w]
57. Barile E, De SK, Carlson CB, Chen V, Knutzen C, Riel-Mehan M, Yang L, Dahl R, Chiang G, Pellecchia M..  (2010)  Design, synthesis, and structure-activity relationships of 3-ethynyl-1H-indazoles as inhibitors of the phosphatidylinositol 3-kinase signaling pathway..  J Med Chem,  53  (23): (8368-8375).  [PMID:21062009] [10.1021/jm100825h]
58. Charrier JD, Miller A, Kay DP, Brenchley G, Twin HC, Collier PN, Ramaya S, Keily SB, Durrant SJ, Knegtel RM, Tanner AJ, Brown K, Curnock AP, Jimenez JM..  (2011)  Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors..  J Med Chem,  54  (7): (2341-2350).  [PMID:21391610] [10.1021/jm101499u]
59. Okamoto M, Kojima H, Saito N, Okabe T, Masuda Y, Furuya T, Nagano T..  (2011)  Virtual screening and further development of novel ALK inhibitors..  Bioorg Med Chem,  19  (10): (3086-3095).  [PMID:21515061] [10.1016/j.bmc.2011.04.008]
60. Shallal HM, Russu WA..  (2011)  Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives..  Eur J Med Chem,  46  (6): (2043-2057).  [PMID:21429632] [10.1016/j.ejmech.2011.02.057]
61. Lin WH, Hsieh SY, Yen SC, Chen CT, Yeh TK, Hsu T, Lu CT, Chen CP, Chen CW, Chou LH, Huang YL, Cheng AH, Chang YI, Tseng YJ, Yen KR, Chao YS, Hsu JT, Jiaang WT..  (2011)  Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3)..  Bioorg Med Chem,  19  (14): (4173-4182).  [PMID:21708468] [10.1016/j.bmc.2011.06.016]
62. Ishikawa T, Seto M, Banno H, Kawakita Y, Oorui M, Taniguchi T, Ohta Y, Tamura T, Nakayama A, Miki H, Kamiguchi H, Tanaka T, Habuka N, Sogabe S, Yano J, Aertgeerts K, Kamiyama K..  (2011)  Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold..  J Med Chem,  54  (23): (8030-8050).  [PMID:22003817] [10.1021/jm2008634]
63. Li WW, Wang XY, Zheng RL, Yan HX, Cao ZX, Zhong L, Wang ZR, Ji P, Yang LL, Wang LJ, Xu Y, Liu JJ, Yang J, Zhang CH, Ma S, Feng S, Sun QZ, Wei YQ, Yang SY..  (2012)  Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo..  J Med Chem,  55  (8): (3852-3866).  [PMID:22452518] [10.1021/jm300042x]
64. Nakano H, Saito N, Parker L, Tada Y, Abe M, Tsuganezawa K, Yokoyama S, Tanaka A, Kojima H, Okabe T, Nagano T..  (2012)  Rational evolution of a novel type of potent and selective proviral integration site in Moloney murine leukemia virus kinase 1 (PIM1) inhibitor from a screening-hit compound..  J Med Chem,  55  (11): (5151-5164).  [PMID:22540945] [10.1021/jm3001289]
65. Duveau DY, Hu X, Walsh MJ, Shukla S, Skoumbourdis AP, Boxer MB, Ambudkar SV, Shen M, Thomas CJ..  (2013)  Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors..  Bioorg Med Chem Lett,  23  (3): (682-686).  [PMID:23273517] [10.1016/j.bmcl.2012.11.111]
66. Garofalo AW, Adler M, Aubele DL, Bowers S, Franzini M, Goldbach E, Lorentzen C, Neitz RJ, Probst GD, Quinn KP, Santiago P, Sham HL, Tam D, Truong AP, Ye XM, Ren Z..  (2013)  Novel cinnoline-based inhibitors of LRRK2 kinase activity..  Bioorg Med Chem Lett,  23  (1): (71-74).  [PMID:23219325] [10.1016/j.bmcl.2012.11.021]
67. Yang LL, Li GB, Ma S, Zou C, Zhou S, Sun QZ, Cheng C, Chen X, Wang LJ, Feng S, Li LL, Yang SY..  (2013)  Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo..  J Med Chem,  56  (4): (1641-1655).  [PMID:23362959] [10.1021/jm301537p]
68. Mortensen DS, Sapienza J, Lee BG, Perrin-Ninkovic SM, Harris R, Shevlin G, Parnes JS, Whitefield B, Hickman M, Khambatta G, Bisonette RR, Peng S, Gamez JC, Leisten J, Narla RK, Fultz KE, Sankar S..  (2013)  Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase..  Bioorg Med Chem Lett,  23  (6): (1588-1591).  [PMID:23414803] [10.1016/j.bmcl.2013.01.110]
69. Garofalo AW, Adler M, Aubele DL, Brigham EF, Chian D, Franzini M, Goldbach E, Kwong GT, Motter R, Probst GD, Quinn KP, Ruslim L, Sham HL, Tam D, Tanaka P, Truong AP, Ye XM, Ren Z..  (2013)  Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors..  Bioorg Med Chem Lett,  23  (7): (1974-1977).  [PMID:23453068] [10.1016/j.bmcl.2013.02.041]
70. Franzini M, Ye XM, Adler M, Aubele DL, Garofalo AW, Gauby S, Goldbach E, Probst GD, Quinn KP, Santiago P, Sham HL, Tam D, Truong A, Ren Z..  (2013)  Triazolopyridazine LRRK2 kinase inhibitors..  Bioorg Med Chem Lett,  23  (7): (1967-1973).  [PMID:23454015] [10.1016/j.bmcl.2013.02.043]
