6wjc
From Proteopedia
(Difference between revisions)
| Line 1: | Line 1: | ||
==Muscarinic acetylcholine receptor 1 - muscarinic toxin 7 complex== | ==Muscarinic acetylcholine receptor 1 - muscarinic toxin 7 complex== | ||
| - | <StructureSection load='6wjc' size='340' side='right'caption='[[6wjc]]' scene=''> | + | <StructureSection load='6wjc' size='340' side='right'caption='[[6wjc]], [[Resolution|resolution]] 2.55Å' 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=6WJC OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6WJC FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[6wjc]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Bmnh_1946.1.20.48 Bmnh 1946.1.20.48] and [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6WJC OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6WJC FirstGlance]. <br> |
| - | </td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6wjc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6wjc OCA], [http://pdbe.org/6wjc PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6wjc RCSB], [http://www.ebi.ac.uk/pdbsum/6wjc PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6wjc 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=ACM:ACETAMIDE'>ACM</scene>, <scene name='pdbligand=OIN:(1R,5S)-8-METHYL-8-AZABICYCLO[3.2.1]OCT-3-YL+(2R)-3-HYDROXY-2-PHENYLPROPANOATE'>OIN</scene>, <scene name='pdbligand=Y01:CHOLESTEROL+HEMISUCCINATE'>Y01</scene></td></tr> |
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CHRM1 ([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='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6wjc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6wjc OCA], [http://pdbe.org/6wjc PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6wjc RCSB], [http://www.ebi.ac.uk/pdbsum/6wjc PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6wjc ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/ACM1_HUMAN ACM1_HUMAN]] The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover. [[http://www.uniprot.org/uniprot/3SIM7_DENAN 3SIM7_DENAN]] Binds irreversibly and specifically to an allosteric site of the muscarinic acetylcholine M1 receptor (CHRM1).<ref>PMID:10799315</ref> <ref>PMID:11562434</ref> <ref>PMID:12488533</ref> <ref>PMID:21557730</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Muscarinic toxins (MTs) are natural toxins produced by mamba snakes that primarily bind to muscarinic acetylcholine receptors (MAChRs) and modulate their function. Despite their similar primary and tertiary structures, MTs show distinct binding selectivity toward different MAChRs. The molecular details of how MTs distinguish MAChRs are not well understood. Here, we present the crystal structure of M1AChR in complex with MT7, a subtype-selective anti-M1AChR snake venom toxin. The structure reveals the molecular basis of the extreme subtype specificity of MT7 for M1AChR and the mechanism by which it regulates receptor function. Through in vitro engineering of MT7 finger regions that was guided by the structure, we have converted the selectivity from M1AChR toward M2AChR, suggesting that the three-finger fold is a promising scaffold for developing G protein-coupled receptor modulators. | ||
| + | |||
| + | Structure and selectivity engineering of the M1 muscarinic receptor toxin complex.,Maeda S, Xu J, N Kadji FM, Clark MJ, Zhao J, Tsutsumi N, Aoki J, Sunahara RK, Inoue A, Garcia KC, Kobilka BK Science. 2020 Jul 10;369(6500):161-167. doi: 10.1126/science.aax2517. PMID:32646996<ref>PMID:32646996</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 6wjc" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Bmnh 1946 1.20 48]] | ||
| + | [[Category: Human]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Kobilka | + | [[Category: Lysozyme]] |
| - | [[Category: Maeda S]] | + | [[Category: Kobilka, B K]] |
| + | [[Category: Maeda, S]] | ||
| + | [[Category: Gpcr]] | ||
| + | [[Category: Membrane protein]] | ||
| + | [[Category: Natural toxin]] | ||
Revision as of 11:44, 22 July 2020
Muscarinic acetylcholine receptor 1 - muscarinic toxin 7 complex
| |||||||||||
