5dsg - Revision history

OCA at 14:08, 13 March 2024

OCA — Wed, 13 Mar 2024 14:08:18 GMT

←Older revision		Revision as of 14:08, 13 March 2024
Line 10:		Line 10:
	== Function ==		== Function ==
	[https://www.uniprot.org/uniprot/ACM4_HUMAN ACM4_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 inhibition of adenylate cyclase.[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/ACM4_HUMAN ACM4_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 inhibition of adenylate cyclase.[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>
-	<div style="background-color:#fffaf0;">
-	== Publication Abstract from PubMed ==
-	Muscarinic M1-M5 acetylcholine receptors are G-protein-coupled receptors that regulate many vital functions of the central and peripheral nervous systems. In particular, the M1 and M4 receptor subtypes have emerged as attractive drug targets for treatments of neurological disorders, such as Alzheimer's disease and schizophrenia, but the high conservation of the acetylcholine-binding pocket has spurred current research into targeting allosteric sites on these receptors. Here we report the crystal structures of the M1 and M4 muscarinic receptors bound to the inverse agonist, tiotropium. Comparison of these structures with each other, as well as with the previously reported M2 and M3 receptor structures, reveals differences in the orthosteric and allosteric binding sites that contribute to a role in drug selectivity at this important receptor family. We also report identification of a cluster of residues that form a network linking the orthosteric and allosteric sites of the M4 receptor, which provides new insight into how allosteric modulation may be transmitted between the two spatially distinct domains.
-
-	Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.,Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A Nature. 2016 Mar 17;531(7594):335-40. doi: 10.1038/nature17188. Epub 2016 Mar 9. PMID:26958838<ref>PMID:26958838</ref>
-
-	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	</div>
-	<div class="pdbe-citations 5dsg" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==

OCA at 21:57, 28 June 2023

OCA — Wed, 28 Jun 2023 21:57:40 GMT

←Older revision		Revision as of 21:57, 28 June 2023
Line 3:		Line 3:
	<StructureSection load='5dsg' size='340' side='right'caption='[[5dsg]], [[Resolution\|resolution]] 2.60Å' scene=''>		<StructureSection load='5dsg' size='340' side='right'caption='[[5dsg]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5dsg]] is a 2 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=5DSG OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5DSG FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5dsg]] is a 2 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=5DSG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5DSG FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0HK:(1R,2R,4S,5S,7S)-7-{[HYDROXY(DITHIOPHEN-2-YL)ACETYL]OXY}-9,9-DIMETHYL-3-OXA-9-AZONIATRICYCLO[3.3.1.0~2,4~]NONANE'>0HK</scene>, <scene name='pdbligand=EDT:{[-(BIS-CARBOXYMETHYL-AMINO)-ETHYL]-CARBOXYMETHYL-AMINO}-ACETIC+ACID'>EDT</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=P6G:HEXAETHYLENE+GLYCOL'>P6G</scene>, <scene name='pdbligand=PG6:1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE'>PG6</scene>~~</td></tr>~~	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 2.6Å</td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CHRM4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])~~</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0HK:(1R,2R,4S,5S,7S)-7-{[HYDROXY(DITHIOPHEN-2-YL)ACETYL]OXY}-9,9-DIMETHYL-3-OXA-9-AZONIATRICYCLO[3.3.1.0~2,4~]NONANE'>0HK</scene>, <scene name='pdbligand=EDT:{[-(BIS-CARBOXYMETHYL-AMINO)-ETHYL]-CARBOXYMETHYL-AMINO}-ACETIC+ACID'>EDT</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=P6G:HEXAETHYLENE+GLYCOL'>P6G</scene>, <scene name='pdbligand=PG6:1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE'>PG6</scene></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=5dsg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dsg OCA], [~~http~~://pdbe.org/5dsg PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5dsg RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5dsg PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5dsg 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=5dsg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dsg OCA], [https://pdbe.org/5dsg PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5dsg RCSB], [https://www.ebi.ac.uk/pdbsum/5dsg PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5dsg ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/ACM4_HUMAN ACM4_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 inhibition of adenylate cyclase.	+	[https://www.uniprot.org/uniprot/ACM4_HUMAN ACM4_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 inhibition of adenylate cyclase.[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>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 19:		Line 19:
	</div>		</div>
	<div class="pdbe-citations 5dsg" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5dsg" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Muscarinic acetylcholine receptor\|Muscarinic acetylcholine receptor]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Escherichia virus T4]]
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Christopoulos, A]]	+	[[Category: Christopoulos A]]
-	[[Category: Kobilka~~, B K~~]]	+	[[Category: Kobilka BK]]
-	[[Category: Sexton~~, P M~~]]	+	[[Category: Sexton PM]]
-	[[Category: Thal~~, D M]]~~	+	[[Category: Thal DM]]
-	~~[[Category: Antagonist]]~~	+
-	~~[[Category: Gpcr]]~~	+
-	~~[[Category: Membrane]]~~	+
-	~~[[Category: Membrane protein]]~~	+
-	~~[[Category: Signaling~~]]	+

