2fxr
From Proteopedia
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human beta tryptase II complexed with activated ketone 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
2FXR is a Single protein structure of sequence from Homo sapiens with C3A as ligand. Active as Tryptase, with EC number 3.4.21.59 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 Mon Nov 12 22:11:37 2007