71. Lin WH, Hsu JT, Hsieh SY, Chen CT, Song JS, Yen SC, Hsu T, Lu CT, Chen CH, Chou LH, Yang YN, Chiu CH, Chen CP, Tseng YJ, Yen KJ, Yeh CF, Chao YS, Yeh TK, Jiaang WT..  (2013)  Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3)..  Bioorg Med Chem,  21  (11): (2856-2867).  [PMID:23618709] [10.1016/j.bmc.2013.03.083]
72. Troxler T, Greenidge P, Zimmermann K, Desrayaud S, Drückes P, Schweizer T, Stauffer D, Rovelli G, Shimshek DR..  (2013)  Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2..  Bioorg Med Chem Lett,  23  (14): (4085-4090).  [PMID:23768909] [10.1016/j.bmcl.2013.05.054]
73. Gogate PN, Ethirajan M, Kurenova EV, Magis AT, Pandey RK, Cance WG..  (2014)  Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction..  Eur J Med Chem,  80  (154-166).  [PMID:24780592] [10.1016/j.ejmech.2014.04.041]
74. Xie F, Zhu H, Zhang H, Lang Q, Tang L, Huang Q, Yu L..  (2015)  In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor..  Eur J Med Chem,  89  (310-319).  [PMID:25462247] [10.1016/j.ejmech.2014.10.044]
75. Zhang P, Li S, Gao Y, Lu W, Huang K, Ye D, Li X, Chu Y..  (2014)  Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake..  Bioorg Med Chem Lett,  24  (24): (5639-5643).  [PMID:25467150] [10.1016/j.bmcl.2014.10.078]
76. Song Z, Yang Y, Liu Z, Peng X, Guo J, Yang X, Wu K, Ai J, Ding J, Geng M, Zhang A..  (2015)  Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases..  J Med Chem,  58  (1): (197-211).  [PMID:24785465] [10.1021/jm5005144]
77. Muth F, Günther M, Bauer SM, Döring E, Fischer S, Maier J, Drückes P, Köppler J, Trappe J, Rothbauer U, Koch P, Laufer SA..  (2015)  Tetra-substituted pyridinylimidazoles as dual inhibitors of p38α mitogen-activated protein kinase and c-Jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases..  J Med Chem,  58  (1): (443-456).  [PMID:25475894] [10.1021/jm501557a]
78. Roth GJ, Binder R, Colbatzky F, Dallinger C, Schlenker-Herceg R, Hilberg F, Wollin SL, Kaiser R..  (2015)  Nintedanib: from discovery to the clinic..  J Med Chem,  58  (3): (1053-1063).  [PMID:25474320] [10.1021/jm501562a]
79. Lawrence HR, Mahajan K, Luo Y, Zhang D, Tindall N, Huseyin M, Gevariya H, Kazi S, Ozcan S, Mahajan NP, Lawrence NJ..  (2015)  Development of novel ACK1/TNK2 inhibitors using a fragment-based approach..  J Med Chem,  58  (6): (2746-2763).  [PMID:25699576] [10.1021/jm501929n]
80. Kovackova S, Chang L, Bekerman E, Neveu G, Barouch-Bentov R, Chaikuad A, Heroven C, Šála M, De Jonghe S, Knapp S, Einav S, Herdewijn P..  (2015)  Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents..  J Med Chem,  58  (8): (3393-3410).  [PMID:25822739] [10.1021/jm501759m]
81. Zhang CH, Zheng MW, Li YP, Lin XD, Huang M, Zhong L, Li GB, Zhang RJ, Lin WT, Jiao Y, Wu XA, Yang J, Xiang R, Chen LJ, Zhao YL, Cheng W, Wei YQ, Yang SY..  (2015)  Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer..  J Med Chem,  58  (9): (3957-3974).  [PMID:25835317] [10.1021/acs.jmedchem.5b00270]
82. Lin XD, Yang HW, Ma S, Li WW, Zhang CH, Wang WJ, Xiang R, Li LL, Yang SY..  (2015)  Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors..  Bioorg Med Chem Lett,  25  (20): (4534-4538).  [PMID:26342867] [10.1016/j.bmcl.2015.08.068]
83. Carta D, Bortolozzi R, Hamel E, Basso G, Moro S, Viola G, Ferlin MG..  (2015)  Novel 3-Substituted 7-Phenylpyrrolo[3,2-f]quinolin-9(6H)-ones as Single Entities with Multitarget Antiproliferative Activity..  J Med Chem,  58  (20): (7991-8010).  [PMID:26418966] [10.1021/acs.jmedchem.5b00805]
84. Ravez S, Arsenlis S, Barczyk A, Dupont A, Frédérick R, Hesse S, Kirsch G, Depreux P, Goossens L..  (2015)  Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors..  Bioorg Med Chem,  23  (22): (7340-7347).  [PMID:26526740] [10.1016/j.bmc.2015.10.035]
85. Nakano H, Hasegawa T, Saito N, Furukawa K, Mukaida N, Kojima H, Okabe T, Nagano T..  (2015)  Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent..  Bioorg Med Chem Lett,  25  (24): (5687-5693).  [PMID:26547690] [10.1016/j.bmcl.2015.10.098]
