1. 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] |
2. Chen H, Ma J, Li W, Eliseenkova AV, Xu C, Neubert TA, Miller WT, Mohammadi M. (2007) A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases.. Mol Cell, 27 (5): (717-30). [PMID:17803937] |
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] |
4. Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M et al.. (2010) A structure-guided approach to creating covalent FGFR inhibitors.. Chem Biol, 17 (3): (285-95). [PMID:20338520] |
5. Greenman C, Stephens P, Smith R, Dalgliesh GL, Hunter C, Bignell G, Davies H, Teague J, Butler A, Stevens C et al.. (2007) Patterns of somatic mutation in human cancer genomes.. Nature, 446 (7132): (153-8). [PMID:17344846] |
6. 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] |
7. Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ et al.. (2006) Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.. J Med Chem, 49 (12): (3563-80). [PMID:16759099] |
8. Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H et al.. (2011) Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.. J Med Chem, 54 (20): (7066-83). [PMID:21936542] |
9. Cheng H, Li C, Bailey S, Baxi SM, Goulet L, Guo L, Hoffman J, Jiang Y, Johnson TO, Johnson TW et al.. (2013) Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.. ACS Med Chem Lett, 4 (1): (91-7). [PMID:24900568] |
10. Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H et al.. (2010) MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.. Cancer Res, 70 (4): (1524-33). [PMID:20145145] |
11. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.. Nat Chem Biol, 4 (11): (691-9). [PMID:18849971] |
12. Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q et al.. (2009) AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).. Blood, 114 (14): (2984-92). [PMID:19654408] |
13. Zhao G, Li WY, Chen D, Henry JR, Li HY, Chen Z, Zia-Ebrahimi M, Bloem L, Zhai Y, Huss K et al.. (2011) A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models.. Mol Cancer Ther, 10 (11): (2200-10). [PMID:21900693] |
14. Hall MD, Salam NK, Hellawell JL, Fales HM, Kensler CB, Ludwig JA, Szakács G, Hibbs DE, Gottesman MM. (2009) Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.. J Med Chem, 52 (10): (3191-204). [PMID:19397322] |
15. 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] |
16. Pandey A, Volkots DL, Seroogy JM, Rose JW, Yu JC, Lambing JL, Hutchaleelaha A, Hollenbach SJ, Abe K, Giese NA et al.. (2002) Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.. J Med Chem, 45 (17): (3772-93). [PMID:12166950] |
17. 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] |
18. Hennequin LF, Thomas AP, Johnstone C, Stokes ES, Plé PA, Lohmann JJ, Ogilvie DJ, Dukes M, Wedge SR, Curwen JO et al.. (1999) Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.. J Med Chem, 42 (26): (5369-89). [PMID:10639280] |
19. Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N et al.. (2015) First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway.. Cancer Discov, 5 (4): (424-37). [PMID:25776529] |
20. Cai X, Zhai HX, Wang J, Forrester J, Qu H, Yin L, Lai CJ, Bao R, Qian C. (2010) Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.. J Med Chem, 53 (5): (2000-9). [PMID:20143778] |
21. Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J et al.. (2009) Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.. J Med Chem, 52 (20): (6362-8). [PMID:19827834] |
22. Hobson AD, Harris CM, van der Kam EL, Turner SC, Abibi A, Aguirre AL, Bousquet P, Kebede T, Konopacki DB, Gintant G et al.. (2015) Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.. J Med Chem, 58 (23): (9154-70). [PMID:26509640] |
23. Yeh BK, Igarashi M, Eliseenkova AV, Plotnikov AN, Sher I, Ron D, Aaronson SA, Mohammadi M. (2003) Structural basis by which alternative splicing confers specificity in fibroblast growth factor receptors.. Proc Natl Acad Sci USA, 100 (5): (2266-71). [PMID:12591959] |
24. Hall TG, Yu Y, Eathiraj S, Wang Y, Savage RE, Lapierre JM, Schwartz B, Abbadessa G. (2016) Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation.. PLoS ONE, 11 (9): (e0162594). [PMID:27627808] |
25. Brameld KA, Owens TD, Verner E, Venetsanakos E, Bradshaw JM, Phan VT, Tam D, Leung K, Shu J, LaStant J et al.. (2017) Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.. J Med Chem, 60 (15): (6516-6527). [PMID:28665128] |
26. 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] |
27. 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] |
28. 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] |
29. Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E et al.. (2020) Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.. J Med Chem, 129 (3): (589-97). [PMID:32787110] |
30. Xiang H, Liu L, Gao Y, Ahene A, Macal M, Hsu AW, Dreiling L, Collins H. (2020) Population pharmacokinetic analysis of phase 1 bemarituzumab data to support phase 2 gastroesophageal adenocarcinoma FIGHT trial.. Cancer Chemother Pharmacol, 86 (5): (595-606). [PMID:32965540] |
