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4k5y
From Proteopedia
(Difference between revisions)
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| - | + | ==Crystal structure of human corticotropin-releasing factor receptor 1 (CRF1R) in complex with the antagonist CP-376395== | |
| - | + | <StructureSection load='4k5y' size='340' side='right' caption='[[4k5y]], [[Resolution|resolution]] 2.98Å' scene=''> | |
| - | {{ | + | == Structural highlights == |
| - | + | <table><tr><td colspan='2'>[[4k5y]] 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=4K5Y OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4K5Y FirstGlance]. <br> | |
| - | ==Function== | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=1Q5:3,6-DIMETHYL-N-(PENTAN-3-YL)-2-(2,4,6-TRIMETHYLPHENOXY)PYRIDIN-4-AMINE'>1Q5</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=PGW:(1R)-2-{[(S)-{[(2S)-2,3-DIHYDROXYPROPYL]OXY}(HYDROXY)PHOSPHORYL]OXY}-1-[(HEXADECANOYLOXY)METHYL]ETHYL+(9Z)-OCTADEC-9-ENOATE'>PGW</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> |
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3eht|3eht]], [[3ehu|3ehu]], [[3ehs|3ehs]]</td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CRF1R, CRFR, CRFR1, CRHR, CRHR1, E ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=4k5y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4k5y OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4k5y RCSB], [http://www.ebi.ac.uk/pdbsum/4k5y PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
[[http://www.uniprot.org/uniprot/CRFR1_HUMAN CRFR1_HUMAN]] Receptor for corticotropin releasing factor (CRH). Shows high-affinity CRF binding. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.<ref>PMID:18801728</ref> | [[http://www.uniprot.org/uniprot/CRFR1_HUMAN CRFR1_HUMAN]] Receptor for corticotropin releasing factor (CRH). Shows high-affinity CRF binding. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.<ref>PMID:18801728</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Structural analysis of class B G-protein-coupled receptors (GPCRs), cell-surface proteins that respond to peptide hormones, has been restricted to the amino-terminal extracellular domain, thus providing little understanding of the membrane-spanning signal transduction domain. The corticotropin-releasing factor receptor type 1 is a class B receptor which mediates the response to stress and has been considered a drug target for depression and anxiety. Here we report the crystal structure of the transmembrane domain of the human corticotropin-releasing factor receptor type 1 in complex with the small-molecule antagonist CP-376395. The structure provides detailed insight into the architecture of class B receptors. Atomic details of the interactions of the receptor with the non-peptide ligand that binds deep within the receptor are described. This structure provides a model for all class B GPCRs and may aid in the design of new small-molecule drugs for diseases of brain and metabolism. | ||
| + | |||
| + | Structure of class B GPCR corticotropin-releasing factor receptor 1.,Hollenstein K, Kean J, Bortolato A, Cheng RK, Dore AS, Jazayeri A, Cooke RM, Weir M, Marshall FH Nature. 2013 Jul 25;499(7459):438-43. doi: 10.1038/nature12357. Epub 2013 Jul 17. PMID:23863939<ref>PMID:23863939</ref> | ||
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | == | + | ==See Also== |
| - | + | *[[Lysozyme 3D structures|Lysozyme 3D structures]] | |
| - | [[Category: Bortolato, A | + | == References == |
| - | [[Category: Cheng, R K.Y | + | <references/> |
| - | [[Category: Cooke, R M | + | __TOC__ |
| - | [[Category: Dore, A S | + | </StructureSection> |
| - | [[Category: Hollenstein, K | + | [[Category: Human]] |
| - | [[Category: Jazayeri, A | + | [[Category: Bortolato, A]] |
| - | [[Category: Kean, J | + | [[Category: Cheng, R K.Y]] |
| - | [[Category: Marshall, F H | + | [[Category: Cooke, R M]] |
| - | [[Category: Weir, M | + | [[Category: Dore, A S]] |
| - | + | [[Category: Hollenstein, K]] | |
| + | [[Category: Jazayeri, A]] | ||
| + | [[Category: Kean, J]] | ||
| + | [[Category: Marshall, F H]] | ||
| + | [[Category: Weir, M]] | ||
[[Category: Family b]] | [[Category: Family b]] | ||
[[Category: G-protein]] | [[Category: G-protein]] | ||
Revision as of 19:25, 25 December 2014
Crystal structure of human corticotropin-releasing factor receptor 1 (CRF1R) in complex with the antagonist CP-376395
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Categories: Human | Bortolato, A | Cheng, R K.Y | Cooke, R M | Dore, A S | Hollenstein, K | Jazayeri, A | Kean, J | Marshall, F H | Weir, M | Family b | G-protein | Gpcr | Membrane | Membrane protein | Receptor | Signalling protein
