1. Pinto DJ, Orwat MJ, Wang S, Fevig JM, Quan ML, Amparo E, Cacciola J, Rossi KA, Alexander RS, Smallwood AM, Luettgen JM, Liang L, Aungst BJ, Wright MR, Knabb RM, Wong PC, Wexler RR, Lam PY.. (2001) Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.. J Med Chem, 44 (4): (566-578). [PMID:11170646] [10.1021/jm000409z] |
2. Enyedy IJ, Lee SL, Kuo AH, Dickson RB, Lin CY, Wang S.. (2001) Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase.. J Med Chem, 44 (9): (1349-1355). [PMID:11311057] [10.1021/jm000395x] |
3. Wang S, Beck R, Burd A, Blench T, Marlin F, Ayele T, Buxton S, Dagostin C, Malic M, Joshi R et al.. (2010) Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors.. J Med Chem, 53 (4): (1473-82). [PMID:20121197] [10.1021/op500134e] |
4. Crocetti L, Giovannoni MP, Schepetkin IA, Quinn MT, Khlebnikov AI, Cilibrizzi A, Piaz VD, Graziano A, Vergelli C. (2011) Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.. Bioorg Med Chem, 19 (15): (4460-72). [PMID:21741848] [10.1021/op500134e] |
5. Subasinghe NL, Travins JM, Ali F, Huang H, Ballentine SK, Marugán JJ, Khalil E, Hufnagel HR, Bone RF, DesJarlais RL et al.. (2006) A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.. Bioorg Med Chem Lett, 16 (8): (2200-4). [PMID:16460935] [10.1021/op500134e] |
6. Kwan JC, Eksioglu EA, Liu C, Paul VJ, Luesch H. (2009) Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.. J Med Chem, 52 (18): (5732-47). [PMID:19715320] [10.1021/op500134e] |
7. Setyono-Han B, Stürzebecher J, Schmalix WA, Muehlenweg B, Sieuwerts AM, Timmermans M, Magdolen V, Schmitt M, Klijn JG, Foekens JA. (2005) Suppression of rat breast cancer metastasis and reduction of primary tumour growth by the small synthetic urokinase inhibitor WX-UK1.. Thromb Haemost, 93 (4): (779-86). [PMID:15841327] [10.1021/op500134e] |
8. Steinmetzer T, Schweinitz A, Stürzebecher A, Dönnecke D, Uhland K, Schuster O, Steinmetzer P, Müller F, Friedrich R, Than ME, Bode W, Stürzebecher J.. (2006) Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase.. J Med Chem, 49 (14): (4116-4126). [PMID:16821772] [10.1021/jm051272l] |
9. Schepetkin IA, Khlebnikov AI, Quinn MT.. (2007) N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.. J Med Chem, 50 (20): (4928-4938). [PMID:17850059] [10.1021/jm070600+] |
10. Joossens J, Ali OM, El-Sayed I, Surpateanu G, Van der Veken P, Lambeir AM, Setyono-Han B, Foekens JA, Schneider A, Schmalix W, Haemers A, Augustyns K.. (2007) Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.. J Med Chem, 50 (26): (6638-6646). [PMID:18052026] [10.1021/jm700962j] |
11. Wang S, Beck R, Blench T, Burd A, Buxton S, Malic M, Ayele T, Shaikh S, Chahwala S, Chander C, Holland R, Merette S, Zhao L, Blackney M, Watts A.. (2010) Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis.. J Med Chem, 53 (4): (1465-1472). [PMID:20121198] [10.1021/jm901475e] |
12. Lu T, Markotan T, Ballentine SK, Giardino EC, Spurlino J, Crysler CS, Brown K, Maryanoff BE, Tomczuk BE, Damiano BP, Shukla U, End D, Andrade-Gordon P, Bone RF, Player MR.. (2010) Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.. J Med Chem, 53 (4): (1843-1856). [PMID:20102150] [10.1021/jm901802n] |
