3ns7

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[[Image:3ns7.png|left|200px]]
 
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{{STRUCTURE_3ns7| PDB=3ns7 | SCENE= }}
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==Succinic Acid Amides as P2-P3 Replacements for Inhibitors of Interleukin-1beta Converting Enzyme (ICE or Caspase 1)==
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<StructureSection load='3ns7' size='340' side='right'caption='[[3ns7]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3ns7]] is a 2 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=3NS7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3NS7 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]] 2.6&#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=3NS:(3S)-4-HYDROXY-3-{[(2S)-4-{[2-(2-METHYL-1H-BENZIMIDAZOL-1-YL)ETHYL]AMINO}-2-(1-METHYLETHYL)-4-OXOBUTANOYL]AMINO}BUTANOIC+ACID'>3NS</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=3ns7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ns7 OCA], [https://pdbe.org/3ns7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3ns7 RCSB], [https://www.ebi.ac.uk/pdbsum/3ns7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3ns7 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/CASP1_HUMAN CASP1_HUMAN] Thiol protease that cleaves IL-1 beta between an Asp and an Ala, releasing the mature cytokine which is involved in a variety of inflammatory processes. Important for defense against pathogens. Cleaves and activates sterol regulatory element binding proteins (SREBPs). Can also promote apoptosis.<ref>PMID:7876192</ref> <ref>PMID:15498465</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Succinic acid amides have been found to be effective P2-P3 scaffold replacements for peptidic ICE inhibitors. Heteroarylalkyl fragments occupying the P4 position provided access to compounds with nM affinities. Utilization of an acylal prodrug moiety was required to overcome biopharmaceutical issues which led to the identification of 17f, a potential clinical candidate.
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===Succinic Acid Amides as P2-P3 Replacements for Inhibitors of Interleukin-1beta Converting Enzyme (ICE or Caspase 1)===
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Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1).,Galatsis P, Caprathe B, Gilmore J, Thomas A, Linn K, Sheehan S, Harter W, Kostlan C, Lunney E, Stankovic C, Rubin J, Brady K, Allen H, Talanian R Bioorg Med Chem Lett. 2010 Sep 1;20(17):5184-90. Epub 2010 Jul 8. PMID:20656488<ref>PMID:20656488</ref>
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{{ABSTRACT_PUBMED_20656488}}
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==About this Structure==
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<div class="pdbe-citations 3ns7" style="background-color:#fffaf0;"></div>
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[[3ns7]] is a 2 chain structure of [[Caspase]] with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3NS7 OCA].
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==See Also==
==See Also==
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*[[Caspase|Caspase]]
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*[[Caspase 3D structures|Caspase 3D structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:020656488</ref><references group="xtra"/>
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__TOC__
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[[Category: Caspase-1]]
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Galatsis, P.]]
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[[Category: Large Structures]]
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[[Category: Cysteine protease]]
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[[Category: Galatsis P]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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Current revision

Succinic Acid Amides as P2-P3 Replacements for Inhibitors of Interleukin-1beta Converting Enzyme (ICE or Caspase 1)

PDB ID 3ns7

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