6m9t

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'''Unreleased structure'''
 
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The entry 6m9t is ON HOLD until Paper Publication
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==Crystal structure of EP3 receptor bound to misoprostol-FA==
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<StructureSection load='6m9t' size='340' side='right'caption='[[6m9t]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6m9t]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_virus_T4 Escherichia virus T4] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6M9T OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6M9T FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.5&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=J9P:7-[(1~{R},2~{R},3~{R})-2-[(~{E},4~{S})-4-methyl-4-oxidanyl-oct-1-enyl]-3-oxidanyl-5-oxidanylidene-cyclopentyl]heptanoic+acid'>J9P</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=SO4:SULFATE+ION'>SO4</scene></td></tr>
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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=6m9t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6m9t OCA], [https://pdbe.org/6m9t PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6m9t RCSB], [https://www.ebi.ac.uk/pdbsum/6m9t PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6m9t ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/ENLYS_BPT4 ENLYS_BPT4] Endolysin with lysozyme activity that degrades host peptidoglycans and participates with the holin and spanin proteins in the sequential events which lead to the programmed host cell lysis releasing the mature viral particles. Once the holin has permeabilized the host cell membrane, the endolysin can reach the periplasm and break down the peptidoglycan layer.<ref>PMID:22389108</ref> [https://www.uniprot.org/uniprot/PE2R3_HUMAN PE2R3_HUMAN] Receptor for prostaglandin E2 (PGE2) (PubMed:8307176, PubMed:7883006, PubMed:8117308, PubMed:8135729, PubMed:7981210). The activity of this receptor can couple to both the inhibition of adenylate cyclase mediated by G(i) proteins, and to an elevation of intracellular calcium (PubMed:7883006, PubMed:8117308, PubMed:8135729, PubMed:7981210). Required for normal development of fever in response to pyrinogens, including IL1B, prostaglandin E2 and bacterial lipopolysaccharide (LPS). Required for normal potentiation of platelet aggregation by prostaglandin E2, and thus plays a role in the regulation of blood coagulation. Required for increased HCO3(-) secretion in the duodenum in response to mucosal acidification, and thereby contributes to the protection of the mucosa against acid-induced ulceration. Not required for normal kidney function, normal urine volume and osmolality (By similarity).[UniProtKB:P30557]<ref>PMID:7883006</ref> <ref>PMID:7981210</ref> <ref>PMID:8117308</ref> <ref>PMID:8135729</ref> <ref>PMID:8307176</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Misoprostol is a life-saving drug in many developing countries for women at risk of post-partum hemorrhaging owing to its affordability, stability, ease of administration and clinical efficacy. However, misoprostol lacks receptor and tissue selectivities, and thus its use is accompanied by a number of serious side effects. The development of pharmacological agents combining the advantages of misoprostol with improved selectivity is hindered by the absence of atomic details of misoprostol action in labor induction. Here, we present the 2.5 A resolution crystal structure of misoprostol free-acid form bound to the myometrium labor-inducing prostaglandin E2 receptor 3 (EP3). The active state structure reveals a completely enclosed binding pocket containing a structured water molecule that coordinates misoprostol's ring structure. Modeling of selective agonists in the EP3 structure reveals rationales for selectivity. These findings will provide the basis for the next generation of uterotonic drugs that will be suitable for administration in low resource settings.
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Authors:
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Crystal structure of misoprostol bound to the labor inducer prostaglandin E2 receptor.,Audet M, White KL, Breton B, Zarzycka B, Han GW, Lu Y, Gati C, Batyuk A, Popov P, Velasquez J, Manahan D, Hu H, Weierstall U, Liu W, Shui W, Katritch V, Cherezov V, Hanson MA, Stevens RC Nat Chem Biol. 2019 Jan;15(1):11-17. doi: 10.1038/s41589-018-0160-y. Epub 2018, Dec 3. PMID:30510194<ref>PMID:30510194</ref>
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Description:
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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<div class="pdbe-citations 6m9t" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Escherichia virus T4]]
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Audet M]]
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[[Category: Batyuk A]]
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[[Category: Breton B]]
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[[Category: Cherezov V]]
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[[Category: Gati C]]
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[[Category: Han GW]]
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[[Category: Hanson MA]]
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[[Category: Hu H]]
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[[Category: Katrich V]]
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[[Category: Liu W]]
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[[Category: Lu Y]]
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[[Category: Manahan D]]
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[[Category: Popov P]]
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[[Category: Shui W]]
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[[Category: Stevens RC]]
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[[Category: Velasquez J]]
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[[Category: Weierstall U]]
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[[Category: White KL]]
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[[Category: Zarzycka B]]

Current revision

Crystal structure of EP3 receptor bound to misoprostol-FA

PDB ID 6m9t

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