5l8i
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==crystal structure of human FABP6 apo-protein== | |
| + | <StructureSection load='5l8i' size='340' side='right' caption='[[5l8i]], [[Resolution|resolution]] 1.88Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5l8i]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5L8I OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5L8I FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=P33:3,6,9,12,15,18-HEXAOXAICOSANE-1,20-DIOL'>P33</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</scene>, <scene name='pdbligand=PGE:TRIETHYLENE+GLYCOL'>PGE</scene></td></tr> | ||
| + | <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=5l8i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5l8i OCA], [http://pdbe.org/5l8i PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5l8i RCSB], [http://www.ebi.ac.uk/pdbsum/5l8i PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5l8i ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/FABP6_HUMAN FABP6_HUMAN]] Ileal protein which stimulates gastric acid and pepsinogen secretion. Seems to be able to bind to bile salts and bilirubins. Isoform 2 is essential for the survival of colon cancer cells to bile acid-induced apoptosis.<ref>PMID:17909007</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Fatty acid binding protein 6 (FABP6) is a potential drug discovery target, which, if inhibited, may have a therapeutic benefit for the treatment of diabetes. Currently, there are no published inhibitors of FABP6, and with the target believed to be amenable to fragment-based drug discovery, a structurally enabled program was initiated. This program successfully identified fragment hits using the surface plasmon resonance (SPR) platform. Several hits were validated with SAR and were found to be displaced by the natural ligand taurocholate. We report the first crystal structure of human FABP6 in the unbound form, in complex with cholate, and with one of the key fragments. | ||
| - | + | Identification and Investigation of Novel Binding Fragments in the Fatty Acid Binding Protein 6 (FABP6).,Hendrick AG, Muller I, Willems H, Leonard PM, Irving S, Davenport R, Ito T, Reeves J, Wright S, Allen V, Wilkinson S, Heffron H, Bazin R, Turney J, Mitchell PJ J Med Chem. 2016 Aug 18. PMID:27500412<ref>PMID:27500412</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 5l8i" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Davenport, R]] | ||
| + | [[Category: Hendrick, A]] | ||
| + | [[Category: Leonard, P M]] | ||
| + | [[Category: Mitchell, P]] | ||
| + | [[Category: Mueller, I]] | ||
| + | [[Category: Fabp6]] | ||
| + | [[Category: Fatty acid binding protein 6]] | ||
| + | [[Category: Fragment]] | ||
| + | [[Category: Gastrotropin]] | ||
| + | [[Category: I-babp]] | ||
| + | [[Category: Ileal]] | ||
| + | [[Category: Ileal bile acid binding protein]] | ||
| + | [[Category: Signaling protein]] | ||
Revision as of 04:33, 9 September 2016
crystal structure of human FABP6 apo-protein
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