13. Massey AP, Harley WR, Pasupuleti N, Gorin FA, Nantz MH.. (2012) 2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator.. Bioorg Med Chem Lett, 22 (7): (2635-2639). [PMID:22366654] [10.1016/j.bmcl.2011.12.123] |
14. Wang F, Eric Knabe W, Li L, Jo I, Mani T, Roehm H, Oh K, Li J, Khanna M, Meroueh SO.. (2012) Design, synthesis, biochemical studies, cellular characterization, and structure-based computational studies of small molecules targeting the urokinase receptor.. Bioorg Med Chem, 20 (15): (4760-4773). [PMID:22771232] [10.1016/j.bmc.2012.06.002] |
15. Crocetti L, Schepetkin IA, Cilibrizzi A, Graziano A, Vergelli C, Giomi D, Khlebnikov AI, Quinn MT, Giovannoni MP.. (2013) Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase.. J Med Chem, 56 (15): (6259-6272). [PMID:23844670] [10.1021/jm400742j] |
16. Bijak M, Ziewiecki R, Saluk J, Ponczek M, Pawlaczyk I, Krotkiewski H, Wachowicz B, Nowak P.. (2013) Thrombin inhibitory activity of some polyphenolic compounds.. Med Chem Res, (1-14). [PMID:24610996] [10.1007/s00044-013-0829-4] |
17. Meneyrol J, Follmann M, Lassalle G, Wehner V, Barre G, Rousseaux T, Altenburger JM, Petit F, Bocskei Z, Schreuder H, Alet N, Herault JP, Millet L, Dol F, Florian P, Schaeffer P, Sadoun F, Klieber S, Briot C, Bono F, Herbert JM.. (2013) 5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor.. J Med Chem, 56 (23): (9441-9456). [PMID:24175584] [10.1021/jm4005835] |
18. Lucas SD, Gonçalves LM, Carvalho LA, Correia HF, Da Costa EM, Guedes RA, Moreira R, Guedes RC.. (2013) Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.. J Med Chem, 56 (23): (9802-9806). [PMID:24224573] [10.1021/jm4011725] |
19. Ko HS, Kim JS, Cho SM, Lee HJ, Ahn KS, Kim SH, Lee EO.. (2014) Urokinase-type plasminogen activator expression and Rac1/WAVE-2/Arp2/3 pathway are blocked by pterostilbene to suppress cell migration and invasion in MDA-MB-231 cells.. Bioorg Med Chem Lett, 24 (4): (1176-1179). [PMID:24440300] [10.1016/j.bmcl.2013.12.115] |
20. Goswami R, Mukherjee S, Ghadiyaram C, Wohlfahrt G, Sistla RK, Nagaraj J, Satyam LK, Subbarao K, Palakurthy RK, Gopinath S, Krishnamurthy NR, Ikonen T, Moilanen A, Subramanya HS, Kallio P, Ramachandra M.. (2014) Structure-guided discovery of 1,3,5 tri-substituted benzenes as potent and selective matriptase inhibitors exhibiting in vivo antitumor efficacy.. Bioorg Med Chem, 22 (12): (3187-3203). [PMID:24794746] [10.1016/j.bmc.2014.04.013] |
21. Spicer TP, Jiang J, Taylor AB, Choi JY, Hart PJ, Roush WR, Fields GB, Hodder PS, Minond D.. (2014) Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.. J Med Chem, 57 (22): (9598-9611). [PMID:25330343] [10.1021/jm501284e] |
22. Goswami R, Wohlfahrt G, Törmäkangas O, Moilanen A, Lakshminarasimhan A, Nagaraj J, Arumugam KN, Mukherjee S, Chacko AR, Krishnamurthy NR, Jaleel M, Palakurthy RK, Samiulla DS, Ramachandra M.. (2015) Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.. Bioorg Med Chem Lett, 25 (22): (5309-5314). [PMID:26421993] [10.1016/j.bmcl.2015.09.042] |
23. Zhang X, Glunz PW, Johnson JA, Jiang W, Jacutin-Porte S, Ladziata V, Zou Y, Phillips MS, Wurtz NR, Parkhurst B, Rendina AR, Harper TM, Cheney DL, Luettgen JM, Wong PC, Seiffert D, Wexler RR, Priestley ES.. (2016) Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.. J Med Chem, 59 (15): (7125-7137). [PMID:27455395] [10.1021/acs.jmedchem.6b00469] |
