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serine protease 1

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 2397

Nomenclature: serine protease 1

Family: S1: Chymotrypsin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 247 7q34 PRSS1 serine protease 1
Mouse - 264 6 B1 Prss1 serine protease 1 (trypsin 1)
Rat - 247 4q23 Prss3b protease, serine, 3B
Previous and Unofficial Names Click here for help
cationic trypsin-3 | cationic trypsin III | cationic trypsinogen | protease | protease, serine 1 | protease, serine, 1 (trypsin 1) | protease, serine 1 (trypsin 1) | protease, serine, 3 | protease, serine, 3B | Prss3 | Try1 | Try3 | Trygn16 | trypsinogen 16
Database Links Click here for help
Specialist databases
MEROPS S01.127 (Hs)
Other databases
Alphafold P07477 (Hs), P08426 (Rn)
BRENDA 3.4.21.4
ChEMBL Target CHEMBL209 (Hs)
Ensembl Gene ENSG00000204983 (Hs), ENSMUSG00000062751 (Mm), ENSRNOG00000013382 (Rn)
Entrez Gene 5644 (Hs), 114228 (Mm), 286911 (Rn)
Human Protein Atlas ENSG00000204983 (Hs)
KEGG Enzyme 3.4.21.4
KEGG Gene hsa:5644 (Hs), mmu:114228 (Mm), rno:286911 (Rn)
OMIM 276000 (Hs)
Orphanet ORPHA118080 (Hs)
Pharos P07477 (Hs)
RefSeq Nucleotide NM_002769 (Hs), NM_053243 (Mm), NM_173127 (Rn)
RefSeq Protein NP_002760 (Hs), NP_444473 (Mm), NP_775150 (Rn)
UniProtKB P07477 (Hs), P08426 (Rn)
Wikipedia PRSS1 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.21.4

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
RWJ-56423 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Bt Inhibition 8.1 pKi 1
⤷ pKi 8.1 (Ki 8.09x10-9 M) [1]
nafamostat Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 3
⤷ pIC50 7.8 (IC50 1.7x10-8 M) [3]
compound 9 [PMID: 3514912] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 4
⤷ pIC50 7.7 (IC50 1.95x10-8 M) [4]
camostat Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table 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 Click here for help
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 Allergy, 36 (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: serine protease 1. Last modified on 27/02/2018. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2397.