86. Meredith EL, Mainolfi N, Poor S, Qiu Y, Miranda K, Powers J, Liu D, Ma F, Solovay C, Rao C, Johnson L, Ji N, Artman G, Hardegger L, Hanks S, Shen S, Woolfenden A, Fassbender E, Sivak JM, Zhang Y, Long D, Cepeda R, Liu F, Hosagrahara VP, Lee W, Tarsa P, Anderson K, Elliott J, Jaffee B..  (2015)  Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration..  J Med Chem,  58  (23): (9273-9286).  [PMID:26568411] [10.1021/acs.jmedchem.5b01227]
87. Han W, Menezes DL, Xu Y, Knapp MS, Elling R, Burger MT, Ni ZJ, Smith A, Lan J, Williams TE, Verhagen J, Huh K, Merritt H, Chan J, Kaufman S, Voliva CF, Pecchi S..  (2016)  Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model..  Bioorg Med Chem Lett,  26  (3): (742-746).  [PMID:26774655] [10.1016/j.bmcl.2016.01.003]
88. Simov V, Deshmukh SV, Dinsmore CJ, Elwood F, Fernandez RB, Garcia Y, Gibeau C, Gunaydin H, Jung J, Katz JD, Kraybill B, Lapointe B, Patel SB, Siu T, Su H, Young JR..  (2016)  Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors..  Bioorg Med Chem Lett,  26  (7): (1803-1808).  [PMID:26927423] [10.1016/j.bmcl.2016.02.035]
89. Daydé-Cazals B, Fauvel B, Singer M, Feneyrolles C, Bestgen B, Gassiot F, Spenlinhauer A, Warnault P, Van Hijfte N, Borjini N, Chevé G, Yasri A..  (2016)  Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors..  J Med Chem,  59  (8): (3886-3905).  [PMID:27010810] [10.1021/acs.jmedchem.6b00087]
90. Wang Q, Liu F, Wang B, Zou F, Chen C, Liu X, Wang A, Qi S, Wang W, Qi Z, Zhao Z, Hu Z, Wang W, Wang L, Zhang S, Wang Y, Liu J, Liu Q..  (2016)  Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs)..  J Med Chem,  59  (8): (3964-3979).  [PMID:27077705] [10.1021/acs.jmedchem.6b00200]
91. Schroeder RL, Goyal N, Bratton M, Townley I, Pham NA, Tram P, Stone T, Geathers J, Nguyen K, Sridhar J..  (2016)  Identification of quinones as novel PIM1 kinase inhibitors..  Bioorg Med Chem Lett,  26  (13): (3187-3191).  [PMID:27173800] [10.1016/j.bmcl.2016.04.079]
92. Kim H, Lee C, Yang JS, Choi S, Park CH, Kang JS, Oh SJ, Yun J, Kim MH, Han G..  (2016)  Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia..  Eur J Med Chem,  120  (74-85).  [PMID:27187860] [10.1016/j.ejmech.2016.05.022]
93. Cheeseman MD, Chessum NE, Rye CS, Pasqua AE, Tucker MJ, Wilding B, Evans LE, Lepri S, Richards M, Sharp SY, Ali S, Rowlands M, O'Fee L, Miah A, Hayes A, Henley AT, Powers M, Te Poele R, De Billy E, Pellegrino L, Raynaud F, Burke R, van Montfort RL, Eccles SA, Workman P, Jones K..  (2017)  Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen..  J Med Chem,  60  (1): (180-201).  [PMID:28004573] [10.1021/acs.jmedchem.6b01055]
94. Ma F, Liu P, Lei M, Liu J, Wang H, Zhao S, Hu L..  (2017)  Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3)..  Eur J Med Chem,  127  (72-86).  [PMID:28038328] [10.1016/j.ejmech.2016.12.038]
95. Lu Y, Mao F, Li X, Zheng X, Wang M, Xu Q, Zhu J, Li J..  (2017)  Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs)..  J Med Chem,  60  (12): (5099-5119).  [PMID:28541695] [10.1021/acs.jmedchem.7b00468]
96. Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S..  (2017)  Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers..  J Med Chem,  60  (12): (4869-4881).  [PMID:28557458] [10.1021/acs.jmedchem.6b01862]
97. Zhu W, Chen H, Wang Y, Wang J, Peng X, Chen X, Gao Y, Li C, He Y, Ai J, Geng M, Zheng M, Liu H..  (2017)  Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer..  J Med Chem,  60  (14): (6018-6035).  [PMID:28714692] [10.1021/acs.jmedchem.7b00076]
98. Zhao F, Zhang LD, Hao Y, Chen N, Bai R, Wang YJ, Zhang CC, Li GS, Hao LJ, Shi C, Zhang J, Mao Y, Fan Y, Xia GX, Yu JX, Liu YJ..  (2017)  Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization..  Eur J Med Chem,  134  (147-158).  [PMID:28411455] [10.1016/j.ejmech.2017.03.085]
99. He L, Li D, Zhang C, Bai P, Chen L..  (2017)  Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC..  Bioorg Med Chem Lett,  27  (17): (4171-4175).  [PMID:28734581] [10.1016/j.bmcl.2017.07.009]
