3fev - Revision history

OCA at 09:07, 30 October 2024

2024-10-30T09:07:48Z

← Older revision		Revision as of 09:07, 30 October 2024
Line 9:		Line 9:
	</table>		</table>
	== Function ==		== Function ==
	[https://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> [https://www.uniprot.org/uniprot/3SIM1_DENAN 3SIM1_DENAN] Shows a non-competitive interaction with adrenergic and muscarinic receptors. Binds to alpha-2b (ADRA2B) (IC(50)=2.3 nM), alpha-1a (ADRA1A), alpha-1b (ADRA1B), and alpha-2c (ADRA2C) adrenergic receptors. Reversibly binds to M1 (CHRM1) muscarinic acetylcholine receptors, probably by interacting with the orthosteric site (PubMed:~~7778123~~, PubMed:~~12488533~~, PubMed:~~24793485~~). Also reveals a slightly weaker effect at M3 (CHRM3) and M4 (CHRM4) receptors (PubMed:~~7778123~~, PubMed:~~12488533~~, PubMed:~~24793485~~). The order of potency is ADRA2B>>CHRM1>ADRA1A>ADRA1B>ADRA2C/CHRM4 (PubMed:24793485).<ref>PMID:12488533</ref> <ref>PMID:21557730</ref> <ref>PMID:24793485</ref> <ref>PMID:7778123</ref>		[https://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> [https://www.uniprot.org/uniprot/3SIM1_DENAN 3SIM1_DENAN] Shows a non-competitive interaction with adrenergic and muscarinic receptors. Binds to alpha-2b (ADRA2B) (IC(50)=2.3 nM), alpha-1a (ADRA1A), alpha-1b (ADRA1B), and alpha-2c (ADRA2C) adrenergic receptors. Reversibly binds to M1 (CHRM1) muscarinic acetylcholine receptors, probably by interacting with the orthosteric site (PubMed:12488533, PubMed:24793485, PubMed:7778123). Also reveals a slightly weaker effect at M3 (CHRM3) and M4 (CHRM4) receptors (PubMed:12488533, PubMed:24793485, PubMed:7778123). The order of potency is ADRA2B>>CHRM1>ADRA1A>ADRA1B>ADRA2C/CHRM4 (PubMed:24793485).<ref>PMID:12488533</ref> <ref>PMID:21557730</ref> <ref>PMID:24793485</ref> <ref>PMID:7778123</ref>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 15:		Line 15:
	<jmolCheckbox>		<jmolCheckbox>
	<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fe/3fev_consurf.spt"</scriptWhenChecked>		<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fe/3fev_consurf.spt"</scriptWhenChecked>
	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/~~initialview01~~.spt</scriptWhenUnchecked>		<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>
	</jmolCheckbox>		</jmolCheckbox>

OCA at 15:29, 1 November 2023

2023-11-01T15:29:14Z

← Older revision		Revision as of 15:29, 1 November 2023
Line 3:		Line 3:
	<StructureSection load='3fev' size='340' side='right'caption='[[3fev]], [[Resolution\|resolution]] 1.30Å' scene=''>		<StructureSection load='3fev' size='340' side='right'caption='[[3fev]], [[Resolution\|resolution]] 1.30Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3fev]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3FEV FirstGlance]. <br>		<table><tr><td colspan='2'>[[3fev]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Dendroaspis_angusticeps Dendroaspis angusticeps]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3FEV FirstGlance]. <br>
	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=SO4:SULFATE+ION'>SO4</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]] 1.3Å</td></tr>
	<tr id='~~related~~'><td class="sblockLbl"><b>[[~~Related_structure~~\|~~Related~~:]]</b></td><td class="sblockDat"><~~div style~~='~~overflow~~: ~~auto; max-height: 3em;~~'>~~[[2vlw\|2vlw]]~~</~~div~~></td></tr>		<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [https://pdbe.org/3fev PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [https://www.ebi.ac.uk/pdbsum/3fev PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3fev 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=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [https://pdbe.org/3fev PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [https://www.ebi.ac.uk/pdbsum/3fev PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3fev ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[https://www.uniprot.org/uniprot/~~TXM1_DENAN TXM1_DENAN]~~] Binds ~~irreversibly~~ to M1 (CHRM1) muscarinic acetylcholine receptors, ~~and~~ reveals a slightly weaker effect at M3 (CHRM3) ~~receptor~~.		[https://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> [https://www.uniprot.org/uniprot/3SIM1_DENAN 3SIM1_DENAN] Shows a non-competitive interaction with adrenergic and muscarinic receptors. Binds to alpha-2b (ADRA2B) (IC(50)=2.3 nM), alpha-1a (ADRA1A), alpha-1b (ADRA1B), and alpha-2c (ADRA2C) adrenergic receptors. Reversibly binds to M1 (CHRM1) muscarinic acetylcholine receptors, probably by interacting with the orthosteric site (PubMed:7778123, PubMed:12488533, PubMed:24793485). Also reveals a slightly weaker effect at M3 (CHRM3) and M4 (CHRM4) receptors (PubMed:7778123, PubMed:12488533, PubMed:24793485). The order of potency is ADRA2B>>CHRM1>ADRA1A>ADRA1B>ADRA2C/CHRM4 (PubMed:24793485).<ref>PMID:12488533</ref> <ref>PMID:21557730</ref> <ref>PMID:24793485</ref> <ref>PMID:7778123</ref>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 33:		Line 33:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
			[[Category: Dendroaspis angusticeps]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Fruchart-Gaillard, C]]		[[Category: Fruchart-Gaillard C]]
	[[Category: Menez, A]]		[[Category: Menez A]]
	[[Category: Menez, R]]		[[Category: Menez R]]
	[[Category: Mourier, G]]		[[Category: Mourier G]]
	[[Category: Servant, D]]		[[Category: Servant D]]
	[[Category: Stura~~, E A]]~~		[[Category: Stura EA]]
	~~[[Category: Acetylcholine receptor inhibitor]]~~
	~~[[Category: Chimera]]~~
	~~[[Category: Green mamba snake toxin]]~~
	~~[[Category: Hm1 muscarinic receptor]]~~
	~~[[Category: Muscarinic toxin]]~~
	~~[[Category: Neurotoxin]]~~
	~~[[Category: Postsynaptic neurotoxin]]~~
	~~[[Category: Secreted]]~~
	~~[[Category: Toxin~~]]

