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7dd7
From Proteopedia
(Difference between revisions)
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==Structure of Calcium-Sensing Receptor in complex with Evocalcet== | ==Structure of Calcium-Sensing Receptor in complex with Evocalcet== | ||
| - | <StructureSection load='7dd7' size='340' side='right'caption='[[7dd7]]' scene=''> | + | <StructureSection load='7dd7' size='340' side='right'caption='[[7dd7]], [[Resolution|resolution]] 3.20Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7DD7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7DD7 FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[7dd7]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Chick Chick]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7DD7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7DD7 FirstGlance]. <br> |
| - | </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=7dd7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7dd7 OCA], [https://pdbe.org/7dd7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7dd7 RCSB], [https://www.ebi.ac.uk/pdbsum/7dd7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7dd7 ProSAT]</span></td></tr> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=H43:2-[4-[(3S)-3-[[(1R)-1-naphthalen-1-ylethyl]amino]pyrrolidin-1-yl]phenyl]ethanoic+acid'>H43</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=TRP:TRYPTOPHAN'>TRP</scene></td></tr> |
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CASR ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9031 CHICK])</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=7dd7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7dd7 OCA], [https://pdbe.org/7dd7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7dd7 RCSB], [https://www.ebi.ac.uk/pdbsum/7dd7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7dd7 ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Calcium-sensing receptor (CaSR) is a class C G protein-coupled receptor (GPCR) that plays an important role in calcium homeostasis and parathyroid hormone secretion. Here, we present multiple cryo-electron microscopy structures of full-length CaSR in distinct ligand-bound states. Ligands (Ca(2+) and l-tryptophan) bind to the extracellular domain of CaSR and induce large-scale conformational changes, leading to the closure of two heptahelical transmembrane domains (7TMDs) for activation. The positive modulator (evocalcet) and the negative allosteric modulator (NPS-2143) occupy the similar binding pocket in 7TMD. The binding of NPS-2143 causes a considerable rearrangement of two 7TMDs, forming an inactivated TM6/TM6 interface. Moreover, a total of 305 disease-causing missense mutations of CaSR have been mapped to the structure in the active state, creating hotspot maps of five clinical endocrine disorders. Our results provide a structural framework for understanding the activation, allosteric modulation mechanism, and disease therapy for class C GPCRs. | ||
| + | |||
| + | Structural basis for activation and allosteric modulation of full-length calcium-sensing receptor.,Wen T, Wang Z, Chen X, Ren Y, Lu X, Xing Y, Lu J, Chang S, Zhang X, Shen Y, Yang X Sci Adv. 2021 Jun 4;7(23). pii: 7/23/eabg1483. doi: 10.1126/sciadv.abg1483. Print, 2021 Jun. PMID:34088669<ref>PMID:34088669</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 7dd7" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Chick]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Shen | + | [[Category: Shen, Y Q]] |
| - | [[Category: Wen | + | [[Category: Wen, T L]] |
| - | [[Category: Yang X]] | + | [[Category: Yang, X]] |
| + | [[Category: Calcium-sensing receptor]] | ||
| + | [[Category: Casr]] | ||
| + | [[Category: Evocalcet]] | ||
| + | [[Category: Membrane protein]] | ||
Current revision
Structure of Calcium-Sensing Receptor in complex with Evocalcet
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