4ps0

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==Caspase-8 specific unnatural amino acid peptides==
==Caspase-8 specific unnatural amino acid peptides==
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<StructureSection load='4ps0' size='340' side='right' caption='[[4ps0]], [[Resolution|resolution]] 1.63&Aring;' scene=''>
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<StructureSection load='4ps0' size='340' side='right'caption='[[4ps0]], [[Resolution|resolution]] 1.63&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4ps0]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4PS0 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4PS0 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4ps0]] 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=4PS0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4PS0 FirstGlance]. <br>
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</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=1U8:(3S)-3-AMINO-5-[(2,6-DIMETHYLBENZOYL)OXY]-4-OXOPENTANOIC+ACID'>1U8</scene>, <scene name='pdbligand=BAL:BETA-ALANINE'>BAL</scene>, <scene name='pdbligand=HYP:4-HYDROXYPROLINE'>HYP</scene></td></tr>
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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]] 1.63&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4jj7|4jj7]], [[4jj8|4jj8]], [[4prz|4prz]], [[4pry|4pry]], [[4jje|4jje]], [[4ps1|4ps1]]</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=1U8:(3S)-3-AMINO-5-[(2,6-DIMETHYLBENZOYL)OXY]-4-OXOPENTANOIC+ACID'>1U8</scene>, <scene name='pdbligand=BAL:BETA-ALANINE'>BAL</scene>, <scene name='pdbligand=HYP:4-HYDROXYPROLINE'>HYP</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Caspase-3 Caspase-3], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.56 3.4.22.56] </span></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=4ps0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ps0 OCA], [https://pdbe.org/4ps0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ps0 RCSB], [https://www.ebi.ac.uk/pdbsum/4ps0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ps0 ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ps0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ps0 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ps0 RCSB], [http://www.ebi.ac.uk/pdbsum/4ps0 PDBsum]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/CASP3_HUMAN CASP3_HUMAN]] Involved in the activation cascade of caspases responsible for apoptosis execution. At the onset of apoptosis it proteolytically cleaves poly(ADP-ribose) polymerase (PARP) at a '216-Asp-|-Gly-217' bond. Cleaves and activates sterol regulatory element binding proteins (SREBPs) between the basic helix-loop-helix leucine zipper domain and the membrane attachment domain. Cleaves and activates caspase-6, -7 and -9. Involved in the cleavage of huntingtin. Triggers cell adhesion in sympathetic neurons through RET cleavage.<ref>PMID:7596430</ref> <ref>PMID:21357690</ref>
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[https://www.uniprot.org/uniprot/CASP3_HUMAN CASP3_HUMAN] Involved in the activation cascade of caspases responsible for apoptosis execution. At the onset of apoptosis it proteolytically cleaves poly(ADP-ribose) polymerase (PARP) at a '216-Asp-|-Gly-217' bond. Cleaves and activates sterol regulatory element binding proteins (SREBPs) between the basic helix-loop-helix leucine zipper domain and the membrane attachment domain. Cleaves and activates caspase-6, -7 and -9. Involved in the cleavage of huntingtin. Triggers cell adhesion in sympathetic neurons through RET cleavage.<ref>PMID:7596430</ref> <ref>PMID:21357690</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Caspases are fundamental to many essential biological processes, including apoptosis, differentiation, and inflammation. Unregulated caspase activity is also implicated in the development and progression of several diseases, such as cancer, neurodegenerative disorders, and sepsis. Unfortunately, it is difficult to determine exactly which caspase(s) of the 11 isoforms that humans express is responsible for specific biological functions. This lack of resolution is primarily due to highly homologous active sites and overlapping substrates. Currently available peptide-based inhibitors and probes are based on specificity garnered from peptide substrate libraries. For example, the canonical tetrapeptide LETD was discovered as the canonical sequence that is optimally recognized by caspase-8; however, LETD-based inhibitors and substrates promiscuously bind to other isoforms with equal affinity, including caspases-3, -6, and -9. In order to mitigate this problem, we report the identification of a new series of compounds that are &gt;100-fold selective for inhibiting the initiator caspases-8 and -9 over the executioner caspases-3, -6, and -7.
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Selective inhibition of initiator versus executioner caspases using small peptides containing unnatural amino acids.,Vickers CJ, Gonzalez-Paez GE, Litwin KM, Umotoy JC, Coutsias EA, Wolan DW ACS Chem Biol. 2014 Oct 17;9(10):2194-8. doi: 10.1021/cb5004256. Epub 2014 Aug 5. PMID:25079698<ref>PMID:25079698</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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==See Also==
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</div>
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*[[Caspase 3D structures|Caspase 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Caspase-3]]
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[[Category: Homo sapiens]]
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[[Category: Gonzalez-Paez, G E]]
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[[Category: Large Structures]]
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[[Category: Vickers, C J]]
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[[Category: Gonzalez-Paez GE]]
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[[Category: Wolan, D W]]
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[[Category: Vickers CJ]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Wolan DW]]
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[[Category: Protease]]
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Current revision

Caspase-8 specific unnatural amino acid peptides

PDB ID 4ps0

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