OCA at 07:59, 2 March 2022

2022-03-02T07:59:39Z

← Older revision		Revision as of 07:59, 2 March 2022
Line 3:		Line 3:
	<StructureSection load='3fev' size='340' side='right'caption='[[3fev]], [[Resolution\|resolution]] 1.30Å' scene=''>		<StructureSection load='3fev' size='340' side='right'caption='[[3fev]], [[Resolution\|resolution]] 1.30Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3fev]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3FEV FirstGlance]. <br>		<table><tr><td colspan='2'>[[3fev]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3FEV FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2vlw\|2vlw]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[2vlw\|2vlw]]</div></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=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [~~http~~://pdbe.org/3fev PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3fev PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3fev 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=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [https://pdbe.org/3fev PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [https://www.ebi.ac.uk/pdbsum/3fev PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3fev ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[~~http~~://www.uniprot.org/uniprot/TXM1_DENAN TXM1_DENAN]] Binds irreversibly to M1 (CHRM1) muscarinic acetylcholine receptors, and reveals a slightly weaker effect at M3 (CHRM3) receptor.		[[https://www.uniprot.org/uniprot/TXM1_DENAN TXM1_DENAN]] Binds irreversibly to M1 (CHRM1) muscarinic acetylcholine receptors, and reveals a slightly weaker effect at M3 (CHRM3) receptor.
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]

OCA at 14:58, 10 May 2019

2019-05-10T14:58:58Z

← Older revision		Revision as of 14:58, 10 May 2019
Line 1:		Line 1:

	==Crystal structure of the chimeric muscarinic toxin MT7 with loop 1 from MT1.==		==Crystal structure of the chimeric muscarinic toxin MT7 with loop 1 from MT1.==
	<StructureSection load='3fev' size='340' side='right' caption='[[3fev]], [[Resolution\|resolution]] 1.30Å' scene=''>		<StructureSection load='3fev' size='340' side='right'caption='[[3fev]], [[Resolution\|resolution]] 1.30Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3fev]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3FEV FirstGlance]. <br>		<table><tr><td colspan='2'>[[3fev]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3FEV FirstGlance]. <br>
Line 14:		Line 14:
	Check<jmol>		Check<jmol>
	<jmolCheckbox>		<jmolCheckbox>
	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fe/3fev_consurf.spt"</scriptWhenChecked>		<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fe/3fev_consurf.spt"</scriptWhenChecked>
	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>		<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>
Line 33:		Line 33:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
			[[Category: Large Structures]]
	[[Category: Fruchart-Gaillard, C]]		[[Category: Fruchart-Gaillard, C]]
	[[Category: Menez, A]]		[[Category: Menez, A]]

OCA at 09:45, 3 August 2017

2017-08-03T09:45:16Z

← Older revision		Revision as of 09:45, 3 August 2017
Line 1:		Line 1:

