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- PA: Serine (S) Peptidases
- S1: Chymotrypsin
S1: Chymotrypsin C
Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Enzymes
3194
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acrosin
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cathepsin G
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chymase 1
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chymotrypsin C
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chymotrypsin like
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chymotrypsin like elastase 1
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chymotrypsin like elastase 2A
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chymotrypsinogen B1 Show summary »« Hide summary
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complement C1r
C
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complement C1s
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complement factor B
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coagulation factor II, thrombin / prothrombin
C
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coagulation factor VII
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coagulation factor IX
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coagulation factor X
C
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coagulation factor XI
C
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coagulation factor XII
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elastase, neutrophil expressed
C
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granzyme A
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granzyme B
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granzyme K
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HtrA serine peptidase 1 Show summary »« Hide summary
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kallikrein B1
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kallikrein 1
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kallikrein related peptidase 2
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kallikrein related peptidase 3
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kallikrein related peptidase 4
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kallikrein related peptidase 5
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kallikrein related peptidase 6
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kallikrein related peptidase 7
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kallikrein related peptidase 8
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kallikrein related peptidase 14
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plasminogen
C
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plasminogen activator, tissue type
C
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plasminogen activator, urokinase
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serine protease 1
C
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serine protease 2
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serine protease 3
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serine protease 8
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protein C, inactivator of coagulation factors Va and VIIIa
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proteinase 3
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ST14 transmembrane serine protease matriptase
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transmembrane serine protease 2
C
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transmembrane serine protease 6
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transmembrane serine protease 11D
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transmembrane serine protease 15 Show summary »« Hide summary
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tryptase alpha/beta 1
C
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tryptase gamma 1
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References
1. Chen M, Yang S, Wu Y, Zhao Z, Zhai X, Dong D. (2021) High temperature requirement A1 in cancer: biomarker and therapeutic target. Cancer Cell Int, 21 (1): 513. [PMID:34563186]
2. Cheng L, Pettersen D, Ohlsson B, Schell P, Karle M, Evertsson E, Pahlen S, Jonforsen M, Plowright AT, Bostrom J et al.. (2014) Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. ACS Med Chem Lett, 5 (5): 538-543. [PMID:24900876]
3. Coste T, Hervé D, Neau JP, Jouvent E, Ba F, Bergametti F, Lamy M, Cogez J, Derache N, Schneckenburger R et al.. (2021) Heterozygous HTRA1 nonsense or frameshift mutations are pathogenic. Brain, 144 (9): 2616-2624. [PMID:34270682]
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]
5. Erba F, Fiorucci L, Pascarella S, Menegatti E, Ascenzi P, Ascoli F. (2001) Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. Biochem Pharmacol, 61 (3): 271-6. [PMID:11172730]
6. Eriksson BI, Wille-Jørgensen P, Kälebo P, Mouret P, Rosencher N, Bösch P, Baur M, Ekman S, Bach D, Lindbratt S et al.. (1997) A comparison of recombinant hirudin with a low-molecular-weight heparin to prevent thromboembolic complications after total hip replacement. N Engl J Med, 337 (19): 1329-35. [PMID:9358126]
7. Furugohri T, Isobe K, Honda Y, Kamisato-Matsumoto C, Sugiyama N, Nagahara T, Morishima Y, Shibano T. (2008) DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost, 6 (9): 1542-9. [PMID:18624979]
8. Hara T, Yokoyama A, Ishihara H, Yokoyama Y, Nagahara T, Iwamoto M. (1994) DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa. Thromb Haemost, 71 (3): 314-9. [PMID:8029795]
9. Hauel NH, Nar H, Priepke H, Ries U, Stassen JM, Wienen W. (2002) Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem, 45 (9): 1757-66. [PMID:11960487]
10. Hayashi M, Hamada A, Okaya Y, Wakitani K, Aisaka K. (2001) Inhibitory effect of JTV-803, a new cyclic guanidine derivative, on factor Xa in vitro and in vivo. Eur J Pharmacol, 428 (2): 163-8. [PMID:11675032]
11. Hays SJ, Caprathe BW, Gilmore JL, Amin N, Emmerling MR, Michael W, Nadimpalli R, Nath R, Raser KJ, Stafford D et al.. (1998) 2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease. J Med Chem, 41 (7): 1060-7. [PMID:9544206]
12. He F, Li X, Cai S, Lu L, Zhang T, Yang M, Fan N, Wang X, Liu X. (2022) Polymorphism rs11200638 enhanced HtrA1 responsiveness and expression are associated with age-related macular degeneration. Eye (Lond), 36 (8): 1631-1638. [PMID:34326497]
13. Ieko M, Tarumi T, Takeda M, Naito S, Nakabayashi T, Koike T. (2004) Synthetic selective inhibitors of coagulation factor Xa strongly inhibit thrombin generation without affecting initial thrombin forming time necessary for platelet activation in hemostasis. J Thromb Haemost, 2 (4): 612-8. [PMID:15102016]
14. Imiya M, Matsuo T. (1997) Inhibition of collagen-induced platelet aggregation by argatroban in patients with acute cerebral infarction. Thromb Res, 88 (2): 245-50. [PMID:9361377]
15. Johnson PH, Sze P, Winant RC, Hudson D, Underhill P, Lazar JB, Olsen C, Almquist R. (1991) Structure-function and refolding studies of the thrombin-specific inhibitor hirudin. Haemostasis, 21 Suppl 1: 41-8. [PMID:1894196]
16. Kawashima I, Tani T, Shimoda K, Takiguchi Y. (1987) Characterization of pancreatic elastase II cDNAs: two elastase II mRNAs are expressed in human pancreas. DNA, 6 (2): 163-72. [PMID:3646943]
17. Kelley RF, Kirchhofer DK, Lai J, Lee CV, Liang X-C, Lipari MT, Loyet KM, Sai T, Van Lookeren Campagne M, Wu Y et al.. (2017) Anti-htra1 antibodies and methods of use thereof. Patent number: WO2017075212A1. Assignee: Genentech, Hoffmann-La Roche. Priority date: 30/10/2015. Publication date: 04/05/2017.