31. Tsimafeyeu I, Ludes-Meyers J, Stepanova E, Daeyaert F, Khochenkov D, Joose JB, Solomko E, Van Akene K, Peretolchina N, Yin W et al.. (2016) Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models.. Eur J Cancer, 61 (3): (20-8). [PMID:27136102] |
32. Kurosu H, Choi M, Ogawa Y, Dickson AS, Goetz R, Eliseenkova AV, Mohammadi M, Rosenblatt KP, Kliewer SA, Kuro-O M. (2007) Tissue-specific expression of betaKlotho and fibroblast growth factor (FGF) receptor isoforms determines metabolic activity of FGF19 and FGF21.. J Biol Chem, 282 (37): (26687-26695). [PMID:17623664] |
33. 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] |
34. 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] |
35. Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Rucklin G.. (2004) SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.. Bioorg Med Chem Lett, 14 (13): (3601-3605). [PMID:15177483] |
36. Rewcastle GW, Murray DK, Elliott WL, Fry DW, Howard CT, Nelson JM, Roberts BJ, Vincent PW, Showalter HD, Winters RT, Denny WA.. (1998) Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.. J Med Chem, 41 (5): (742-751). [PMID:9513602] |
37. Borzilleri RM, Zheng X, Qian L, Ellis C, Cai ZW, Wautlet BS, Mortillo S, Jeyaseelan R, Kukral DW, Fura A, Kamath A, Vyas V, Tokarski JS, Barrish JC, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS.. (2005) Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.. J Med Chem, 48 (12): (3991-4008). [PMID:15943473] |
38. Kuo GH, Prouty C, Wang A, Emanuel S, Deangelis A, Zhang Y, Song F, Beall L, Connolly PJ, Karnachi P, Chen X, Gruninger RH, Sechler J, Fuentes-Pesquera A, Middleton SA, Jolliffe L, Murray WV.. (2005) Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.. J Med Chem, 48 (15): (4892-4909). [PMID:16033269] |
39. 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] |
40. 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] |
41. Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Neumann U, Rucklin G.. (2006) Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.. Bioorg Med Chem Lett, 16 (2): (262-266). [PMID:16249085] |
42. 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] |
43. Zhao H, Serby MD, Xin Z, Szczepankiewicz BG, Liu M, Kosogof C, Liu B, Nelson LT, Johnson EF, Wang S, Pederson T, Gum RJ, Clampit JE, Haasch DL, Abad-Zapatero C, Fry EH, Rondinone C, Trevillyan JM, Sham HL, Liu G.. (2006) Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.. J Med Chem, 49 (15): (4455-4458). [PMID:16854050] |
44. Potashman MH, Bready J, Coxon A, DeMelfi TM, DiPietro L, Doerr N, Elbaum D, Estrada J, Gallant P, Germain J, Gu Y, Harmange JC, Kaufman SA, Kendall R, Kim JL, Kumar GN, Long AM, Neervannan S, Patel VF, Polverino A, Rose P, Plas Sv, Whittington D, Zanon R, Zhao H.. (2007) Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors.. J Med Chem, 50 (18): (4351-4373). [PMID:17696416] |
45. 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] |
46. Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P.. (2008) Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.. J Med Chem, 51 (21): (6642-6645). [PMID:18834107] |
47. D'Angelo ND, Bellon SF, Booker SK, Cheng Y, Coxon A, Dominguez C, Fellows I, Hoffman D, Hungate R, Kaplan-Lefko P, Lee MR, Li C, Liu L, Rainbeau E, Reider PJ, Rex K, Siegmund A, Sun Y, Tasker AS, Xi N, Xu S, Yang Y, Zhang Y, Burgess TL, Dussault I, Kim TS.. (2008) Design, synthesis, and biological evaluation of potent c-Met inhibitors.. J Med Chem, 51 (18): (5766-5779). [PMID:18763753] |
48. 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] |
49. 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] |
50. 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] |
51. Qiao L, Choi S, Case A, Gainer TG, Seyb K, Glicksman MA, Lo DC, Stein RL, Cuny GD.. (2009) Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors.. Bioorg Med Chem Lett, 19 (21): (6122-6126). [PMID:19783434] |
52. Deng X, Lim SM, Zhang J, Gray NS.. (2010) Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.. Bioorg Med Chem Lett, 20 (14): (4196-4200). [PMID:20541934] |
53. Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I.. (2011) Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.. Bioorg Med Chem Lett, 21 (1): (315-319). [PMID:21112785] |
54. Kim H, Kim M, Lee J, Yu H, Hah JM.. (2011) Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.. Bioorg Med Chem, 19 (22): (6760-6767). [PMID:22014755] |
55. Cuny GD, Ulyanova NP, Patnaik D, Liu JF, Lin X, Auerbach K, Ray SS, Xian J, Glicksman MA, Stein RL, Higgins JM.. (2012) Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors.. Bioorg Med Chem Lett, 22 (5): (2015-2019). [PMID:22335895] |
56. Lo Monte F, Kramer T, Gu J, Anumala UR, Marinelli L, La Pietra V, Novellino E, Franco B, Demedts D, Van Leuven F, Fuertes A, Dominguez JM, Plotkin B, Eldar-Finkelman H, Schmidt B.. (2012) Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3α.. J Med Chem, 55 (9): (4407-4424). [PMID:22533818] |
57. Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE.. (2011) Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).. J Med Chem, 54 (22): (7860-7883). [PMID:22039836] |
58. Reith AD, Bamborough P, Jandu K, Andreotti D, Mensah L, Dossang P, Choi HG, Deng X, Zhang J, Alessi DR, Gray NS.. (2012) GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.. Bioorg Med Chem Lett, 22 (17): (5625-5629). [PMID:22863203] |
59. Amombo GM, Kramer T, Lo Monte F, Göring S, Fach M, Smith S, Kolb S, Schubenel R, Baumann K, Schmidt B.. (2012) Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3.. Bioorg Med Chem Lett, 22 (24): (7634-7640). [PMID:23107479] |
60. 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] |
61. 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] |
62. Kusakabe K, Ide N, Daigo Y, Tachibana Y, Itoh T, Yamamoto T, Hashizume H, Hato Y, Higashino K, Okano Y, Sato Y, Inoue M, Iguchi M, Kanazawa T, Ishioka Y, Dohi K, Kido Y, Sakamoto S, Yasuo K, Maeda M, Higaki M, Ueda K, Yoshizawa H, Baba Y, Shiota T, Murai H, Nakamura Y.. (2013) Indazole-based potent and cell-active Mps1 kinase inhibitors: rational design from pan-kinase inhibitor anthrapyrazolone (SP600125).. J Med Chem, 56 (11): (4343-4356). [PMID:23634759] |
63. Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Pandya D, Diep L, Fitzgerald K, Artis DR, Anderson JP, Bergeron M.. (2013) Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.. Bioorg Med Chem Lett, 23 (9): (2743-2749). [PMID:23522834] |
64. Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB.. (2014) Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.. Bioorg Med Chem Lett, 24 (12): (2635-2639). [PMID:24813737] |
65. Horbert R, Pinchuk B, Johannes E, Schlosser J, Schmidt D, Cappel D, Totzke F, Schächtele C, Peifer C.. (2015) Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorβ (PDGF-Rβ) guided by water thermodynamics.. J Med Chem, 58 (1): (170-182). [PMID:25007344] |
66. 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] |
67. 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] |
68. 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] |
69. Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L.. (2015) Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.. Bioorg Med Chem, 23 (21): (7000-7006). [PMID:26455654] |
70. Aman W, Lee J, Kim M, Yang S, Jung H, Hah JM.. (2016) Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.. Bioorg Med Chem Lett, 26 (4): (1188-1192). [PMID:26810260] |
71. Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J.. (2016) Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.. Bioorg Med Chem Lett, 26 (5): (1443-1451). [PMID:26852363] |
72. Fan J, Dai Y, Shao J, Peng X, Wang C, Cao S, Zhao B, Ai J, Geng M, Duan W.. (2016) Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors.. Bioorg Med Chem Lett, 26 (11): (2594-2599). [PMID:27117427] |
73. Cherian J, Nacro K, Poh ZY, Guo S, Jeyaraj DA, Wong YX, Ho M, Yang HY, Joy JK, Kwek ZP, Liu B, Wee JL, Ong EH, Choong ML, Poulsen A, Lee MA, Pendharkar V, Ding LJ, Manoharan V, Chew YS, Sangthongpitag K, Lim S, Ong ST, Hill J, Keller TH.. (2016) Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.. J Med Chem, 59 (7): (3063-3078). [PMID:27011159] |
74. 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] |
75. 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] |
76. Fu J, Xia A, Qi X.. (2016) Identification of novel peptoid agonists of fibroblast growth factor receptor using microarray-based screening.. Medchemcomm, 7 (6): (1183-1189). [PMID:27721968] |
77. 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] |
78. Zhang Y, Chen Y, Zhang D, Wang L, Lu T, Jiao Y.. (2018) Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines.. J Med Chem, 61 (1): (140-157). [PMID:29189002] |
79. Fukuda T, Goto R, Kiho T, Ueda K, Muramatsu S, Hashimoto M, Aki A, Watanabe K, Tanaka N.. (2017) Discovery of DS79182026: A potent orally active hepcidin production inhibitor.. Bioorg Med Chem Lett, 27 (16): (3716-3722). [PMID:28705644] |
80. 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] |
81. 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] |
82. Cho H, Shin I, Ju E, Choi S, Hur W, Kim H, Hong E, Kim ND, Choi HG, Gray NS, Sim T.. (2018) First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.. J Med Chem, 61 (18): (8353-8373). [PMID:30153003] |
83. Assadieskandar A, Yu C, Maisonneuve P, Liu X, Chen YC, Prakash GKS, Kurinov I, Sicheri F, Zhang C.. (2018) Effects of rigidity on the selectivity of protein kinase inhibitors.. Eur J Med Chem, 146 (519-528). [PMID:29407977] |
84. Wang Q, Liu F, Qi S, Qi Z, Yan XE, Wang B, Wang A, Wang W, Chen C, Liu X, Jiang Z, Hu Z, Wang L, Wang W, Ren T, Zhang S, Yun CH, Liu Q, Liu J.. (2018) Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia.. Eur J Med Chem, 150 (366-384). [PMID:29544149] |
85. He LJ, Yang DL, Li SQ, Zhang YJ, Tang Y, Lei J, Frett B, Lin HK, Li HY, Chen ZZ, Xu ZG.. (2018) Facile construction of fused benzimidazole-isoquinolinones that induce cell-cycle arrest and apoptosis in colorectal cancer cells.. Bioorg Med Chem, 26 (14): (3899-3908). [PMID:29921474] |
