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| | <StructureSection load='5l8o' size='340' side='right'caption='[[5l8o]], [[Resolution|resolution]] 2.39Å' scene=''> | | <StructureSection load='5l8o' size='340' side='right'caption='[[5l8o]], [[Resolution|resolution]] 2.39Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[5l8o]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5L8O OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5L8O FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[5l8o]] is a 3 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=5L8O OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5L8O FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CHD:CHOLIC+ACID'>CHD</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.39Å</td></tr> |
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">FABP6, ILBP, ILLBP ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CHD:CHOLIC+ACID'>CHD</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene></td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=5l8o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5l8o OCA], [http://pdbe.org/5l8o PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5l8o RCSB], [http://www.ebi.ac.uk/pdbsum/5l8o PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5l8o ProSAT]</span></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=5l8o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5l8o OCA], [https://pdbe.org/5l8o PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5l8o RCSB], [https://www.ebi.ac.uk/pdbsum/5l8o PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5l8o ProSAT]</span></td></tr> |
| | </table> | | </table> |
| | == Function == | | == 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> | + | [https://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;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
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| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Human]] | + | [[Category: Homo sapiens]] |
| | [[Category: Large Structures]] | | [[Category: Large Structures]] |
| - | [[Category: Davenport, R]] | + | [[Category: Davenport R]] |
| - | [[Category: Hendrick, A]] | + | [[Category: Hendrick A]] |
| - | [[Category: Leonard, P M]] | + | [[Category: Leonard PM]] |
| - | [[Category: Mitchell, P]] | + | [[Category: Mitchell P]] |
| - | [[Category: Mueller, I]] | + | [[Category: Mueller I]] |
| - | [[Category: Cholate]]
| + | |
| - | [[Category: Fabp6]]
| + | |
| - | [[Category: Fatty acid binding protein 6]]
| + | |
| - | [[Category: Fragment]]
| + | |
| - | [[Category: Gastrotropin]]
| + | |
| - | [[Category: I-babp]]
| + | |
| - | [[Category: Ileal]]
| + | |
| - | [[Category: Ileal bile acid binding protein]]
| + | |
| - | [[Category: Lipid binding protein]]
| + | |
| Structural highlights
Function
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.[1]
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[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Fang C, Dean J, Smith JW. A novel variant of ileal bile acid binding protein is up-regulated through nuclear factor-kappaB activation in colorectal adenocarcinoma. Cancer Res. 2007 Oct 1;67(19):9039-46. PMID:17909007 doi:http://dx.doi.org/67/19/9039
- ↑ 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. Identification and Investigation of Novel Binding Fragments in the Fatty Acid Binding Protein 6 (FABP6). J Med Chem. 2016 Aug 18. PMID:27500412 doi:http://dx.doi.org/10.1021/acs.jmedchem.6b00869
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