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2fs8

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Revision as of 14:56, 20 March 2008 by OCA (Talk | contribs)
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Image:2fs8.gif


PDB ID 2fs8

Drag the structure with the mouse to rotate
, resolution 2.500Å
Ligands:
Gene: TPSB2, TPS2 (Homo sapiens)
Activity: Tryptase, with EC number 3.4.21.59
Coordinates: save as pdb, mmCIF, xml



Human beta-tryptase II with inhibitor CRA-29382


Overview

Improved peptide-based inhibitors of human beta tryptase were discovered using information gleaned from tripeptide library screening and structure-guided design methods, including fragment screening. Our efforts sought to improve this class of inhibitors by replacing the traditional Lys or Arg P1 element. The optimized compounds display low nanomolar potency against the mast cell target and several hundred-fold selectivity with respect to serine protease off targets. Thus, replacement of Lys/Arg at P1 in a peptide-like scaffold does not need to be accompanied by a loss in target affinity.

About this Structure

2FS8 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure-guided design of peptide-based tryptase inhibitors., McGrath ME, Sprengeler PA, Hirschbein B, Somoza JR, Lehoux I, Janc JW, Gjerstad E, Graupe M, Estiarte A, Venkataramani C, Liu Y, Yee R, Ho JD, Green MJ, Lee CS, Liu L, Tai V, Spencer J, Sperandio D, Katz BA, Biochemistry. 2006 May 16;45(19):5964-73. PMID:16681368

Page seeded by OCA on Thu Mar 20 16:56:09 2008

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