86. Jiang JK, Huang X, Shamim K, Patel PR, Lee A, Wang AQ, Nguyen K, Tawa G, Cuny GD, Yu PB, Zheng W, Xu X, Sanderson P, Huang W.. (2018) Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.. Bioorg Med Chem Lett, 28 (20): (3356-3362). [PMID:30227946] |
87. Wang B, Wu J, Wu Y, Chen C, Zou F, Wang A, Wu H, Hu Z, Jiang Z, Liu Q, Wang W, Zhang Y, Liu F, Zhao M, Hu J, Huang T, Ge J, Wang L, Ren T, Wang Y, Liu J, Liu Q.. (2018) Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.. Eur J Med Chem, 158 (896-916). [PMID:30253346] |
88. 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] |
89. Dodo K, Kuboki E, Shimizu T, Imamura R, Magarisawa M, Takahashi M, Tokuhiro T, Yotsumoto S, Asano K, Nakao S, Terayama N, Suda T, Tanaka M, Sodeoka M.. (2019) Development of a Water-Soluble Indolylmaleimide Derivative IM-93 Showing Dual Inhibition of Ferroptosis and NETosis.. ACS Med Chem Lett, 10 (9): (1272-1278). [PMID:31531196] |
90. Zhang Q, Hu X, Wan G, Wang J, Li L, Wu X, Liu Z, Yu L.. (2019) Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.. Eur J Med Chem, 184 (111728-111728). [PMID:31610375] |
91. 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] |
92. Narayan S, Ramisetti S, Jaiswal AS, Law BK, Singh-Pillay A, Singh P, Amin S, Sharma AK.. (2019) ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.. Eur J Med Chem, 161 (456-467). [PMID:30384048] |
93. Wang L, Zhang Y, Zhang Q, Zhu G, Zhang Z, Duan C, Lu T, Tang W.. (2019) Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.. Eur J Med Chem, 163 (243-255). [PMID:30529543] |
94. Wang Y, Dou X, Jiang L, Jin H, Zhang L, Zhang L, Liu Z.. (2019) Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia.. Eur J Med Chem, 171 (221-234). [PMID:30925338] |
95. Liang X, Zang J, Li X, Tang S, Huang M, Geng M, Chou CJ, Li C, Cao Y, Xu W, Liu H, Zhang Y.. (2019) Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.. J Med Chem, 62 (8): (3898-3923). [PMID:30901208] |
96. Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW.. (2019) Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.. J Med Chem, 62 (10): (5096-5110). [PMID:31013427] |
97. Lin X, Yosaatmadja Y, Kalyukina M, Middleditch MJ, Zhang Z, Lu X, Ding K, Patterson AV, Smaill JB, Squire CJ.. (2019) Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4.. ACS Med Chem Lett, 10 (8): (1180-1186). [PMID:31413803] |
98. Wang X, Yu C, Wang C, Ma Y, Wang T, Li Y, Huang Z, Zhou M, Sun P, Zheng J, Yang S, Fan Y, Xiang R.. (2019) Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.. Eur J Med Chem, 181 (111535-111535). [PMID:31376566] |
99. Zhao L, Li Y, Wang Y, Qiao Z, Miao Z, Yang J, Huang L, Tian C, Li L, Chen D, Yang S.. (2019) Discovery of 4H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models.. J Med Chem, 62 (23): (10691-10710). [PMID:31693351] |
100. Jang J, Son JB, To C, Bahcall M, Kim SY, Kang SY, Mushajiang M, Lee Y, Jänne PA, Choi HG, Gray NS.. (2017) Discovery of a potent dual ALK and EGFR T790M inhibitor.. Eur J Med Chem, 136 (497-510). [PMID:28528303] |
101. 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] |
102. Oukoloff K, Coquelle N, Bartolini M, Naldi M, Le Guevel R, Bach S, Josselin B, Ruchaud S, Catto M, Pisani L, Denora N, Iacobazzi RM, Silman I, Sussman JL, Buron F, Colletier JP, Jean L, Routier S, Renard PY.. (2019) Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3.. Eur J Med Chem, 168 (58-77). [PMID:30798053] |
103. Heider F, Ansideri F, Tesch R, Pantsar T, Haun U, Döring E, Kudolo M, Poso A, Albrecht W, Laufer SA, Koch P.. (2019) Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors.. Eur J Med Chem, 175 (309-329). [PMID:31096153] |
104. Lu X, Chen H, Patterson AV, Smaill JB, Ding K.. (2019) Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects.. J Med Chem, 62 (6): (2905-2915). [PMID:30403487] |
105. 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] |
106. 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] |
107. Kuriwaki I, Kameda M, Hisamichi H, Kikuchi S, Iikubo K, Kawamoto Y, Moritomo H, Kondoh Y, Amano Y, Tateishi Y, Echizen Y, Iwai Y, Noda A, Tomiyama H, Suzuki T, Hirano M.. (2020) Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2.. Bioorg Med Chem, 28 (10): (115453-115453). [PMID:32278710] |
108. Rezende Miranda R,Fu Y,Chen X,Perino J,Cao P,Carpten J,Chen Y,Zhang C. (2020) Development of a Potent and Specific FGFR4 Inhibitor for the Treatment of Hepatocellular Carcinoma.. J Med Chem, 63 (20): (11484-11497). [PMID:33030342] |
109. Yan G,Zhong X,Pu C,Yue L,Shan H,Lan S,Zhou M,Hou X,Yang J,Li D,Fan S,Li R. (2021) Targeting Cysteine Located Outside the Active Site: An Effective Strategy for Covalent ALKi Design.. J Med Chem, 64 (3.0): (1558-1569). [PMID:33471528] |
110. Ding X,Stasi LP,Ho MH,Zhao B,Wang H,Long K,Xu Q,Sang Y,Sun C,Hu H,Yu H,Wan Z,Wang L,Edge C,Liu Q,Li Y,Dong K,Guan X,Tattersall FD,Reith AD,Ren F. (2018) Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors.. Bioorg Med Chem Lett, 28 (9.0): (1615-1620). [PMID:29588215] |