24. Middendorp SJ, Wilbs J, Quarroz C, Calzavarini S, Angelillo-Scherrer A, Heinis C.. (2017) Peptide Macrocycle Inhibitor of Coagulation Factor XII with Subnanomolar Affinity and High Target Selectivity.. J Med Chem, 60 (3): (1151-1158). [PMID:28045547] [10.1021/acs.jmedchem.6b01548] |
25. Choi JY, Fuerst R, Knapinska AM, Taylor AB, Smith L, Cao X, Hart PJ, Fields GB, Roush WR.. (2017) Structure-Based Design and Synthesis of Potent and Selective Matrix Metalloproteinase 13 Inhibitors.. J Med Chem, 60 (13): (5816-5825). [PMID:28653849] [10.1021/acs.jmedchem.7b00514] |
26. Buckley BJ, Aboelela A, Minaei E, Jiang LX, Xu Z, Ali U, Fildes K, Cheung CY, Cook SM, Johnson DC, Bachovchin DA, Cook GM, Apte M, Huang M, Ranson M, Kelso MJ.. (2018) 6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.. J Med Chem, 61 (18): (8299-8320). [PMID:30130401] [10.1021/acs.jmedchem.8b00838] |
27. Islam I, Yuan S, West CW, Adler M, Bothe U, Bryant J, Chang Z, Chu K, Emayan K, Gualtieri G, Ho E, Light D, Mallari C, Morser J, Phillips G, Schaefer C, Sukovich D, Whitlow M, Chen D, Buckman BO.. (2018) Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.. Bioorg Med Chem Lett, 28 (20): (3372-3375). [PMID:30201291] [10.1016/j.bmcl.2018.09.001] |
28. Chen P, Zhang D, Li M, Wu Q, Lam YPY, Guo Y, Chen C, Bai N, Malhotra S, Li W, O'Connor PB, Fu H.. (2019) Discovery of novel, potent, isosteviol-based antithrombotic agents.. Eur J Med Chem, 183 (111722-111722). [PMID:31563807] [10.1016/j.ejmech.2019.111722] |
29. Walker AL, Bingham RP, Edgar EV, Ferrie A, Holmes DS, Liddle J, Polyakova O, Rella M, Smith KJ, Thorpe JH, Wang Y, White GV, Young RJ, Hovnanian A.. (2019) Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.. Bioorg Med Chem Lett, 29 (12): (1454-1458). [PMID:31005442] [10.1016/j.bmcl.2019.04.022] |
30. Walker AL, Denis A, Bingham RP, Bouillot A, Edgar EV, Ferrie A, Holmes DS, Laroze A, Liddle J, Fouchet MH, Moquette A, Nassau P, Pearce AC, Polyakova O, Smith KJ, Thomas P, Thorpe JH, Trottet L, Wang Y, Hovnanian A.. (2019) Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.. Bioorg Med Chem Lett, 29 (20): (126675-126675). [PMID:31521475] [10.1016/j.bmcl.2019.126675] |
31. Wang D, Yang Y, Jiang L, Wang Y, Li J, Andreasen PA, Chen Z, Huang M, Xu P.. (2019) Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.. J Med Chem, 62 (4): (2172-2183). [PMID:30707839] [10.1021/acs.jmedchem.8b01908] |
32. Li, X X, Smith, R A RA and Dobson, C M CM.. (1992) Sequential 1H NMR assignments and secondary structure of the kringle domain from urokinase.. Biochemistry, (13): [PMID:1327118] |
33. Buko, A M AM and 5 more authors.. (1991) Characterization of a posttranslational fucosylation in the growth factor domain of urinary plasminogen activator.. Proceedings of the National Academy of Sciences of the United States of America, (1): [PMID:2023947] |
34. Nagai, M M and 6 more authors.. (1985) Molecular cloning of cDNA coding for human preprourokinase.. Gene, [PMID:2415429] |