OCA at 08:01, 8 January 2020

OCA — Wed, 08 Jan 2020 08:01:05 GMT

←Older revision		Revision as of 08:01, 8 January 2020
Line 1:		Line 1:

	==Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium==		==Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium==
-	<StructureSection load='5dsg' size='340' side='right' caption='[[5dsg]], [[Resolution\|resolution]] 2.60Å' scene=''>	+	<StructureSection load='5dsg' size='340' side='right'caption='[[5dsg]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5dsg]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DSG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DSG FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5dsg]] is a 2 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=5DSG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DSG FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0HK:(1R,2R,4S,5S,7S)-7-{[HYDROXY(DITHIOPHEN-2-YL)ACETYL]OXY}-9,9-DIMETHYL-3-OXA-9-AZONIATRICYCLO[3.3.1.0~2,4~]NONANE'>0HK</scene>, <scene name='pdbligand=EDT:{[-(BIS-CARBOXYMETHYL-AMINO)-ETHYL]-CARBOXYMETHYL-AMINO}-ACETIC+ACID'>EDT</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=P6G:HEXAETHYLENE+GLYCOL'>P6G</scene>, <scene name='pdbligand=PG6:1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE'>PG6</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0HK:(1R,2R,4S,5S,7S)-7-{[HYDROXY(DITHIOPHEN-2-YL)ACETYL]OXY}-9,9-DIMETHYL-3-OXA-9-AZONIATRICYCLO[3.3.1.0~2,4~]NONANE'>0HK</scene>, <scene name='pdbligand=EDT:{[-(BIS-CARBOXYMETHYL-AMINO)-ETHYL]-CARBOXYMETHYL-AMINO}-ACETIC+ACID'>EDT</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=P6G:HEXAETHYLENE+GLYCOL'>P6G</scene>, <scene name='pdbligand=PG6:1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE'>PG6</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CHRM4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=5dsg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dsg OCA], [http://pdbe.org/5dsg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5dsg RCSB], [http://www.ebi.ac.uk/pdbsum/5dsg PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5dsg 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=5dsg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dsg OCA], [http://pdbe.org/5dsg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5dsg RCSB], [http://www.ebi.ac.uk/pdbsum/5dsg PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5dsg ProSAT]</span></td></tr>
	</table>		</table>
Line 22:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Christopoulos, A]]		[[Category: Christopoulos, A]]
	[[Category: Kobilka, B K]]		[[Category: Kobilka, B K]]

OCA at 04:42, 21 September 2017

OCA — Thu, 21 Sep 2017 04:42:10 GMT

←Older revision		Revision as of 04:42, 21 September 2017
Line 5:		Line 5:
	<table><tr><td colspan='2'>[[5dsg]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DSG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DSG FirstGlance]. <br>		<table><tr><td colspan='2'>[[5dsg]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DSG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DSG FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0HK:(1R,2R,4S,5S,7S)-7-{[HYDROXY(DITHIOPHEN-2-YL)ACETYL]OXY}-9,9-DIMETHYL-3-OXA-9-AZONIATRICYCLO[3.3.1.0~2,4~]NONANE'>0HK</scene>, <scene name='pdbligand=EDT:{[-(BIS-CARBOXYMETHYL-AMINO)-ETHYL]-CARBOXYMETHYL-AMINO}-ACETIC+ACID'>EDT</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=P6G:HEXAETHYLENE+GLYCOL'>P6G</scene>, <scene name='pdbligand=PG6:1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE'>PG6</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0HK:(1R,2R,4S,5S,7S)-7-{[HYDROXY(DITHIOPHEN-2-YL)ACETYL]OXY}-9,9-DIMETHYL-3-OXA-9-AZONIATRICYCLO[3.3.1.0~2,4~]NONANE'>0HK</scene>, <scene name='pdbligand=EDT:{[-(BIS-CARBOXYMETHYL-AMINO)-ETHYL]-CARBOXYMETHYL-AMINO}-ACETIC+ACID'>EDT</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=P6G:HEXAETHYLENE+GLYCOL'>P6G</scene>, <scene name='pdbligand=PG6:1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE'>PG6</scene></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=5dsg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dsg OCA], [http://pdbe.org/5dsg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5dsg RCSB], [http://www.ebi.ac.uk/pdbsum/5dsg PDBsum]</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=5dsg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dsg OCA], [http://pdbe.org/5dsg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5dsg RCSB], [http://www.ebi.ac.uk/pdbsum/5dsg PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5dsg ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==