111. Fairhurst RA,Knoepfel T,Buschmann N,Leblanc C,Mah R,Todorov M,Nimsgern P,Ripoche S,Niklaus M,Warin N,Luu VH,Madoerin M,Wirth J,Graus-Porta D,Weiss A,Kiffe M,Wartmann M,Kinyamu-Akunda J,Sterker D,Stamm C,Adler F,Buhles A,Schadt H,Couttet P,Blank J,Galuba I,Trappe J,Voshol J,Ostermann N,Zou C,Berghausen J,Del Rio Espinola A,Jahnke W,Furet P. (2020) Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.. J Med Chem, 63 (21.0): (12542-12573). [PMID:32930584] |
112. Kuriwaki I,Kameda M,Iikubo K,Hisamichi H,Kawamoto Y,Kikuchi S,Moritomo H,Kondoh Y,Terasaka T,Amano Y,Tateishi Y,Echizen Y,Iwai Y,Noda A,Tomiyama H,Nakazawa T,Hirano M. (2021) Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency.. Bioorg Med Chem, 33 (116019-116019). [PMID:33486159] |
113. Liu H,Niu D,Tham Sjin RT,Dubrovskiy A,Zhu Z,McDonald JJ,Fahnoe K,Wang Z,Munson M,Scholte A,Barrague M,Fitzgerald M,Liu J,Kothe M,Sun F,Murtie J,Ge J,Rocnik J,Harvey D,Ospina B,Perron K,Zheng G,Shehu E,D'Agostino LA. (2020) Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma.. ACS Med Chem Lett, 11 (10): (1899-1904). [PMID:33062171] |
114. Chen X,Liu Y,Zhang L,Chen D,Dong Z,Zhao C,Liu Z,Xia Q,Wu J,Chen Y,Zheng X,Cai Y. (2021) Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer.. Eur J Med Chem, 214 (113219-113219). [PMID:33618175] |
115. Yang J,Chen K,Zhang G,Yang QY,Li YS,Huang SZ,Wang YL,Yang W,Jiang XJ,Yan HX,Zhu JQ,Xiang R,Luo YF,Li WM,Wei YQ,Li LL,Yang SY. (2018) Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.. Eur J Med Chem, 143 (1148-1164). [PMID:29133048] |
116. Liang X, Tang S, Liu X, Liu Y, Xu Q, Wang X, Saidahmatov A, Li C, Wang J, Zhou Y, Zhang Y, Geng M, Huang M, Liu H.. (2022) Discovery of Novel Pyrrolo[2,3-d]pyrimidine-based Derivatives as Potent JAK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors.. J Med Chem, 65 (2.0): (1243-1264). [PMID:33586434] |
117. Miki, T T and 6 more authors.. (1992) Determination of ligand-binding specificity by alternative splicing: two distinct growth factor receptors encoded by a single gene.. Proceedings of the National Academy of Sciences of the United States of America, (1): [PMID:1309608] |
118. Dell, K R KR and Williams, L T LT.. (1992) A novel form of fibroblast growth factor receptor 2. Alternative splicing of the third immunoglobulin-like domain confers ligand binding specificity.. The Journal of biological chemistry, (15): [PMID:1400433] |
119. Seno, M M, Sasada, R R, Watanabe, T T, Ishimaru, K K and Igarashi, K K.. (1991) Two cDNAs encoding novel human FGF receptor.. Biochimica et biophysica acta, (13): [PMID:1647213] |
120. Dionne, C A CA and 8 more authors.. (1990) Cloning and expression of two distinct high-affinity receptors cross-reacting with acidic and basic fibroblast growth factors.. The EMBO journal, [PMID:1697263] |
121. Houssaint, E E and 6 more authors.. (1990) Related fibroblast growth factor receptor genes exist in the human genome.. Proceedings of the National Academy of Sciences of the United States of America, [PMID:2172978] |
122. Hattori, Y Y and 9 more authors.. (1990) K-sam, an amplified gene in stomach cancer, is a member of the heparin-binding growth factor receptor genes.. Proceedings of the National Academy of Sciences of the United States of America, [PMID:2377625] |
123. Gorry, M C MC and 9 more authors.. (1995) Crouzon syndrome: mutations in two spliceoforms of FGFR2 and a common point mutation shared with Jackson-Weiss syndrome.. Human molecular genetics, [PMID:7581378] |
124. Oldridge, M M and 9 more authors.. (1995) Mutations in the third immunoglobulin domain of the fibroblast growth factor receptor-2 gene in Crouzon syndrome.. Human molecular genetics, [PMID:7655462] |
125. Park, W J WJ and 7 more authors.. (1995) Analysis of phenotypic features and FGFR2 mutations in Apert syndrome.. American journal of human genetics, [PMID:7668257] |
126. Lajeunie, E E and 5 more authors.. (1995) FGFR2 mutations in Pfeiffer syndrome.. Nature genetics, [PMID:7719333] |
127. Wilkie, A O AO and 9 more authors.. (1995) Apert syndrome results from localized mutations of FGFR2 and is allelic with Crouzon syndrome.. Nature genetics, [PMID:7719344] |
128. Rutland, P P and 9 more authors.. (1995) Identical mutations in the FGFR2 gene cause both Pfeiffer and Crouzon syndrome phenotypes.. Nature genetics, [PMID:7719345] |
129. Wilson, S E SE and 5 more authors.. (1994) Hepatocyte growth factor (HGF), keratinocyte growth factor (KGF), and their receptors in human breast cells and tissues: alternative receptors.. Cellular & molecular biology research, [PMID:7866434] |
130. Jabs, E W EW and 9 more authors.. (1994) Jackson-Weiss and Crouzon syndromes are allelic with mutations in fibroblast growth factor receptor 2.. Nature genetics, [PMID:7874170] |
131. Reardon, W W and 5 more authors.. (1994) Mutations in the fibroblast growth factor receptor 2 gene cause Crouzon syndrome.. Nature genetics, [PMID:7987400] |
