2fxr

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[[Image:2fxr.gif|left|200px]]
[[Image:2fxr.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2fxr |SIZE=350|CAPTION= <scene name='initialview01'>2fxr</scene>, resolution 2.50&Aring;
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The line below this paragraph, containing "STRUCTURE_2fxr", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=C3A:ALLYL+{(1S)-1-[(5-{4-[(2,3-DIHYDRO-1H-INDEN-2-YLAMINO)CARBONYL]BENZYL}-1,2,4-OXADIAZOL-3-YL)CARBONYL]-3-PYRROLIDIN-3-YLPROPYL}CARBAMATE'>C3A</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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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>
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or leave the SCENE parameter empty for the default display.
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|GENE= TPSB2, TPS2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2fxr| PDB=2fxr | SCENE= }}
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|RELATEDENTRY=[[2fww|2FWW]], [[2fx4|2FX4]], [[2fx6|2FX6]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2fxr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2fxr OCA], [http://www.ebi.ac.uk/pdbsum/2fxr PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2fxr RCSB]</span>
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}}
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'''human beta tryptase II complexed with activated ketone inhibitor CRA-29382'''
'''human beta tryptase II complexed with activated ketone inhibitor CRA-29382'''
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[[Category: Tryptase]]
[[Category: Tryptase]]
[[Category: Katz, B A.]]
[[Category: Katz, B A.]]
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[[Category: activated ketone inhibitor]]
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[[Category: Activated ketone inhibitor]]
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[[Category: cra-29382]]
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[[Category: Cra-29382]]
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[[Category: pyrrolidine]]
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[[Category: Pyrrolidine]]
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[[Category: serine protease]]
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[[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 Mar 31 03:09:05 2008''
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Revision as of 01:25, 4 May 2008

Image:2fxr.gif

Template:STRUCTURE 2fxr

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. 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 Sun May 4 04:25:45 2008

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OCA

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