6zfz - Revision history

OCA at 13:48, 24 January 2024

OCA — Wed, 24 Jan 2024 13:48:56 GMT

←Older revision		Revision as of 13:48, 24 January 2024
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	<StructureSection load='6zfz' size='340' side='right'caption='[[6zfz]], [[Resolution\|resolution]] 2.17Å' scene=''>		<StructureSection load='6zfz' size='340' side='right'caption='[[6zfz]], [[Resolution\|resolution]] 2.17Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6zfz]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6ZFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ZFZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6zfz]] 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=6ZFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ZFZ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EPE:4-(2-HYDROXYETHYL)-1-PIPERAZINE+ETHANESULFONIC+ACID'>EPE</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=PGE:TRIETHYLENE+GLYCOL'>PGE</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=QJT:1-[3-(4-butylpiperidin-1-yl)propyl]-3,4-dihydroquinolin-2-one'>QJT</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]] 2.17Å</td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </span></td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EPE:4-(2-HYDROXYETHYL)-1-PIPERAZINE+ETHANESULFONIC+ACID'>EPE</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=PGE:TRIETHYLENE+GLYCOL'>PGE</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=QJT:1-[3-(4-butylpiperidin-1-yl)propyl]-3,4-dihydroquinolin-2-one'>QJT</scene></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=6zfz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6zfz OCA], [https://pdbe.org/6zfz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6zfz RCSB], [https://www.ebi.ac.uk/pdbsum/6zfz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6zfz 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=6zfz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6zfz OCA], [https://pdbe.org/6zfz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6zfz RCSB], [https://www.ebi.ac.uk/pdbsum/6zfz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6zfz ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[https://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.	+	[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/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.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Escherichia virus T4]]
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	~~[[Category: Lysozyme]]~~	+	[[Category: Cooke RM]]
-	[[Category: Cooke~~, R M~~]]	+	[[Category: Rucktooa P]]
-	[[Category: Rucktooa, P]]	+
-	~~[[Category: Gpcr]]~~	+
-	~~[[Category: Membrane protein~~]]	+

OCA at 10:00, 8 December 2021

OCA — Wed, 08 Dec 2021 10:00:56 GMT

←Older revision		Revision as of 10:00, 8 December 2021
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	== Function ==		== Function ==
	[[https://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.		[[https://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.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Current therapies for Alzheimer's disease seek to correct for defective cholinergic transmission by preventing the breakdown of acetylcholine through inhibition of acetylcholinesterase, these however have limited clinical efficacy. An alternative approach is to directly activate cholinergic receptors responsible for learning and memory. The M1-muscarinic acetylcholine (M1) receptor is the target of choice but has been hampered by adverse effects. Here we aimed to design the drug properties needed for a well-tolerated M1-agonist with the potential to alleviate cognitive loss by taking a stepwise translational approach from atomic structure, cell/tissue-based assays, evaluation in preclinical species, clinical safety testing, and finally establishing activity in memory centers in humans. Through this approach, we rationally designed the optimal properties, including selectivity and partial agonism, into HTL9936-a potential candidate for the treatment of memory loss in Alzheimer's disease. More broadly, this demonstrates a strategy for targeting difficult GPCR targets from structure to clinic.
		+
		+	From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.,Brown AJH, Bradley SJ, Marshall FH, Brown GA, Bennett KA, Brown J, Cansfield JE, Cross DM, de Graaf C, Hudson BD, Dwomoh L, Dias JM, Errey JC, Hurrell E, Liptrot J, Mattedi G, Molloy C, Nathan PJ, Okrasa K, Osborne G, Patel JC, Pickworth M, Robertson N, Shahabi S, Bundgaard C, Phillips K, Broad LM, Goonawardena AV, Morairty SR, Browning M, Perini F, Dawson GR, Deakin JFW, Smith RT, Sexton PM, Warneck J, Vinson M, Tasker T, Tehan BG, Teobald B, Christopoulos A, Langmead CJ, Jazayeri A, Cooke RM, Rucktooa P, Congreve MS, Weir M, Tobin AB Cell. 2021 Nov 24;184(24):5886-5901.e22. doi: 10.1016/j.cell.2021.11.001. PMID:34822784<ref>PMID:34822784</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6zfz" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
	*[[Muscarinic acetylcholine receptor\|Muscarinic acetylcholine receptor]]		*[[Muscarinic acetylcholine receptor\|Muscarinic acetylcholine receptor]]
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>