132. Park, W J WJ and 7 more authors.. (1995) Novel FGFR2 mutations in Crouzon and Jackson-Weiss syndromes show allelic heterogeneity and phenotypic variability.. Human molecular genetics, [PMID:8528214] |
133. Meyers, G A GA and 11 more authors.. (1996) FGFR2 exon IIIa and IIIc mutations in Crouzon, Jackson-Weiss, and Pfeiffer syndromes: evidence for missense changes, insertions, and a deletion due to alternative RNA splicing.. American journal of human genetics, [PMID:8644708] |
134. Moloney, D M DM and 6 more authors.. (1996) Exclusive paternal origin of new mutations in Apert syndrome.. Nature genetics, [PMID:8673103] |
135. Wada, C C and 7 more authors.. (1996) [Nucleotide sequences at intron 6 and exon 7 junction of fibroblast growth factor receptor 2 and rapid mutational analysis in Apert syndrome].. Rinsho byori. The Japanese journal of clinical pathology, [PMID:8676562] |
136. Przylepa, K A KA and 11 more authors.. (1996) Fibroblast growth factor receptor 2 mutations in Beare-Stevenson cutis gyrata syndrome.. Nature genetics, [PMID:8696350] |
137. Steinberger, D D, Mulliken, J B JB and Müller, U U.. (1996) Crouzon syndrome: previously unrecognized deletion, duplication, and point mutation within FGFR2 gene.. Human mutation, [PMID:8956050] |
138. Oldridge, M M and 12 more authors.. (1997) Genotype-phenotype correlation for nucleotide substitutions in the IgII-IgIII linker of FGFR2.. Human molecular genetics, [PMID:9002682] |
139. Tartaglia, M M, Valeri, S S, Velardi, F F, Di Rocco, C C and Battaglia, P A PA.. (1997) Trp290Cys mutation in exon IIIa of the fibroblast growth factor receptor 2 (FGFR2) gene is associated with Pfeiffer syndrome.. Human genetics, [PMID:9150725] |
140. Steinberger, D D, Collmann, H H, Schmalenberger, B B and Müller, U U.. (1997) A novel mutation (a886g) in exon 5 of FGFR2 in members of a family with Crouzon phenotype and plagiocephaly.. Journal of medical genetics, [PMID:9152842] |
141. Tartaglia, M M and 5 more authors.. (1997) Jackson-Weiss syndrome: identification of two novel FGFR2 missense mutations shared with Crouzon and Pfeiffer craniosynostotic disorders.. Human genetics, [PMID:9385368] |
142. Tsai, F J FJ and 5 more authors.. (1998) Two common mutations 934C to G and 937C to G of fibroblast growth factor receptor 2 (FGFR2) gene in Chinese patients with Apert syndrome.. Human mutation, [PMID:9452027] |
143. Steinberger, D D, Vriend, G G, Mulliken, J B JB and Müller, U U.. (1998) The mutations in FGFR2-associated craniosynostoses are clustered in five structural elements of immunoglobulin-like domain III of the receptor.. Human genetics, [PMID:9521581] |
144. Paznekas, W A WA and 12 more authors.. (1998) Genetic heterogeneity of Saethre-Chotzen syndrome, due to TWIST and FGFR mutations.. American journal of human genetics, [PMID:9585583] |
145. Passos-Bueno, M R MR and 7 more authors.. (1998) Description of a new mutation and characterization of FGFR1, FGFR2, and FGFR3 mutations among Brazilian patients with syndromic craniosynostoses.. American journal of medical genetics, (7): [PMID:9677057] |
146. Mathijssen, I M IM, Vaandrager, J M JM, Hoogeboom, A J AJ, Hesseling-Janssen, A L AL and van den Ouweland, A M AM.. (1998) Pfeiffer's syndrome resulting from an S351C mutation in the fibroblast growth factor receptor-2 gene.. The Journal of craniofacial surgery, [PMID:9693549] |
147. Passos-Bueno, M R MR, Richieri-Costa, A A, Sertié, A L AL and Kneppers, A A.. (1998) Presence of the Apert canonical S252W FGFR2 mutation in a patient without severe syndactyly.. Journal of medical genetics, [PMID:9719378] |
148. Zhang, Y Y, Gorry, M C MC, Post, J C JC and Ehrlich, G D GD.. (1999) Genomic organization of the human fibroblast growth factor receptor 2 (FGFR2) gene and comparative analysis of the human FGFR gene family.. Gene, (1): [PMID:10196476] |
149. Cornejo-Roldan, L R LR, Roessler, E E and Muenke, M M.. (1999) Analysis of the mutational spectrum of the FGFR2 gene in Pfeiffer syndrome.. Human genetics, [PMID:10394936] |
150. Everett, E T ET, Britto, D A DA, Ward, R E RE and Hartsfield, J K JK.. (1999) A novel FGFR2 gene mutation in Crouzon syndrome associated with apparent nonpenetrance.. The Cleft palate-craniofacial journal : official publication of the American Cleft Palate-Craniofacial Association, [PMID:10574673] |
151. Stauber, D J DJ, DiGabriele, A D AD and Hendrickson, W A WA.. (2000) Structural interactions of fibroblast growth factor receptor with its ligands.. Proceedings of the National Academy of Sciences of the United States of America, (4): [PMID:10618369] |
152. Ueda, T T and 10 more authors.. (1999) Deletion of the carboxyl-terminal exons of K-sam/FGFR2 by short homology-mediated recombination, generating preferential expression of specific messenger RNAs.. Cancer research, (15): [PMID:10626794] |
153. Reardon, W W and 16 more authors.. (2000) Evidence for digenic inheritance in some cases of Antley-Bixler syndrome?. Journal of medical genetics, [PMID:10633130] |