OCA at 17:13, 10 May 2016

OCA — Tue, 10 May 2016 17:13:20 GMT

←Older revision		Revision as of 17:13, 10 May 2016
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5dsg is ~~ON HOLD until Paper~~ Publication	+	==Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium==
		+	<StructureSection load='5dsg' size='340' side='right' caption='[[5dsg]], [[Resolution\|resolution]] 2.60Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5dsg]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DSG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DSG FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0HK:(1R,2R,4S,5S,7S)-7-{[HYDROXY(DITHIOPHEN-2-YL)ACETYL]OXY}-9,9-DIMETHYL-3-OXA-9-AZONIATRICYCLO[3.3.1.0~2,4~]NONANE'>0HK</scene>, <scene name='pdbligand=EDT:{[-(BIS-CARBOXYMETHYL-AMINO)-ETHYL]-CARBOXYMETHYL-AMINO}-ACETIC+ACID'>EDT</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=P6G:HEXAETHYLENE+GLYCOL'>P6G</scene>, <scene name='pdbligand=PG6:1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE'>PG6</scene></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=5dsg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dsg OCA], [http://pdbe.org/5dsg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5dsg RCSB], [http://www.ebi.ac.uk/pdbsum/5dsg PDBsum]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/ACM4_HUMAN ACM4_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 inhibition of adenylate cyclase.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Muscarinic M1-M5 acetylcholine receptors are G-protein-coupled receptors that regulate many vital functions of the central and peripheral nervous systems. In particular, the M1 and M4 receptor subtypes have emerged as attractive drug targets for treatments of neurological disorders, such as Alzheimer's disease and schizophrenia, but the high conservation of the acetylcholine-binding pocket has spurred current research into targeting allosteric sites on these receptors. Here we report the crystal structures of the M1 and M4 muscarinic receptors bound to the inverse agonist, tiotropium. Comparison of these structures with each other, as well as with the previously reported M2 and M3 receptor structures, reveals differences in the orthosteric and allosteric binding sites that contribute to a role in drug selectivity at this important receptor family. We also report identification of a cluster of residues that form a network linking the orthosteric and allosteric sites of the M4 receptor, which provides new insight into how allosteric modulation may be transmitted between the two spatially distinct domains.

-	~~Authors:~~ Thal, D~~.M.~~, ~~Kobilka~~, B.K., ~~Sexton~~, P~~.M.~~, ~~Christopoulos~~, A.	+	Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.,Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A Nature. 2016 Mar 17;531(7594):335-40. doi: 10.1038/nature17188. Epub 2016 Mar 9. PMID:26958838<ref>PMID:26958838</ref>

-	~~Description: Structure~~ of the ~~M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[Category: Unreleased Structures]]~~	+	</div>
-	~~[[Category~~: ~~Sexton, P.M]]~~	+	<div class="pdbe-citations 5dsg" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
	[[Category: Christopoulos, A]]		[[Category: Christopoulos, A]]
-	[[Category: Thal, D.M]]	+	[[Category: Kobilka, B K]]
-	[[Category: ~~Kobilka, B.K~~]]	+	[[Category: Sexton, P M]]
		+	[[Category: Thal, D M]]
		+	[[Category: Antagonist]]
		+	[[Category: Gpcr]]
		+	[[Category: Membrane]]
		+	[[Category: Membrane protein]]
		+	[[Category: Signaling]]

OCA at 11:23, 16 December 2015

OCA — Wed, 16 Dec 2015 11:23:02 GMT

←Older revision		Revision as of 11:23, 16 December 2015
Line 7:		Line 7:
	Description: Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium		Description: Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
-	[[Category: Thal, D.M]]
	[[Category: Sexton, P.M]]		[[Category: Sexton, P.M]]
	[[Category: Christopoulos, A]]		[[Category: Christopoulos, A]]
		+	[[Category: Thal, D.M]]
	[[Category: Kobilka, B.K]]		[[Category: Kobilka, B.K]]

OCA: Protected "5dsg" [edit=sysop:move=sysop]

OCA — Wed, 30 Sep 2015 13:27:52 GMT

Protected "5dsg" [edit=sysop:move=sysop]

←Older revision

Revision as of 13:27, 30 September 2015

OCA: New page: '''Unreleased structure''' The entry 5dsg is ON HOLD until Paper Publication Authors: Thal, D.M., Kobilka, B.K., Sexton, P.M., Christopoulos, A. Description: Structure of the M4 muscar...

OCA — Wed, 30 Sep 2015 13:27:51 GMT

New page: '''Unreleased structure''' The entry 5dsg is ON HOLD until Paper Publication Authors: Thal, D.M., Kobilka, B.K., Sexton, P.M., Christopoulos, A. Description: Structure of the M4 muscar...

New page

'''Unreleased structure'''

The entry 5dsg is ON HOLD until Paper Publication

Authors: Thal, D.M., Kobilka, B.K., Sexton, P.M., Christopoulos, A.

Description: Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium
[[Category: Unreleased Structures]]
[[Category: Thal, D.M]]
[[Category: Sexton, P.M]]
[[Category: Christopoulos, A]]
[[Category: Kobilka, B.K]]