	==Crystal structure of the chimeric muscarinic toxin MT7 with loop 1 from MT1.==		==Crystal structure of the chimeric muscarinic toxin MT7 with loop 1 from MT1.==
	<StructureSection load='3fev' size='340' side='right' caption='[[3fev]], [[Resolution\|resolution]] 1.30Å' scene=''>		<StructureSection load='3fev' size='340' side='right' caption='[[3fev]], [[Resolution\|resolution]] 1.30Å' scene=''>
Line 5:		Line 6:
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2vlw\|2vlw]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2vlw\|2vlw]]</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=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [http://pdbe.org/3fev PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [http://www.ebi.ac.uk/pdbsum/3fev 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=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [http://pdbe.org/3fev PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [http://www.ebi.ac.uk/pdbsum/3fev PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3fev ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==

OCA at 23:37, 7 February 2016

2016-02-07T23:37:46Z

← Older revision		Revision as of 23:37, 7 February 2016
Line 5:		Line 5:
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2vlw\|2vlw]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2vlw\|2vlw]]</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=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [http://www.ebi.ac.uk/pdbsum/3fev 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=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [http://pdbe.org/3fev PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [http://www.ebi.ac.uk/pdbsum/3fev PDBsum]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 17:		Line 17:
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>
	</jmolCheckbox>		</jmolCheckbox>
	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/~~chain_selection~~.php?pdb_ID=~~2ata~~ ConSurf].		</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3fev ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
Line 27:		Line 27:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
			<div class="pdbe-citations 3fev" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 19:00, 24 December 2014

2014-12-24T19:00:17Z

← Older revision		Revision as of 19:00, 24 December 2014
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3fev]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3FEV FirstGlance]. <br>		<table><tr><td colspan='2'>[[3fev]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3FEV FirstGlance]. <br>
	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene><br>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2vlw\|2vlw]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2vlw\|2vlw]]</td></tr>
	<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [http://www.ebi.ac.uk/pdbsum/3fev 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=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [http://www.ebi.ac.uk/pdbsum/3fev PDBsum]</span></td></tr>
	<table>		</table>
			== Function ==
			[[http://www.uniprot.org/uniprot/TXM1_DENAN TXM1_DENAN]] Binds irreversibly to M1 (CHRM1) muscarinic acetylcholine receptors, and reveals a slightly weaker effect at M3 (CHRM3) receptor.
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 23:		Line 25:
	Engineering of three-finger fold toxins creates ligands with original pharmacological profiles for muscarinic and adrenergic receptors.,Fruchart-Gaillard C, Mourier G, Blanchet G, Vera L, Gilles N, Menez R, Marcon E, Stura EA, Servent D PLoS One. 2012;7(6):e39166. Epub 2012 Jun 14. PMID:22720062<ref>PMID:22720062</ref>		Engineering of three-finger fold toxins creates ligands with original pharmacological profiles for muscarinic and adrenergic receptors.,Fruchart-Gaillard C, Mourier G, Blanchet G, Vera L, Gilles N, Menez R, Marcon E, Stura EA, Servent D PLoS One. 2012;7(6):e39166. Epub 2012 Jun 14. PMID:22720062<ref>PMID:22720062</ref>

	From ~~MEDLINEÂ®~~/~~PubMedÂ®~~, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
	== References ==		== References ==
Line 29:		Line 31:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Fruchart-Gaillard, C.]]		[[Category: Fruchart-Gaillard, C]]
	[[Category: Menez, A.]]		[[Category: Menez, A]]
	[[Category: Menez, R.]]		[[Category: Menez, R]]
	[[Category: Mourier, G.]]		[[Category: Mourier, G]]
	[[Category: Servant, D.]]		[[Category: Servant, D]]
	[[Category: Stura, E A.]]		[[Category: Stura, E A]]
	[[Category: Acetylcholine receptor inhibitor]]		[[Category: Acetylcholine receptor inhibitor]]
	[[Category: Chimera]]		[[Category: Chimera]]