18. Kotian PL, Babu YS, Wu M, Chintareddy VR, Kumar VS, Zhang W. (2015) Human plasma kallikrein inhibitors. Patent number: WO2015134998A1. Assignee: Biocryst Pharmaceuticals. Priority date: 07/03/2014. Publication date: 11/09/2015.
19. Lin MK, Yang J, Hsu CW, Gore A, Bassuk AG, Brown LM, Colligan R, Sengillo JD, Mahajan VB, Tsang SH. (2018) HTRA1, an age-related macular degeneration protease, processes extracellular matrix proteins EFEMP1 and TSP1. Aging Cell, 17 (4): e12710. [PMID:29730901]
20. Liverton NJ, Carroll SS, Dimuzio J, Fandozzi C, Graham DJ, Hazuda D, Holloway MK, Ludmerer SW, McCauley JA, McIntyre CJ et al.. (2010) MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. Antimicrob Agents Chemother, 54 (1): 305-11. [PMID:19841155]
21. Longhurst HJ, Lindsay K, Petersen RS, Fijen LM, Gurugama P, Maag D, Butler JS, Shah MY, Golden A, Xu Y et al.. (2024) CRISPR-Cas9 In Vivo Gene Editing of KLKB1 for Hereditary Angioedema. N Engl J Med, 390 (5): 432-441. [PMID:38294975]
22. Mori S, Itoh Y, Shinohata R, Sendo T, Oishi R, Nishibori M. (2003) Nafamostat mesilate is an extremely potent inhibitor of human tryptase. J Pharmacol Sci, 92 (4): 420-3. [PMID:12939527]
23. Muthusamy K, Ferrer A, Klee EW, Wierenga KJ, Gavrilova RH. (2021) Clinicoradiographic and genetic features of cerebral small vessel disease indicate variability in mode of inheritance for monoallelic HTRA1 variants. Mol Genet Genomic Med, 9 (10): e1799. [PMID:34510819]
24. Pakkala M, Hekim C, Soininen P, Leinonen J, Koistinen H, Weisell J, Stenman UH, Vepsäläinen J, Närvänen A. (2007) Activity and stability of human kallikrein-2-specific linear and cyclic peptide inhibitors. J Pept Sci, 13 (5): 348-53. [PMID:17436344]
25. Perzborn E, Strassburger J, Wilmen A, Pohlmann J, Roehrig S, Schlemmer KH, Straub A. (2005) In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939--an oral, direct Factor Xa inhibitor. J Thromb Haemost, 3 (3): 514-21. [PMID:15748242]
26. Pinto DJ, Smallheer JM, Cheney DL, Knabb RM, Wexler RR. (2010) Factor Xa inhibitors: next-generation antithrombotic agents. J Med Chem, 53 (17): 6243-74. [PMID:20503967]
27. Sasaki M, Miyahisa I, Itono S, Yashiro H, Hiyoshi H, Tsuchimori K, Hamagami KI, Moritoh Y, Watanabe M, Tohyama K et al.. (2019) Discovery and characterization of a small-molecule enteropeptidase inhibitor, SCO-792. Pharmacol Res Perspect, 7 (5): e00517. [PMID:31508234]
28. Schaefer M, Buchmueller A, Dittmer F, Straßburger J, Wilmen A. (2019) Allosteric Inhibition as a New Mode of Action for BAY 1213790, a Neutralizing Antibody Targeting the Activated Form of Coagulation Factor XI. J Mol Biol, 431 (24): 4817-4833. [PMID:31655039]
29. Seidel H, Kolde HJ. (2018) Monitoring of Argatroban and Lepirudin: What is the Input of Laboratory Values in "Real Life"?. Clin Appl Thromb Hemost, 24 (2): 287-294. [PMID:28320219]
30. Shang T, Pinho M, Ray D, Khera A. (2021) Two Unique Mutations in HTRA1-Related Cerebral Small Vessel Disease in North America and Africa and Literature Review. J Stroke Cerebrovasc Dis, 30 (11): 106029. [PMID:34461444]
31. Sofia MJ, Katzenellenbogen JA. (1986) Enol lactone inhibitors of serine proteases. The effect of regiochemistry on the inactivation behavior of phenyl-substituted (halomethylene)tetra- and -dihydrofuranones and (halomethylene)tetrahydropyranones toward alpha-chymotrypsin: stable acyl enzyme intermediate. J Med Chem, 29 (2): 230-8. [PMID:3512826]