100. Adams CM, Anderson K, Artman G, Bizec JC, Cepeda R, Elliott J, Fassbender E, Ghosh M, Hanks S, Hardegger LA, Hosagrahara VP, Jaffee B, Jendza K, Ji N, Johnson L, Lee W, Liu D, Liu F, Long D, Ma F, Mainolfi N, Meredith EL, Miranda K, Peng Y, Poor S, Powers J, Qiu Y, Rao C, Shen S, Sivak JM, Solovay C, Tarsa P, Woolfenden A, Zhang C, Zhang Y..  (2018)  The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration..  J Med Chem,  61  (4): (1622-1635).  [PMID:29400470] [10.1021/acs.jmedchem.7b01731]
101. Fukuda T, Goto R, Kiho T, Ueda K, Muramatsu S, Hashimoto M, Aki A, Watanabe K, Tanaka N..  (2017)  Discovery of DS28120313 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4,6-disubstituted indazole derivatives..  Bioorg Med Chem Lett,  27  (23): (5252-5257).  [PMID:29079471] [10.1016/j.bmcl.2017.10.031]
102. Czarna A, Wang J, Zelencova D, Liu Y, Deng X, Choi HG, Zhang T, Zhou W, Chang JW, Kildalsen H, Seternes OM, Gray NS, Engh RA, Rothweiler U..  (2018)  Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors..  J Med Chem,  61  (17): (7560-7572).  [PMID:30095246] [10.1021/acs.jmedchem.7b01847]
103. Malínková V, Řezníčková E, Jorda R, Gucký T, Kryštof V..  (2017)  Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1..  Bioorg Med Chem,  25  (24): (6523-6535).  [PMID:29089259] [10.1016/j.bmc.2017.10.032]
104. Monastyrskyi A, Nilchan N, Quereda V, Noguchi Y, Ruiz C, Grant W, Cameron M, Duckett D, Roush W..  (2018)  Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer..  Bioorg Med Chem,  26  (3): (590-602).  [PMID:29289448] [10.1016/j.bmc.2017.12.020]
105. Myers SH, Temps C, Houston DR, Brunton VG, Unciti-Broceta A..  (2018)  Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening..  J Med Chem,  61  (5): (2104-2110).  [PMID:29466002] [10.1021/acs.jmedchem.7b01605]
106. Kettle JG, Anjum R, Barry E, Bhavsar D, Brown C, Boyd S, Campbell A, Goldberg K, Grondine M, Guichard S, Hardy CJ, Hunt T, Jones RDO, Li X, Moleva O, Ogg D, Overman RC, Packer MJ, Pearson S, Schimpl M, Shao W, Smith A, Smith JM, Stead D, Stokes S, Tucker M, Ye Y..  (2018)  Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors..  J Med Chem,  61  (19): (8797-8810).  [PMID:30204441] [10.1021/acs.jmedchem.8b00938]
107. Li X, Huang Y, Cheng J, Zhang L, Mao F, Zhu J, Sheng C, Li J..  (2018)  Discovery of novel Syk/PDGFR-α/c-Kit inhibitors as multi-targeting drugs to treat rheumatoid arthritis..  Bioorg Med Chem,  26  (15): (4375-4381).  [PMID:30078608] [10.1016/j.bmc.2018.06.029]
108. Hudson L, Mui J, Vázquez S, Carvalho DM, Williams E, Jones C, Bullock AN, Hoelder S..  (2018)  Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept..  J Med Chem,  61  (16): (7261-7272).  [PMID:30085668] [10.1021/acs.jmedchem.8b00782]
109. Zhang Y, Lv H, Luo L, Xu Y, Pan Y, Wang Y, Lin H, Xiong J, Guo P, Zhang J, Li X, Ye F..  (2018)  Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer..  Eur J Med Chem,  157  (1300-1325).  [PMID:30195240] [10.1016/j.ejmech.2018.08.031]
110. Liu X, Wang B, Chen C, Qi Z, Zou F, Wang J, Hu C, Wang A, Ge J, Liu Q, Yu K, Hu Z, Jiang Z, Wang W, Wang L, Wang W, Ren T, Bai M, Liu Q, Liu J..  (2019)  Discovery of ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs)..  J Med Chem,  62  (10): (5006-5024).  [PMID:31046271] [10.1021/acs.jmedchem.9b00176]
111. Baska F, Sipos A, Őrfi Z, Nemes Z, Dobos J, Szántai-Kis C, Szabó E, Szénási G, Dézsi L, Hamar P, Cserepes MT, Tóvári J, Garamvölgyi R, Krekó M, Őrfi L..  (2019)  Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases..  Eur J Med Chem,  184  (111710-111710).  [PMID:31614258] [10.1016/j.ejmech.2019.111710]
112. Martínez-González S, Rodríguez-Arístegui S, Gómez de la Oliva CA, Hernández AI, González Cantalapiedra E, Varela C, García AB, Rabal O, Oyarzabal J, Bischoff JR, Klett J, Albarrán MI, Cebriá A, Ajenjo N, García-Serelde B, Gómez-Casero E, Cuadrado-Urbano M, Cebrián D, Blanco-Aparicio C, Pastor J..  (2019)  Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors..  Eur J Med Chem,  168  (87-109).  [PMID:30802730] [10.1016/j.ejmech.2019.02.022]
