protease, serine 1

Target id: 2397

Nomenclature: protease, serine 1

Family: S1: Chymotrypsin

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     protease, serine 1 has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 247 7q34 PRSS1 protease, serine 1
Mouse - 264 6 B1 Prss1 protease, serine 1 (trypsin 1)
Rat - 247 4q22 Prss3b protease, serine, 3B
Previous and Unofficial Names
cationic trypsin III | cationic trypsin-3 | cationic trypsinogen | Try1 | Try3 | Trygn16 | trypsinogen 16 | protease, serine, 1 (trypsin 1) | Prss3 | protease, serine, 3 | protease, serine, 3B | protease
Database Links
Specialist databases
MEROPS S01.127 (Hs)
Other databases
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.21.4

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
RWJ-56423 Bt Inhibition 8.1 pKi 1
pKi 8.1 (Ki 8.09x10-9 M) [1]
nafamostat Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.7x10-8 M) [3]
compound 9 [PMID: 3514912] Hs Inhibition 7.7 pIC50 4
pIC50 7.7 (IC50 1.95x10-8 M) [4]
camostat Hs Inhibition 7.3 pIC50 5
pIC50 7.3 (IC50 5.06x10-8 M) [5]
View species-specific inhibitor tables
Immunopharmacology Comments
Inhibition of PRSS1 (and TPSAB1), released from mast cells in response to allergen exposure, abrogates the subsequent allergic airway response in vivo [1-2]: e.g. see dual TPSAB1/PRSS1 inhibitor RWJ-58643.
Clinically-Relevant Mutations and Pathophysiology
Disease:  Hereditary pancreatitis
Synonyms: Hereditary chronic pancreatitis [Orphanet: ORPHA676]
OMIM: 167800
Orphanet: ORPHA676
Disease:  Trypsinogen deficiency
OMIM: 614044

References

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1. Costanzo MJ, Yabut SC, Almond Jr HR, Andrade-Gordon P, Corcoran TW, De Garavilla L, Kauffman JA, Abraham WM, Recacha R, Chattopadhyay D et al.. (2003) Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone. J. Med. Chem.46 (18): 3865-76. [PMID:12930148]

2. Erin EM, Leaker BR, Zacharasiewicz A, Higgins LA, Nicholson GC, Boyce MJ, de Boer P, Jones RC, Durham SR, Barnes PJ et al.. (2006) Effects of a reversible beta-tryptase and trypsin inhibitor (RWJ-58643) on nasal allergic responses. Clin. Exp. Allergy36 (4): 458-64. [PMID:16630150]

3. 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]

4. Kaminski JM, Bauer L, Mack SR, Anderson Jr RA, Waller DP, Zaneveld LJ. (1986) Synthesis and inhibition of human acrosin and trypsin and acute toxicity of aryl 4-guanidinobenzoates. J. Med. Chem.29 (4): 514-9. [PMID:3514912]

5. Senokuchi K, Nakai H, Nakayama Y, Odagaki Y, Sakaki K, Kato M, Maruyama T, Miyazaki T, Ito H, Kamiyasu K et al.. (1995) New orally active serine protease inhibitors. J. Med. Chem.38 (14): 2521-3. [PMID:7629790]

How to cite this page

S1: Chymotrypsin: protease, serine 1. Last modified on 04/10/2016. Accessed on 17/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2397.