2fpz

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(New page: 200px<br /> <applet load="2fpz" size="450" color="white" frame="true" align="right" spinBox="true" caption="2fpz, resolution 2.000&Aring;" /> '''Human tryptase wit...)
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[[Image:2fpz.gif|left|200px]]<br />
 
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<applet load="2fpz" size="450" color="white" frame="true" align="right" spinBox="true"
 
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caption="2fpz, resolution 2.000&Aring;" />
 
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'''Human tryptase with 2-amino benzimidazole'''<br />
 
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==Overview==
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==Human tryptase with 2-amino benzimidazole==
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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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<StructureSection load='2fpz' size='340' side='right'caption='[[2fpz]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2fpz]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2FPZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2FPZ FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=270:2H-BENZOIMIDAZOL-2-YLAMINE'>270</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2fpz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2fpz OCA], [https://pdbe.org/2fpz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2fpz RCSB], [https://www.ebi.ac.uk/pdbsum/2fpz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2fpz ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/TRYB2_HUMAN TRYB2_HUMAN] Tryptase is the major neutral protease present in mast cells and is secreted upon the coupled activation-degranulation response of this cell type. Has an immunoprotective role during bacterial infection. Required to efficiently combat K.pneumoniae infection (By similarity).
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fp/2fpz_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2fpz ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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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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==About this Structure==
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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<ref>PMID:16681368</ref>
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2FPZ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with 270 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2FPZ OCA].
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==Reference==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16681368 16681368]
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</div>
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[[Category: Homo sapiens]]
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<div class="pdbe-citations 2fpz" style="background-color:#fffaf0;"></div>
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[[Category: Single protein]]
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[[Category: Tryptase]]
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[[Category: Somoza, J.R.]]
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[[Category: 270]]
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[[Category: drug design]]
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[[Category: serine protease]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 22:09:15 2007''
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==See Also==
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*[[Tryptase|Tryptase]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Somoza JR]]

Current revision

Human tryptase with 2-amino benzimidazole

PDB ID 2fpz

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