113. Abdelaziz AM, Basnet SKC, Islam S, Li M, Tadesse S, Albrecht H, Gerber C, Yu M, Wang S..  (2019)  Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors..  Bioorg Med Chem Lett,  29  (18): (2650-2654).  [PMID:31362920] [10.1016/j.bmcl.2019.07.043]
114. Heng H, Wang Z, Li H, Huang Y, Lan Q, Guo X, Zhang L, Zhi Y, Cai J, Qin T, Xiang L, Wang S, Chen Y, Lu T, Lu S..  (2019)  Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model..  Eur J Med Chem,  176  (248-267).  [PMID:31103903] [10.1016/j.ejmech.2019.05.021]
115. Lin WH, Wu SY, Yeh TK, Chen CT, Song JS, Shiao HY, Kuo CC, Hsu T, Lu CT, Wang PC, Wu TS, Peng YH, Lin HY, Chen CP, Weng YL, Kung FC, Wu MH, Su YC, Huang KW, Chou LH, Hsueh CC, Yen KJ, Kuo PC, Huang CL, Chen LT, Shih C, Tsai HJ, Jiaang WT..  (2019)  Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia..  J Med Chem,  62  (24): (11135-11150).  [PMID:31721578] [10.1021/acs.jmedchem.9b01229]
116. Wang Y, Li L, Fan J, Dai Y, Jiang A, Geng M, Ai J, Duan W..  (2018)  Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors..  J Med Chem,  61  (20): (9085-9104).  [PMID:29522671] [10.1021/acs.jmedchem.7b01843]
117. Farag AK, Hassan AHE, Jeong H, Kwon Y, Choi JG, Oh MS, Park KD, Kim YK, Roh EJ..  (2019)  First-in-class DAPK1/CSF1R dual inhibitors: Discovery of 3,5-dimethoxy-N-(4-(4-methoxyphenoxy)-2-((6-morpholinopyridin-3-yl)amino)pyrimidin-5-yl)benzamide as a potential anti-tauopathies agent..  Eur J Med Chem,  162  (161-175).  [PMID:30445265] [10.1016/j.ejmech.2018.10.057]
118. Bensinger D, Stubba D, Cremer A, Kohl V, Waßmer T, Stuckert J, Engemann V, Stegmaier K, Schmitz K, Schmidt B..  (2019)  Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations..  J Med Chem,  62  (5): (2428-2446).  [PMID:30742435] [10.1021/acs.jmedchem.8b01714]
119. Wang Q, Dai Y, Ji Y, Shi H, Guo Z, Chen D, Chen Y, Peng X, Gao Y, Wang X, Chen L, Jiang Y, Geng M, Shen J, Ai J, Xiong B..  (2019)  Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma..  Eur J Med Chem,  163  (671-689).  [PMID:30572178] [10.1016/j.ejmech.2018.12.015]
120. Kang SJ, Lee JW, Chung SH, Jang SY, Choi J, Suh KH, Kim YH, Ham YJ, Min KH..  (2019)  Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors..  Eur J Med Chem,  163  (660-670).  [PMID:30576901] [10.1016/j.ejmech.2018.12.025]
121. Ikegashira K, Ikenogami T, Yamasaki T, Oka T, Hase Y, Miyagawa N, Inagaki K, Kawahara I, Koga Y, Hashimoto H..  (2019)  Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952..  Bioorg Med Chem Lett,  29  (7): (873-877).  [PMID:30755337] [10.1016/j.bmcl.2019.02.006]
122. Kaiser TM, Dentmon ZW, Dalloul CE, Sharma SK, Liotta DC..  (2020)  Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease..  ACS Med Chem Lett,  11  (4): (491-496).  [PMID:32292555] [10.1021/acsmedchemlett.9b00612]
123. Mathison CJN, Chianelli D, Rucker PV, Nelson J, Roland J, Huang Z, Yang Y, Jiang J, Xie YF, Epple R, Bursulaya B, Lee C, Gao MY, Shaffer J, Briones S, Sarkisova Y, Galkin A, Li L, Li N, Li C, Hua S, Kasibhatla S, Kinyamu-Akunda J, Kikkawa R, Molteni V, Tellew JE..  (2020)  Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma..  ACS Med Chem Lett,  11  (4): (558-565).  [PMID:32292564] [10.1021/acsmedchemlett.0c00015]
124. Hamilton GL,Chen H,Deshmukh G,Eigenbrot C,Fong R,Johnson A,Kohli PB,Lupardus PJ,Liederer BM,Ramaswamy S,Wang H,Wang J,Xu Z,Zhu Y,Vucic D,Patel S.  (2019)  Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group..  Bioorg Med Chem Lett,  29  (12.0): (1497-1501).  [PMID:31000154] [10.1016/j.bmcl.2019.04.014]
125. Zhou Y,Xu X,Wang F,He H,Gong G,Xiong L,Qi B.  (2020)  Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer..  Eur J Med Chem,  204  (112643-112643).  [PMID:32731184] [10.1016/j.ejmech.2020.112643]
126. Dart ML,Machleidt T,Jost E,Schwinn MK,Robers MB,Shi C,Kirkland TA,Killoran MP,Wilkinson JM,Hartnett JR,Zimmerman K,Wood KV.  (2018)  Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift..  ACS Med Chem Lett,  9  (6.0): (546-551).  [PMID:29937980] [10.1021/acsmedchemlett.8b00081]