OCA at 06:26, 1 December 2021

OCA — Wed, 01 Dec 2021 06:26:17 GMT

←Older revision		Revision as of 06:26, 1 December 2021
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	==Structure of M1-StaR-T4L in complex with 77-LH-28-1 at 2.17A==		==Structure of M1-StaR-T4L in complex with 77-LH-28-1 at 2.17A==
-	<StructureSection load='6zfz' size='340' side='right'caption='[[6zfz]]' scene=''>	+	<StructureSection load='6zfz' size='340' side='right'caption='[[6zfz]], [[Resolution\|resolution]] 2.17Å' 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=6ZFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ZFZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6zfz]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6ZFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ZFZ 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=6zfz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6zfz OCA], [https://pdbe.org/6zfz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6zfz RCSB], [https://www.ebi.ac.uk/pdbsum/6zfz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6zfz 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=EPE:4-(2-HYDROXYETHYL)-1-PIPERAZINE+ETHANESULFONIC+ACID'>EPE</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=PGE:TRIETHYLENE+GLYCOL'>PGE</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=QJT:1-[3-(4-butylpiperidin-1-yl)propyl]-3,4-dihydroquinolin-2-one'>QJT</scene></td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [https://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'>[https://proteopedia.org/fgij/fg.htm?mol=6zfz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6zfz OCA], [https://pdbe.org/6zfz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6zfz RCSB], [https://www.ebi.ac.uk/pdbsum/6zfz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6zfz ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[https://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.
		+
		+	==See Also==
		+	*[[Muscarinic acetylcholine receptor\|Muscarinic acetylcholine receptor]]
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Cooke RM]]	+	[[Category: Lysozyme]]
-	[[Category: Rucktooa P]]	+	[[Category: Cooke, R M]]
		+	[[Category: Rucktooa, P]]
		+	[[Category: Gpcr]]
		+	[[Category: Membrane protein]]

OCA at 05:26, 6 October 2021

OCA — Wed, 06 Oct 2021 05:26:41 GMT

←Older revision		Revision as of 05:26, 6 October 2021
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-	'''Unreleased structure'''

-	~~The entry~~ 6zfz ~~is ON HOLD until Paper Publication~~	+	==Structure of M1-StaR-T4L in complex with 77-LH-28-1 at 2.17A==
-		+	<StructureSection load='6zfz' size='340' side='right'caption='[[6zfz]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6ZFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ZFZ FirstGlance]. <br>
-	~~Description~~:	+	</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=6zfz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6zfz OCA], [https://pdbe.org/6zfz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6zfz RCSB], [https://www.ebi.ac.uk/pdbsum/6zfz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6zfz ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Cooke RM]]
		+	[[Category: Rucktooa P]]

OCA at 13:28, 17 June 2021

OCA — Thu, 17 Jun 2021 13:28:48 GMT

←Older revision		Revision as of 13:28, 17 June 2021
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6zfz is ON HOLD	+	The entry 6zfz is ON HOLD until Paper Publication

	Authors:		Authors:

OCA at 08:00, 12 May 2021

OCA — Wed, 12 May 2021 08:00:57 GMT

←Older revision		Revision as of 08:00, 12 May 2021
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6zfz is ON HOLD ~~until sometime in the future~~	+	The entry 6zfz is ON HOLD

	Authors:		Authors:

OCA: Protected "6zfz" [edit=sysop:move=sysop]

OCA — Wed, 24 Jun 2020 18:46:42 GMT

Protected "6zfz" [edit=sysop:move=sysop]

←Older revision

Revision as of 18:46, 24 June 2020

OCA: New page: '''Unreleased structure''' The entry 6zfz is ON HOLD until sometime in the future Authors: Description: Category: Unreleased Structures

OCA — Wed, 24 Jun 2020 18:46:41 GMT

New page: '''Unreleased structure''' The entry 6zfz is ON HOLD until sometime in the future Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 6zfz is ON HOLD until sometime in the future

Authors:

Description:
[[Category: Unreleased Structures]]