35. Oswald, R E RE, Bogusky, M J MJ, Bamberger, M M, Smith, R A RA and Dobson, C M CM.. (1989) Dynamics of the multidomain fibrinolytic protein urokinase from two-dimensional NMR.. Nature, (9): [PMID:2536903] |
36. Riccio, A A and 5 more authors.. (1985) The human urokinase-plasminogen activator gene and its promoter.. Nucleic acids research, (25): [PMID:2987867] |
37. Stief, T W TW, Radtke, K P KP and Heimburger, N N.. (1987) Inhibition of urokinase by protein C-inhibitor (PCI). Evidence for identity of PCI and plasminogen activator inhibitor 3.. Biological chemistry Hoppe-Seyler, [PMID:3501295] |
38. Jacobs, P P and 8 more authors.. (1985) Molecular cloning, sequencing, and expression in Escherichia coli of human preprourokinase cDNA.. DNA (Mary Ann Liebert, Inc.), [PMID:3888571] |
39. Verde, P P, Stoppelli, M P MP, Galeffi, P P, Di Nocera, P P and Blasi, F F.. (1984) Identification and primary sequence of an unspliced human urokinase poly(A)+ RNA.. Proceedings of the National Academy of Sciences of the United States of America, [PMID:6589620] |
40. Schaller, J J and 5 more authors.. (1982) Human low-molecular-weight urinary urokinase. Partial characterization and preliminary sequence data of the two polypeptide chains.. European journal of biochemistry, [PMID:6749491] |
41. Günzler, W A WA and 5 more authors.. (1982) The primary structure of high molecular mass urokinase from human urine. The complete amino acid sequence of the A chain.. Hoppe-Seyler's Zeitschrift fur physiologische Chemie, [PMID:6754569] |
42. Steffens, G J GJ, Günzler, W A WA, Otting, F F, Frankus, E E and Flohé, L L.. (1982) The complete amino acid sequence of low molecular mass urokinase from human urine.. Hoppe-Seyler's Zeitschrift fur physiologische Chemie, [PMID:6754572] |
43. Li, X X, Bokman, A M AM, Llinás, M M, Smith, R A RA and Dobson, C M CM.. (1994) Solution structure of the kringle domain from urokinase-type plasminogen activator.. Journal of molecular biology, (4): [PMID:8107091] |
44. Spraggon, G G and 7 more authors.. (1995) The crystal structure of the catalytic domain of human urokinase-type plasminogen activator.. Structure (London, England : 1993), (15): [PMID:8591045] |
45. Yoshimoto, M M and 7 more authors.. (1996) Characterization of single chain urokinase-type plasminogen activator with a novel amino-acid substitution in the kringle structure.. Biochimica et biophysica acta, (7): [PMID:8652631] |
46. Conne, B B, Berczy, M M and Belin, D D.. (1997) Detection of polymorphisms in the human urokinase-type plasminogen activator gene.. Thrombosis and haemostasis, [PMID:9065988] |
47. Franco, P P and 7 more authors.. (1997) Phosphorylation of human pro-urokinase on Ser138/303 impairs its receptor-dependent ability to promote myelomonocytic adherence and motility.. The Journal of cell biology, (5): [PMID:9151681] |
48. Türkmen, B B and 7 more authors.. (1997) Mutational analysis of the genes encoding urokinase-type plasminogen activator (uPA) and its inhibitor PAI-1 in advanced ovarian cancer.. Electrophoresis, [PMID:9194591] |
49. He, S S, Lin, Y L YL and Liu, Y X YX.. (1999) Functionally inactive protein C inhibitor in seminal plasma may be associated with infertility.. Molecular human reproduction, [PMID:10340997] |
