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tryptase alpha/beta 1

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 2424

Nomenclature: tryptase alpha/beta 1

Family: S1: Chymotrypsin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 275 16p13.3 TPSAB1 tryptase alpha/beta 1
Previous and Unofficial Names Click here for help
tryptase-I | tryptase-II | tryptase-III | TPS1 | TPS2 | TPSB1 | tryptase alpha II
Database Links Click here for help
Specialist databases
MEROPS S01.143 (Hs)
Other databases
Alphafold Q15661 (Hs)
BRENDA 3.4.21.59
ChEMBL Target CHEMBL2617 (Hs)
Ensembl Gene ENSG00000172236 (Hs)
Entrez Gene 7177 (Hs)
Human Protein Atlas ENSG00000172236 (Hs)
KEGG Enzyme 3.4.21.59
KEGG Gene hsa:7177 (Hs)
OMIM 191080 (Hs)
Pharos Q15661 (Hs)
RefSeq Nucleotide NM_003294 (Hs)
RefSeq Protein NP_003285 (Hs)
UniProtKB Q15661 (Hs)
Wikipedia TPSAB1 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.21.59

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 Primary target of this compound Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.0 pKi 1
⤷ pKi 8.0 (Ki 1x10-8 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 10.0 pIC50 4
⤷ pIC50 10.0 (IC50 9.53x10-11 M) [4]
gabexate Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition 8.5 pIC50 2
⤷ pIC50 8.5 (IC50 3.4x10-9 M) [2]
Immunopharmacology Comments
Inhibition of TPSAB1, released from mast cells in response to allergen exposure, abrogates the subsequent allergic airway response in vivo [1,3]: e.g. see inhibitor RWJ-58643.

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. 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]

3. 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]

4. 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]

How to cite this page

S1: Chymotrypsin: tryptase alpha/beta 1. Last modified on 04/10/2016. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2424.