154. Glaser, R L RL and 11 more authors.. (2000) Paternal origin of FGFR2 mutations in sporadic cases of Crouzon syndrome and Pfeiffer syndrome.. American journal of human genetics, [PMID:10712195] |
155. Plotnikov, A N AN, Hubbard, S R SR, Schlessinger, J J and Mohammadi, M M.. (2000) Crystal structures of two FGF-FGFR complexes reveal the determinants of ligand-receptor specificity.. Cell, (12): [PMID:10830168] |
156. Priolo, M M and 7 more authors.. (2000) Pfeiffer syndrome type 2 associated with a single amino acid deletion in the FGFR2 gene.. Clinical genetics, [PMID:10945669] |
157. Johnson, D D, Wall, S A SA, Mann, S S and Wilkie, A O AO.. (2000) A novel mutation, Ala315Ser, in FGFR2: a gene-environment interaction leading to craniosynostosis?. European journal of human genetics : EJHG, [PMID:10951518] |
158. Pellegrini, L L, Burke, D F DF, von Delft, F F, Mulloy, B B and Blundell, T L TL.. (2000) Crystal structure of fibroblast growth factor receptor ectodomain bound to ligand and heparin.. Nature, (26): [PMID:11069186] |
159. Kress, W W, Collmann, H H, Büsse, M M, Halliger-Keller, B B and Mueller, C R CR.. (2000) Clustering of FGFR2 gene mutations inpatients with Pfeiffer and Crouzon syndromes (FGFR2-associated craniosynostoses).. Cytogenetics and cell genetics, [PMID:11173845] |
160. Tsai, F J FJ, Yang, C F CF, Wu, J Y JY, Tsai, C H CH and Lee, C C CC.. (2001) Mutation analysis of Crouzon syndrome and identification of one novel mutation in Taiwanese patients.. Pediatrics international : official journal of the Japan Pediatric Society, [PMID:11380921] |
161. Ibrahimi, O A OA and 5 more authors.. (2001) Structural basis for fibroblast growth factor receptor 2 activation in Apert syndrome.. Proceedings of the National Academy of Sciences of the United States of America, (19): [PMID:11390973] |
162. Chen, X X, Ji, Z L ZL and Chen, Y Z YZ.. (2002) TTD: Therapeutic Target Database.. Nucleic acids research, (1): [PMID:11752352] |
163. Kan, Shih-hsin SH and 14 more authors.. (2002) Genomic screening of fibroblast growth-factor receptor 2 reveals a wide spectrum of mutations in patients with syndromic craniosynostosis.. American journal of human genetics, [PMID:11781872] |
164. Ingersoll, R G RG and 5 more authors.. (2001) Fibroblast growth factor receptor 2 (FGFR2): genomic sequence and variations.. Cytogenetics and cell genetics, [PMID:11856867] |
165. Wang, T-J TJ and 5 more authors.. (2002) Mutation in the FGFR2 gene in a Taiwanese patient with Beare-Stevenson cutis gyrata syndrome.. Clinical genetics, [PMID:12000365] |
166. Lu, Yunbiao Y, Pan, Zhong-Zong ZZ, Devaux, Yvan Y and Ray, Prabir P.. (2003) p21-activated protein kinase 4 (PAK4) interacts with the keratinocyte growth factor receptor and participates in keratinocyte growth factor-mediated inhibition of oxidant-induced cell death.. The Journal of biological chemistry, (21): [PMID:12529371] |
167. Deloukas, P P and 135 more authors.. (2004) The DNA sequence and comparative analysis of human chromosome 10.. Nature, (27): [PMID:15164054] |
168. Kaabeche, Karim K, Lemonnier, Jérome J, Le Mée, Sandrine S, Caverzasio, Joseph J and Marie, Pierre J PJ.. (2004) Cbl-mediated degradation of Lyn and Fyn induced by constitutive fibroblast growth factor receptor-2 activation supports osteoblast differentiation.. The Journal of biological chemistry, (27): [PMID:15190072] |
169. Ceridono, Mara M, Belleudi, Francesca F, Ceccarelli, Simona S and Torrisi, Maria Rosaria MR.. (2005) Tyrosine 769 of the keratinocyte growth factor receptor is required for receptor signaling but not endocytosis.. Biochemical and biophysical research communications, (11): [PMID:15629145] |
170. Eswarakumar, V P VP, Lax, I I and Schlessinger, J J.. (2005) Cellular signaling by fibroblast growth factor receptors.. Cytokine & growth factor reviews, [PMID:15863030] |
171. McGillivray, G G and 9 more authors.. (2005) Familial scaphocephaly syndrome caused by a novel mutation in the FGFR2 tyrosine kinase domain.. Journal of medical genetics, [PMID:16061565] |
172. Robinson, Christopher J CJ, Harmer, Nicholas J NJ, Goodger, Sarah J SJ, Blundell, Tom L TL and Gallagher, John T JT.. (2005) Cooperative dimerization of fibroblast growth factor 1 (FGF1) upon a single heparin saccharide may drive the formation of 2:2:1 FGF1.FGFR2c.heparin ternary complexes.. The Journal of biological chemistry, (23): [PMID:16219767] |
173. Olsen, Shaun K SK and 9 more authors.. (2006) Structural basis by which alternative splicing modulates the organizer activity of FGF8 in the brain.. Genes & development, (15): [PMID:16384934] |
174. Radtke, Michelle L ML and Kolesar, Jill M JM.. (2005) Palifermin (Kepivance) for the treatment of oral mucositis in patients with hematologic malignancies requiring hematopoietic stem cell support.. Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, [PMID:16390600] |
175. Rohmann, Edyta E and 21 more authors.. (2006) Mutations in different components of FGF signaling in LADD syndrome.. Nature genetics, [PMID:16501574] |
