2bm2

From Proteopedia

Revision as of 10:00, 30 October 2007

HUMAN BETA-II TRYPTASE IN COMPLEX WITH 4-(3-AMINOMETHYL-PHENYL)-PIPERIDIN-1-YL-(5-PHENETHYL- PYRIDIN-3-YL)-METHANONE

Overview

Tryptase is a serine protease found almost exclusively in mast cells. It, has trypsin-like specificity, favoring cleavage of substrates with an, arginine (or lysine) at the P1 position, and has optimal catalytic, activity at neutral pH. Current evidence suggests tryptase beta is the, most important form released during mast cell activation in allergic, diseases. It is shown to have numerous pro-inflammatory cellular, activities in vitro, and in animal models tryptase provokes, broncho-constriction and induces a cellular inflammatory infiltrate, characteristic of human asthma. Screening of in-house inhibitors of factor, Xa (a closely related serine protease) identified beta-amidoester, benzamidines as potent inhibitors of recombinant human betaII tryptase., X-ray structure driven template ... [(full description)]

About this Structure

2BM2 is a [Single protein] structure of sequence from [Homo sapiens] with PM2 as [ligand]. Active as [Tryptase], with EC number [3.4.21.59]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

Reference

Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase., Levell J, Astles P, Eastwood P, Cairns J, Houille O, Aldous S, Merriman G, Whiteley B, Pribish J, Czekaj M, Liang G, Maignan S, Guilloteau JP, Dupuy A, Davidson J, Harrison T, Morley A, Watson S, Fenton G, McCarthy C, Romano J, Mathew R, Engers D, Gardyan M, Sides K, Kwong J, Tsay J, Rebello S, Shen L, Wang J, Luo Y, Giardino O, Lim HK, Smith K, Pauls H, Bioorg Med Chem. 2005 Apr 15;13(8):2859-72. PMID:15781396

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