2bm2

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|SITE= <scene name='pdbsite=AC1:Pm2+Binding+Site+For+Chain+D'>AC1</scene>
|SITE= <scene name='pdbsite=AC1:Pm2+Binding+Site+For+Chain+D'>AC1</scene>
|LIGAND= <scene name='pdbligand=PM2:1-[3-(1-{[5-(2-PHENYLETHYL)PYRIDIN-3-YL]CARBONYL}PIPERIDIN-4-YL)PHENYL]METHANAMINE'>PM2</scene>
|LIGAND= <scene name='pdbligand=PM2:1-[3-(1-{[5-(2-PHENYLETHYL)PYRIDIN-3-YL]CARBONYL}PIPERIDIN-4-YL)PHENYL]METHANAMINE'>PM2</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Tryptase Tryptase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.59 3.4.21.59]
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Tryptase Tryptase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.59 3.4.21.59] </span>
|GENE=
|GENE=
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|DOMAIN=
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2bm2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bm2 OCA], [http://www.ebi.ac.uk/pdbsum/2bm2 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2bm2 RCSB]</span>
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[[Category: Watson, S.]]
[[Category: Watson, S.]]
[[Category: Whiteley, B.]]
[[Category: Whiteley, B.]]
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[[Category: PM2]]
 
[[Category: glycoprotein]]
[[Category: glycoprotein]]
[[Category: hydrolase]]
[[Category: hydrolase]]
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[[Category: serine protease inhibitor]]
[[Category: serine protease inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:03:44 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:08:23 2008''

Revision as of 23:08, 30 March 2008

Image:2bm2.gif


PDB ID 2bm2

Drag the structure with the mouse to rotate
, resolution 2.2Å
Sites:
Ligands:
Activity: Tryptase, with EC number 3.4.21.59
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



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 modification and exchange of the benzamidine to optimize potency and pharmacokinetic properties gave selective, potent and orally bioavailable 4-(3-aminomethyl phenyl)piperidinyl-1-amides.

About this Structure

2BM2 is a Single protein structure of sequence from Homo sapiens. 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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