127. Elwaie TA,Abbas SE,Aly EI,George RF,Ali H,Kraiouchkine N,Abdelwahed KS,Fandy TE,El Sayed KA,Abd Elmageed ZY,Ali HI.  (2020)  HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability..  J Med Chem,  63  (24.0): (15906-15945).  [PMID:33314925] [10.1021/acs.jmedchem.0c01647]
128. Sbenati RM,Zaraei SO,El-Gamal MI,Anbar HS,Tarazi H,Zoghbor MM,Mohamood NA,Khakpour MM,Zaher DM,Omar HA,Alach NN,Shehata MK,El-Gamal R.  (2021)  Design, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells..  Eur J Med Chem,  210  (113081-113081).  [PMID:33310290] [10.1016/j.ejmech.2020.113081]
129. Jeong P,Moon Y,Lee JH,Lee SD,Park J,Lee J,Kim J,Lee HJ,Kim NY,Choi J,Heo JD,Shin JE,Park HW,Kim YG,Han SY,Kim YC.  (2020)  Discovery of orally active indirubin-3'-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia..  Eur J Med Chem,  195  (112205-112205).  [PMID:32272419] [10.1016/j.ejmech.2020.112205]
130. Cao DS,Jiang SL,Guan YD,Chen XS,Zhang LX,Zhang Y,Chen AF,Yang JM,Cheng Y.  (2020)  A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone..  Eur J Med Chem,  199  (112421-112421).  [PMID:32428794] [10.1016/j.ejmech.2020.112421]
131. Wang B,Zhang W,Liu X,Zou F,Wang J,Liu Q,Wang A,Hu Z,Chen Y,Qi S,Jiang Z,Chen C,Hu C,Wang L,Wang W,Liu Q,Liu J.  (2020)  Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants..  Eur J Med Chem,  207  (112744-112744).  [PMID:32949955] [10.1016/j.ejmech.2020.112744]
132. Yu, J C JC and 6 more authors..  (1991)  Tyrosine mutations within the alpha platelet-derived growth factor receptor kinase insert domain abrogate receptor-associated phosphatidylinositol-3 kinase activity without affecting mitogenic or chemotactic signal transduction..  Molecular and cellular biology,      [PMID:1646396]
133. Anderson, D D and 5 more authors..  (1990)  Binding of SH2 domains of phospholipase C gamma 1, GAP, and Src to activated growth factor receptors..  Science (New York, N.Y.),    (16):   [PMID:2173144]
134. Matsui, T T and 7 more authors..  (1989)  Isolation of a novel receptor cDNA establishes the existence of two PDGF receptor genes..  Science (New York, N.Y.),    (10):   [PMID:2536956]
135. Claesson-Welsh, L L, Eriksson, A A, Westermark, B B and Heldin, C H CH..  (1989)  cDNA cloning and expression of the human A-type platelet-derived growth factor (PDGF) receptor establishes structural similarity to the B-type PDGF receptor..  Proceedings of the National Academy of Sciences of the United States of America,      [PMID:2544881]
136. Matsui, T T and 6 more authors..  (1989)  Independent expression of human alpha or beta platelet-derived growth factor receptor cDNAs in a naive hematopoietic cell leads to functional coupling with mitogenic and chemotactic signaling pathways..  Proceedings of the National Academy of Sciences of the United States of America,      [PMID:2554309]
137. Eriksson, A A and 8 more authors..  (1995)  Demonstration of functionally different interactions between phospholipase C-gamma and the two types of platelet-derived growth factor receptors..  The Journal of biological chemistry,    (31):   [PMID:7535778]
138. Ebert, M M and 5 more authors..  (1995)  Induction of platelet-derived growth factor A and B chains and over-expression of their receptors in human pancreatic cancer..  International journal of cancer,    (4):   [PMID:7665222]
139. Fretto, L J LJ and 6 more authors..  (1993)  Mechanism of platelet-derived growth factor (PDGF) AA, AB, and BB binding to alpha and beta PDGF receptor..  The Journal of biological chemistry,    (15):   [PMID:7679113]
140. Craven, R J RJ and 8 more authors..  (1995)  Receptor tyrosine kinases expressed in metastatic colon cancer..  International journal of cancer,    (16):   [PMID:7896447]
141. Vassbotn, F S FS, Havnen, O K OK, Heldin, C H CH and Holmsen, H H..  (1994)  Negative feedback regulation of human platelets via autocrine activation of the platelet-derived growth factor alpha-receptor..  The Journal of biological chemistry,    (13):   [PMID:8188664]
