8x7a
From Proteopedia
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8x7a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8x7a OCA], [https://pdbe.org/8x7a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8x7a RCSB], [https://www.ebi.ac.uk/pdbsum/8x7a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8x7a 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=8x7a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8x7a OCA], [https://pdbe.org/8x7a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8x7a RCSB], [https://www.ebi.ac.uk/pdbsum/8x7a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8x7a ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| - | == | + | <div style="background-color:#fffaf0;"> |
| - | + | == Publication Abstract from PubMed == | |
| + | The prostacyclin (PGI(2)) receptor (IP) is a G(s)-coupled receptor associated with blood pressure regulation, allergy, and inflammatory response. It is a main therapeutic target for pulmonary arterial hypertension (PAH) and several other diseases. Here we report cryo-electron microscopy (cryo-EM) structures of the human IP-G(s) complex bound with two anti-PAH drugs, treprostinil and MRE-269 (active form of selexipag), at global resolutions of 2.56 and 2.41 angstrom, respectively. These structures revealed distinct features governing IP ligand binding, receptor activation, and G protein coupling. Moreover, comparison of the activated IP structures uncovered the mechanism and key residues that determine the superior selectivity of MRE-269 over treprostinil. Combined with molecular docking and functional studies, our structures provide insight into agonist selectivity, ligand recognition, receptor activation, and G protein coupling. Our results provide a structural template for further improving IP-targeting drugs to reduce off-target activation of prostanoid receptors and adverse effects. | ||
| + | |||
| + | Molecular recognition and activation of the prostacyclin receptor by anti-pulmonary arterial hypertension drugs.,Wang JJ, Jin S, Zhang H, Xu Y, Hu W, Jiang Y, Chen C, Wang DW, Xu HE, Wu C Sci Adv. 2024 Feb 9;10(6):eadk5184. doi: 10.1126/sciadv.adk5184. Epub 2024 Feb 9. PMID:38335293<ref>PMID:38335293</ref> | ||
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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 8x7a" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
Current revision
Treprostinil bound Prostacyclin Receptor G protein complex
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Categories: Homo sapiens | Large Structures | Chen C | Hu W | Jiang Y | Jin S | Wang DW | Wang JJ | Wu C | Xu HE | Xu Y | Zhang H