176. Zhang, Xiuqin X and 5 more authors.. (2006) Receptor specificity of the fibroblast growth factor family. The complete mammalian FGF family.. The Journal of biological chemistry, (9): [PMID:16597617] |
177. Hatch, Nan E NE, Hudson, Mark M, Seto, Marianne L ML, Cunningham, Michael L ML and Bothwell, Mark M.. (2006) Intracellular retention, degradation, and signaling of glycosylation-deficient FGFR2 and craniosynostosis syndrome-associated FGFR2C278F.. The Journal of biological chemistry, (15): [PMID:16844695] |
178. Huang, Yi-Wen YW and 6 more authors.. (2006) Effect of keratinocyte growth factor on cell viability in primary cultured human prostate cancer stromal cells.. The Journal of steroid biochemistry and molecular biology, [PMID:16854582] |
179. Sjöblom, Tobias T and 28 more authors.. (2006) The consensus coding sequences of human breast and colorectal cancers.. Science (New York, N.Y.), (13): [PMID:16959974] |
180. Zhu, Xuegong X, Lee, Katie K, Asa, Sylvia L SL and Ezzat, Shereen S.. (2007) Epigenetic silencing through DNA and histone methylation of fibroblast growth factor receptor 2 in neoplastic pituitary cells.. The American journal of pathology, [PMID:17456767] |
181. Beaven, Anne W AW and Shea, Thomas C TC.. (2007) Recombinant human keratinocyte growth factor palifermin reduces oral mucositis and improves patient outcomes after stem cell transplant.. Drugs of today (Barcelona, Spain : 1998), [PMID:17728847] |
182. 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] |
183. Lew, Erin D ED, Bae, Jae Hyun JH, Rohmann, Edyta E, Wollnik, Bernd B and Schlessinger, Joseph J.. (2007) Structural basis for reduced FGFR2 activity in LADD syndrome: Implications for FGFR autoinhibition and activation.. Proceedings of the National Academy of Sciences of the United States of America, (11): [PMID:18056630] |
184. Dufour, Cécilie C and 5 more authors.. (2008) FGFR2-Cbl interaction in lipid rafts triggers attenuation of PI3K/Akt signaling and osteoblast survival.. Bone, [PMID:18374639] |
185. Chen, Huaibin H and 9 more authors.. (2008) A crystallographic snapshot of tyrosine trans-phosphorylation in action.. Proceedings of the National Academy of Sciences of the United States of America, (16): [PMID:19060208] |
186. Cha, Jiyoung Y JY, Maddileti, Savitri S, Mitin, Natalia N, Harden, T Kendall TK and Der, Channing J CJ.. (2009) Aberrant receptor internalization and enhanced FRS2-dependent signaling contribute to the transforming activity of the fibroblast growth factor receptor 2 IIIb C3 isoform.. The Journal of biological chemistry, (6): [PMID:19103595] |
187. and Katoh, Masaru M.. (2009) FGFR2 abnormalities underlie a spectrum of bone, skin, and cancer pathologies.. The Journal of investigative dermatology, [PMID:19387476] |
188. Eichholz, Andrew; Merchant, Shairoz and Gaya, Andrew M.. (2010) Anti-angiogenesis therapies: their potential in cancer management.. OncoTargets and therapy, (24): [PMID:20616958] |
189. 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] |
190. Merrill, Amy E AE and 13 more authors.. (2012) Bent bone dysplasia-FGFR2 type, a distinct skeletal disorder, has deficient canonical FGF signaling.. American journal of human genetics, (9): [PMID:22387015] |
191. Gozgit, Joseph M JM and 9 more authors.. (2013) Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models.. Cancer chemotherapy and pharmacology, [PMID:23468082] |
192. Tabernero, Josep J and 18 more authors.. (2015) Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors.. Journal of clinical oncology : official journal of the American Society of Clinical Oncology, (20): [PMID:26324363] |
193. Perles, Zeev Z and 8 more authors.. (2015) A human laterality disorder caused by a homozygous deleterious mutation in MMP21.. Journal of medical genetics, [PMID:26429889] |
194. Qi, Wei W and 39 more authors.. (2017) An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.. Nature chemical biology, [PMID:28135235] |
195. Wind, Sven and 7 more authors.. (2019) Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib.. Clinical pharmacokinetics, [PMID:31016670] |
196. Katoh, M M and 7 more authors.. (1992) K-sam gene encodes secreted as well as transmembrane receptor tyrosine kinase.. Proceedings of the National Academy of Sciences of the United States of America, (1): [PMID:1313574] |
197. Pulleyn, L J LJ and 11 more authors.. (1996) Spectrum of craniosynostosis phenotypes associated with novel mutations at the fibroblast growth factor receptor 2 locus.. European journal of human genetics : EJHG, [PMID:8946174] |
198. May-Dracka TL,Arduini R,Bertolotti-Ciarlet A,Bhisetti G,Brickelmaier M,Cahir-McFarland E,Enyedy I,Fontenot JD,Hesson T,Little K,Lyssikatos J,Marcotte D,McKee T,Murugan P,Patterson T,Peng H,Rushe M,Silvian L,Spilker K,Wu P,Xin Z,Burkly LC. (2018) Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity.. Bioorg Med Chem Lett, 28 (10): (1964-1971). [PMID:29636220] |