50. Behrendt, N N and 5 more authors.. (2000) A urokinase receptor-associated protein with specific collagen binding properties.. The Journal of biological chemistry, (21): [PMID:10636902] |
51. Katz, B A BA and 8 more authors.. (2000) Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.. Chemistry & biology, [PMID:10779411] |
52. Sperl, S S and 8 more authors.. (2000) (4-aminomethyl)phenylguanidine derivatives as nonpeptidic highly selective inhibitors of human urokinase.. Proceedings of the National Academy of Sciences of the United States of America, (9): [PMID:10805774] |
53. Liu, C X CX, Li, Y Y, Obermoeller-McCormick, L M LM, Schwartz, A L AL and Bu, G G.. (2001) The putative tumor suppressor LRP1B, a novel member of the low density lipoprotein (LDL) receptor family, exhibits both overlapping and distinct properties with the LDL receptor-related protein.. The Journal of biological chemistry, (3): [PMID:11384978] |
54. Luikart, Sharon S and 7 more authors.. (2002) Urokinase is required for the formation of mactinin, an alpha-actinin fragment that promotes monocyte/macrophage maturation.. Biochimica et biophysica acta, (19): [PMID:12183060] |
55. Wakita, Toshiaki T and 10 more authors.. (2004) Regulation of carcinoma cell invasion by protein C inhibitor whose expression is decreased in renal cell carcinoma.. International journal of cancer, (10): [PMID:14696115] |
56. Deloukas, P P and 135 more authors.. (2004) The DNA sequence and comparative analysis of human chromosome 10.. Nature, (27): [PMID:15164054] |
57. Katz, Bradley A BA and 14 more authors.. (2004) Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).. Journal of molecular biology, (19): [PMID:15522303] |
58. Olivero, Alan G AG and 18 more authors.. (2005) A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.. The Journal of biological chemistry, (11): [PMID:15632123] |
59. Ustach, Carolyn V CV and Kim, Hyeong-Reh Choi HR.. (2005) Platelet-derived growth factor D is activated by urokinase plasminogen activator in prostate carcinoma cells.. Molecular and cellular biology, [PMID:15988036] |
60. Huai, Qing Q and 13 more authors.. (2006) Structure of human urokinase plasminogen activator in complex with its receptor.. Science (New York, N.Y.), (3): [PMID:16456079] |
61. Ley, Timothy J TJ and 47 more authors.. (2008) DNA sequencing of a cytogenetically normal acute myeloid leukaemia genome.. Nature, (6): [PMID:18987736] |
62. Paterson, Andrew D AD and 8 more authors.. (2010) Persons with Quebec platelet disorder have a tandem duplication of PLAU, the urokinase plasminogen activator gene.. Blood, (11): [PMID:20007542] |
63. Min, Hye-Jin HJ, Lee, Myung Kyu MK, Lee, Jung Weon JW and Kim, Semi S.. (2014) TMPRSS4 induces cancer cell invasion through pro-uPA processing.. Biochemical and biophysical research communications, (28): [PMID:24434139] |
64. Chen, X X, Ji, Z L ZL and Chen, Y Z YZ.. (2002) TTD: Therapeutic Target Database.. Nucleic acids research, (1): [PMID:11752352] |
65. Zhao G, Bolton SA, Kwon C, Hartl KS, Seiler SM, Slusarchyk WA, Sutton JC, Bisacchi GS.. (2004) Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.. Bioorg Med Chem Lett, 14 ( ): (309-312). [PMID:14698147] [10.1016/j.bmcl.2003.11.016] |