2fxr

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[[Image:2fxr.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_2fxr| PDB=2fxr | SCENE= }}
{{STRUCTURE_2fxr| PDB=2fxr | SCENE= }}
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'''human beta tryptase II complexed with activated ketone inhibitor CRA-29382'''
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===human beta tryptase II complexed with activated ketone inhibitor CRA-29382===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 16681368 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16681368}}
==About this Structure==
==About this Structure==
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[[Category: Pyrrolidine]]
[[Category: Pyrrolidine]]
[[Category: Serine protease]]
[[Category: Serine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:25:45 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:11:49 2008''

Revision as of 12:11, 28 July 2008

Image:2fxr.png

Template:STRUCTURE 2fxr

human beta tryptase II complexed with activated ketone inhibitor CRA-29382

Template:ABSTRACT PUBMED 16681368

About this Structure

2FXR 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

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