tryptase alpha/beta 1

Target id: 2424

Nomenclature: tryptase alpha/beta 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 :     tryptase alpha/beta 1 has curated GtoImmuPdb data

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

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 Hs Inhibition 8.0 pKi 1
pKi 8.0 (Ki 1x10-8 M) [1]
nafamostat Hs Inhibition 10.0 pIC50 4
pIC50 10.0 (IC50 9.53x10-11 M) [4]
gabexate 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. Allergy36 (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 17/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2424.