32. Sperzel M, Huetter J. (2007) Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost, 5 (10): 2113-8. [PMID:17666018]
33. Stevens T, Ekholm K, Gränse M, Lindahl M, Kozma V, Jungar C, Ottosson T, Falk-Håkansson H, Churg A, Wright JL et al.. (2011) AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. J Pharmacol Exp Ther, 339 (1): 313-20. [PMID:21791628]
34. Stone GW, McLaurin BT, Cox DA, Bertrand ME, Lincoff AM, Moses JW, White HD, Pocock SJ, Ware JH, Feit F et al.. (2006) Bivalirudin for patients with acute coronary syndromes. N Engl J Med, 355 (21): 2203-16. [PMID:17124018]
35. Sun W, Zhang X, Cummings MD, Albarazanji K, Wu J, Wang M, Alexander R, Zhu B, Zhang Y, Leonard J et al.. (2020) Targeting Enteropeptidase with Reversible Covalent Inhibitors To Achieve Metabolic Benefits. J Pharmacol Exp Ther, 375 (3): 510-521. [PMID:33033171]
36. Tan X, Soualmia F, Furio L, Renard JF, Kempen I, Qin L, Pagano M, Pirotte B, El Amri C, Hovnanian A et al.. (2015) Toward the first class of suicide inhibitors of kallikreins involved in skin diseases. J Med Chem, 58 (2): 598-612. [PMID:25489658]
37. Tully DC, Vidal A, Chatterjee AK, Williams JA, Roberts MJ, Petrassi HM, Spraggon G, Bursulaya B, Pacoma R, Shipway A et al.. (2008) Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design. Bioorg Med Chem Lett, 18 (22): 5895-9. [PMID:18752942]
38. Wang Y, Nie G. (2021) Overview of Human HtrA Family Proteases and Their Distinctive Physiological Roles and Unique Involvement in Diseases, Especially Cancer and Pregnancy Complications. Int J Mol Sci, 22 (19). DOI: 10.3390/ijms221910756 [PMID:34639128]
39. Warkentin TE, Greinacher A, Craven S, Dewar L, Sheppard JA, Ofosu FA. (2005) Differences in the clinically effective molar concentrations of four direct thrombin inhibitors explain their variable prothrombin time prolongation. Thromb Haemost, 94 (5): 958-64. [PMID:16363236]
40. Wienen W, Stassen J-M, Priepke H, Ries UJ, Hauel N. (2007) In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate. Thrombosis and Haemostasis, 98 (01): 155-162. DOI: DOI: 10.1160/TH07-03-0183
41. Witting JI, Bourdon P, Brezniak DV, Maraganore JM, Fenton 2nd JW. (1992) Thrombin-specific inhibition by and slow cleavage of hirulog-1. Biochem J, 283 ( Pt 3): 737-43. [PMID:1290488]
42. Wong PC, Crain EJ, Xin B, Wexler RR, Lam PY, Pinto DJ, Luettgen JM, Knabb RM. (2008) Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. J Thromb Haemost, 6 (5): 820-9. [PMID:18315548]
43. Wu L, Li X, Li Z, Cheng Y, Wu F, Lv C, Zhang W, Tang W. (2021) HtrA serine proteases in cancers: A target of interest for cancer therapy. Biomed Pharmacother, 139: 111603. [PMID:34243596]
44. Yashiro H, Hamagami K, Hiyoshi H, Sugama J, Tsuchimori K, Yamaguchi F, Moritoh Y, Sasaki M, Maekawa T, Yamada Y et al.. (2019) SCO-792, an enteropeptidase inhibitor, improves disease status of diabetes and obesity in mice. Diabetes Obes Metab, 21 (10): 2228-2239. [PMID:31144422]
45. Young WB, Rai R, Shrader WD, Burgess-Henry J, Hu H, Elrod KC, Sprengeler PA, Katz BA, Sukbuntherng J, Mordenti J. (2006) Small molecule inhibitors of plasma kallikrein. Bioorg Med Chem Lett, 16 (7): 2034-6. [PMID:16413183]
How to cite this family page
Database page citation:
S1: Chymotrypsin. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=751.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.
