4z9g
From Proteopedia
(Difference between revisions)
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<StructureSection load='4z9g' size='340' side='right' caption='[[4z9g]], [[Resolution|resolution]] 3.18Å' scene=''> | <StructureSection load='4z9g' size='340' side='right' caption='[[4z9g]], [[Resolution|resolution]] 3.18Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[4z9g]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4Z9G OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4Z9G FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[4z9g]] 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=4Z9G OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4Z9G FirstGlance]. <br> |
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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=SO4:SULFATE+ION'>SO4</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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=SO4:SULFATE+ION'>SO4</scene></td></tr> | ||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4k5y|4k5y]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4k5y|4k5y]]</td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CRHR1, CRFR, CRFR1, CRHR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> | ||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </span></td></tr> | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </span></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=4z9g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4z9g OCA], [http://pdbe.org/4z9g PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4z9g RCSB], [http://www.ebi.ac.uk/pdbsum/4z9g PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4z9g ProSAT]</span></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=4z9g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4z9g OCA], [http://pdbe.org/4z9g PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4z9g RCSB], [http://www.ebi.ac.uk/pdbsum/4z9g PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4z9g ProSAT]</span></td></tr> | ||
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== Function == | == 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 == | ||
| + | The structural analysis of class B G protein-coupled receptors (GPCR), cell surface proteins responding to peptide hormones, has until recently been restricted to the extracellular domain (ECD). Corticotropin-releasing factor receptor type 1 (CRF1R) is a class B receptor mediating stress response and also considered a drug target for depression and anxiety. Here we report the crystal structure of the transmembrane domain of human CRF1R in complex with the small-molecule antagonist CP-376395 in a hexagonal setting with translational non-crystallographic symmetry. Molecular dynamics and metadynamics simulations on this novel structure and the existing TMD structure for CRF1R provides insight as to how the small molecule ligand gains access to the induced-fit allosteric binding site with implications for the observed selectivity against CRF2R. Furthermore, molecular dynamics simulations performed using a full-length receptor model point to key interactions between the ECD and extracellular loop 3 of the TMD providing insight into the full inactive state of multidomain class B GPCRs. | ||
| + | |||
| + | Decoding Corticotropin-Releasing Factor Receptor Type 1 Crystal Structures.,Dore AS, Bortolato A, Hollenstein K, Cheng RKY, Read RJ, Marshall FH Curr Mol Pharmacol. 2017;10(4):334-344. doi: 10.2174/1874467210666170110114727. PMID:28183242<ref>PMID:28183242</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 4z9g" style="background-color:#fffaf0;"></div> | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Human]] | ||
[[Category: Lysozyme]] | [[Category: Lysozyme]] | ||
[[Category: Bortolato, A]] | [[Category: Bortolato, A]] | ||
Revision as of 07:30, 6 December 2017
Crystal structure of human corticotropin-releasing factor receptor 1 (CRF1R) in complex with the antagonist CP-376395 in a hexagonal setting with translational non-crystallographic symmetry
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Categories: Human | Lysozyme | Bortolato, A | Cheng, R K.Y | Dore, A S | Hollenstein, K | Marshall, F H | Read, R J | Family b | G-protein | Gpcr | Hexagonal | Membrane | Membrane protein | Receptor | Signaling protein | Tnc