142. Kawagishi, J J, Kumabe, T T, Yoshimoto, T T and Yamamoto, T T..  (1995)  Structure, organization, and transcription units of the human alpha-platelet-derived growth factor receptor gene, PDGFRA..  Genomics,    (20):   [PMID:8586421]
143. Yokote, K K and 6 more authors..  (1996)  Structural determinants in the platelet-derived growth factor alpha-receptor implicated in modulation of chemotaxis..  The Journal of biological chemistry,    (1):   [PMID:8617789]
144. Yokote, K K, Margolis, B B, Heldin, C H CH and Claesson-Welsh, L L..  (1996)  Grb7 is a downstream signaling component of platelet-derived growth factor alpha- and beta-receptors..  The Journal of biological chemistry,    (29):   [PMID:8940081]
145. Bazenet, C E CE, Gelderloos, J A JA and Kazlauskas, A A..  (1996)  Phosphorylation of tyrosine 720 in the platelet-derived growth factor alpha receptor is required for binding of Grb2 and SHP-2 but not for activation of Ras or cell proliferation..  Molecular and cellular biology,      [PMID:8943348]
146. Heldin, C H CH, Ostman, A A and Rönnstrand, L L..  (1998)  Signal transduction via platelet-derived growth factor receptors..  Biochimica et biophysica acta,    (19):   [PMID:9739761]
147. Abdiu, A A and 5 more authors..  (1998)  Human malignant fibrous histiocytomas in vitro: growth characteristics and their association with expression of mRNA for platelet-derived growth factor, transforming growth factor-alpha and their receptors..  European journal of cancer (Oxford, England : 1990),      [PMID:10070317]
148. Matsumoto, T T and 8 more authors..  (2000)  Differential interaction of CrkII adaptor protein with platelet-derived growth factor alpha- and beta-receptors is determined by its internal tyrosine phosphorylation..  Biochemical and biophysical research communications,    (2):   [PMID:10733900]
149. Rosenkranz, S S and 6 more authors..  (2000)  Src family kinases negatively regulate platelet-derived growth factor alpha receptor-dependent signaling and disease progression..  The Journal of biological chemistry,    (31):   [PMID:10734113]
150. Lindholm, C K CK, Frantz, J D JD, Shoelson, S E SE and Welsh, M M..  (2000)  Shf, a Shb-like adapter protein, is involved in PDGF-alpha-receptor regulation of apoptosis..  Biochemical and biophysical research communications,    (30):   [PMID:11095946]
151. Gilbertson, D G DG and 13 more authors..  (2001)  Platelet-derived growth factor C (PDGF-C), a novel growth factor that binds to PDGF alpha and beta receptor..  The Journal of biological chemistry,    (20):   [PMID:11297552]
152. Karthikeyan, Subramanian S, Leung, Teli T and Ladias, John A A JA..  (2002)  Structural determinants of the Na+/H+ exchanger regulatory factor interaction with the beta 2 adrenergic and platelet-derived growth factor receptors..  The Journal of biological chemistry,    (24):   [PMID:11882663]
153. Heinrich, Michael C MC and 12 more authors..  (2003)  PDGFRA activating mutations in gastrointestinal stromal tumors..  Science (New York, N.Y.),    (31):   [PMID:12522257]
154. Miller-Kasprzak, Ewa E, Niemir, Zofia I ZI and Czekalski, Stanisław S..  (2002)  [Structure and function of PDGF-R-alpha and its expression in normal kidney and kidney diseases]..  Przeglad lekarski,      [PMID:12632922]
155. Cools, Jan J and 25 more authors..  (2003)  A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome..  The New England journal of medicine,    (27):   [PMID:12660384]
156. Griffin, John H JH, Leung, Joey J, Bruner, Rebecca J RJ, Caligiuri, Michael A MA and Briesewitz, Roger R..  (2003)  Discovery of a fusion kinase in EOL-1 cells and idiopathic hypereosinophilic syndrome..  Proceedings of the National Academy of Sciences of the United States of America,    (24):   [PMID:12808148]
157. Chompret, Agnès A and 7 more authors..  (2004)  PDGFRA germline mutation in a family with multiple cases of gastrointestinal stromal tumor..  Gastroenterology,      [PMID:14699510]
158. Yi, Eunhee S ES, Strong, Curtis R CR, Piao, Zhe Z, Perucho, Manuel M and Weidner, Noel N..  (2005)  Epithelioid gastrointestinal stromal tumor with PDGFRA activating mutation and immunoreactivity..  Applied immunohistochemistry & molecular morphology : AIMM,      [PMID:15894928]
