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2p2c
From Proteopedia
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| - | [[Image:2p2c.gif|left|200px]]<br /><applet load="2p2c" size="350" color="white" frame="true" align="right" spinBox="true" | ||
| - | caption="2p2c, resolution 3.24Å" /> | ||
| - | '''Inhibition of caspase-2 by a designed ankyrin repeat protein (DARPin)'''<br /> | ||
| - | == | + | ==Inhibition of caspase-2 by a designed ankyrin repeat protein (DARPin)== |
| - | Specific and potent caspase inhibitors are indispensable for the | + | <StructureSection load='2p2c' size='340' side='right'caption='[[2p2c]], [[Resolution|resolution]] 3.24Å' scene=''> |
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[2p2c]] is a 18 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=2P2C OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2P2C FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.24Å</td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2p2c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p2c OCA], [https://pdbe.org/2p2c PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2p2c RCSB], [https://www.ebi.ac.uk/pdbsum/2p2c PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2p2c ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/CASP2_HUMAN CASP2_HUMAN] Involved in the activation cascade of caspases responsible for apoptosis execution. Might function by either activating some proteins required for cell death or inactivating proteins necessary for cell survival. | ||
| + | == Evolutionary Conservation == | ||
| + | [[Image:Consurf_key_small.gif|200px|right]] | ||
| + | Check<jmol> | ||
| + | <jmolCheckbox> | ||
| + | <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/p2/2p2c_consurf.spt"</scriptWhenChecked> | ||
| + | <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | ||
| + | <text>to colour the structure by Evolutionary Conservation</text> | ||
| + | </jmolCheckbox> | ||
| + | </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=2p2c ConSurf]. | ||
| + | <div style="clear:both"></div> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Specific and potent caspase inhibitors are indispensable for the dissection of the intricate pathways leading to apoptosis. We selected a designed ankyrin repeat protein (DARPin) from a combinatorial library that inhibits caspase-2 in vitro with a subnanomolar inhibition constant and, in contrast to the peptidic caspase inhibitors, with very high specificity for this particular caspase. The crystal structure of this inhibitor (AR_F8) in complex with caspase-2 reveals the molecular basis for the specificity and, together with kinetic analyses, the allosteric mechanism of inhibition. The structure also shows a conformation of the active site that can be exploited for the design of inhibitory compounds. AR_F8 is a specific inhibitor of an initiator caspase and has the potential to help identify the function of caspase-2 in the complex biological apoptotic signaling network. | ||
| - | + | Inhibition of caspase-2 by a designed ankyrin repeat protein: specificity, structure, and inhibition mechanism.,Schweizer A, Roschitzki-Voser H, Amstutz P, Briand C, Gulotti-Georgieva M, Prenosil E, Binz HK, Capitani G, Baici A, Pluckthun A, Grutter MG Structure. 2007 May;15(5):625-36. PMID:17502107<ref>PMID:17502107</ref> | |
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| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | <div class="pdbe-citations 2p2c" style="background-color:#fffaf0;"></div> | |
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| - | + | ==See Also== | |
| + | *[[Caspase 3D structures|Caspase 3D structures]] | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Briand C]] | ||
| + | [[Category: Capitani G]] | ||
| + | [[Category: Gruetter MG]] | ||
| + | [[Category: Roschitzki Voser H]] | ||
Current revision
Inhibition of caspase-2 by a designed ankyrin repeat protein (DARPin)
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