159. and Borbényi, Zita Z..  (2005)  [Disorders with eosinophilia, treatment of hypereosinophilic syndrome]..  Orvosi hetilap,    (1):   [PMID:15921304]
160. Corless, Christopher L CL and 9 more authors..  (2005)  PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib..  Journal of clinical oncology : official journal of the American Society of Clinical Oncology,    (10):   [PMID:15928335]
161. Chen, Lei L LL and 9 more authors..  (2005)  Imatinib resistance in gastrointestinal stromal tumors..  Current oncology reports,      [PMID:15946589]
162. and Tefferi, A A..  (2005)  Modern diagnosis and treatment of primary eosinophilia..  Acta haematologica,      [PMID:15995325]
163. Prenen, Hans H and 8 more authors..  (2006)  Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate..  Clinical cancer research : an official journal of the American Association for Cancer Research,    (15):   [PMID:16638875]
164. de Raedt, Thomas T and 10 more authors..  (2006)  Intestinal neurofibromatosis is a subtype of familial GIST and results from a dominant activating mutation in PDGFRA..  Gastroenterology,      [PMID:17087943]
165. Vantler, Marius M and 5 more authors..  (2006)  PI3-kinase/Akt-dependent antiapoptotic signaling by the PDGF alpha receptor is negatively regulated by Src family kinases..  FEBS letters,    (22):   [PMID:17141222]
166. Sonpavde, Guru G and Hutson, Thomas E TE..  (2007)  Pazopanib: a novel multitargeted tyrosine kinase inhibitor..  Current oncology reports,      [PMID:17288876]
167. Stock, Peggy P and 5 more authors..  (2007)  Platelet-derived growth factor receptor-alpha: a novel therapeutic target in human hepatocellular cancer..  Molecular cancer therapeutics,      [PMID:17604334]
168. Matsui, Junji J and 7 more authors..  (2008)  E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition..  International journal of cancer,    (1):   [PMID:17943726]
169. Feire, Adam L AL, Roy, René M RM, Manley, Kate K and Compton, Teresa T..  (2010)  The glycoprotein B disintegrin-like domain binds beta 1 integrin to mediate cytomegalovirus entry..  Journal of virology,      [PMID:20660204]
170. von Bubnoff, N N and 7 more authors..  (2011)  The low frequency of clinical resistance to PDGFR inhibitors in myeloid neoplasms with abnormalities of PDGFRA might be related to the limited repertoire of possible PDGFRA kinase domain mutations in vitro..  Oncogene,    (24):   [PMID:20972453]
171. Elling, Christian C and 13 more authors..  (2011)  Novel imatinib-sensitive PDGFRA-activating point mutations in hypereosinophilic syndrome induce growth factor independence and leukemia-like disease..  Blood,    (10):   [PMID:21224473]
172. Sévère, Nicolas N, Miraoui, Hichem H and Marie, Pierre J PJ..  (2011)  The Casitas B lineage lymphoma (Cbl) mutant G306E enhances osteogenic differentiation in human mesenchymal stromal cells in part by decreased Cbl-mediated platelet-derived growth factor receptor alpha and fibroblast growth factor receptor 2 ubiquitination..  The Journal of biological chemistry,    (8):   [PMID:21596750]
173. Doi, Toshihiko and 5 more authors..  (2014)  Phase I study of olaratumab in Japanese patients with advanced solid tumors..  Cancer science,      [PMID:24816152]
174. Ricci, Riccardo R and 10 more authors..  (2015)  PDGFRA-mutant syndrome..  Modern pathology : an official journal of the United States and Canadian Academy of Pathology, Inc,      [PMID:25975287]
175. Wu, Yiquan and 8 more authors..  (2017)  Human cytomegalovirus glycoprotein complex gH/gL/gO uses PDGFR-α as a key for entry..  PLoS pathogens,      [PMID:28403202]
176. Wind, Sven and 7 more authors..  (2019)  Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib..  Clinical pharmacokinetics,      [PMID:31016670]

Solution Calculators

Privacy Policy Website Terms of Use Return policy Terms and Conditions of Sale Cookie Policy Sales Policy
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Copyright © 2023-present Aladdin Scientific Corp . All rights reserved.