OCA at 09:47, 21 May 2014

2014-05-21T09:47:29Z

← Older revision		Revision as of 09:47, 21 May 2014
Line 1:		Line 1:
	[[Image:~~3fev~~.~~png~~\|~~left~~\|~~200px~~]]		==Crystal structure of the chimeric muscarinic toxin MT7 with loop 1 from MT1.==
			<StructureSection load='3fev' size='340' side='right' caption='[[3fev]], [[Resolution\|resolution]] 1.30Å' scene=''>
			== Structural highlights ==
			<table><tr><td colspan='2'>[[3fev]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3FEV FirstGlance]. <br>
			</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene><br>
			<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2vlw\|2vlw]]</td></tr>
			<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3fev FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3fev OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3fev RCSB], [http://www.ebi.ac.uk/pdbsum/3fev PDBsum]</span></td></tr>
			<table>
			== Evolutionary Conservation ==
			[[Image:Consurf_key_small.gif\|200px\|right]]
			Check<jmol>
			<jmolCheckbox>
			<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fe/3fev_consurf.spt"</scriptWhenChecked>
			<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
			<text>to colour the structure by Evolutionary Conservation</text>
			</jmolCheckbox>
			</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf].
			<div style="clear:both"></div>
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			Protein engineering approaches are often a combination of rational design and directed evolution using display technologies. Here, we test "loop grafting," a rational design method, on three-finger fold proteins. These small reticulated proteins have exceptional affinity and specificity for their diverse molecular targets, display protease-resistance, and are highly stable and poorly immunogenic. The wealth of structural knowledge makes them good candidates for protein engineering of new functionality. Our goal is to enhance the efficacy of these mini-proteins by modifying their pharmacological properties in order to extend their use in imaging, diagnostics and therapeutic applications. Using the interaction of three-finger fold toxins with muscarinic and adrenergic receptors as a model, chimeric toxins have been engineered by substituting loops on toxin MT7 by those from toxin MT1. The pharmacological impact of these grafts was examined using binding experiments on muscarinic receptors M1 and M4 and on the alpha(1A)-adrenoceptor. Some of the designed chimeric proteins have impressive gain of function on certain receptor subtypes achieving an original selectivity profile with high affinity for muscarinic receptor M1 and alpha(1A)-adrenoceptor. Structure-function analysis supported by crystallographic data for MT1 and two chimeras permits a molecular based interpretation of these gains and details the merits of this protein engineering technique. The results obtained shed light on how loop permutation can be used to design new three-finger proteins with original pharmacological profiles.

	~~{{STRUCTURE_3fev\| PDB=3fev \| SCENE= }}~~		Engineering of three-finger fold toxins creates ligands with original pharmacological profiles for muscarinic and adrenergic receptors.,Fruchart-Gaillard C, Mourier G, Blanchet G, Vera L, Gilles N, Menez R, Marcon E, Stura EA, Servent D PLoS One. 2012;7(6):e39166. Epub 2012 Jun 14. PMID:22720062<ref>PMID:22720062</ref>

	~~===Crystal structure~~ of the ~~chimeric muscarinic toxin MT7 with loop 1 from MT1~~.~~===~~		From MEDLINEÂ®/PubMedÂ®, a database of the U.S. National Library of Medicine.<br>
			</div>
	~~{{ABSTRACT_PUBMED_22720062}}~~		== References ==
			<references/>
	~~==About this Structure==~~		__TOC__
	~~[[3fev]] is a 3 chain structure~~. ~~Full crystallographic information is available from [http://oca~~.~~weizmann.ac.il~~/~~oca-bin/ocashort?id=3FEV OCA].~~		</StructureSection>

	==~~Reference~~==
	<~~ref group="xtra">PMID:022720062<~~/~~ref~~><~~references group="xtra"~~/>
	[[Category: Fruchart-Gaillard, C.]]		[[Category: Fruchart-Gaillard, C.]]
	[[Category: Menez, A.]]		[[Category: Menez, A.]]

OCA: Protected "3fev" [edit=sysop:move=sysop]

2012-07-18T04:30:29Z

Protected "3fev" [edit=sysop:move=sysop]

← Older revision	Revision as of 04:30, 18 July 2012
(No difference)

OCA at 04:30, 18 July 2012

2012-07-18T04:30:28Z

← Older revision		Revision as of 04:30, 18 July 2012
Line 1:		Line 1:
	~~{{Seed}}~~		[[Image:3fev.png\|left\|200px]]
	[[Image:3fev.~~jpg~~\|left\|200px]]

	~~<!--~~
	~~The line below this paragraph, containing "STRUCTURE_3fev", creates the "Structure Box" on the page.~~
	~~You may change the PDB parameter (which sets the PDB file loaded into the applet)~~
	~~or the SCENE parameter (which sets the initial scene displayed when the page is loaded),~~
	~~or leave the SCENE parameter empty for the default display.~~
	~~-->~~
	{{STRUCTURE_3fev\| PDB=3fev \| SCENE= }}		{{STRUCTURE_3fev\| PDB=3fev \| SCENE= }}

	===Crystal structure of the chimeric muscarinic toxin MT7 with loop 1 from MT1.===		===Crystal structure of the chimeric muscarinic toxin MT7 with loop 1 from MT1.===

			{{ABSTRACT_PUBMED_22720062}}

	==About this Structure==		==About this Structure==
	~~3FEV~~ is a 3 ~~chains~~ structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA].		[[3fev]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3FEV OCA].

			==Reference==
			<ref group="xtra">PMID:022720062</ref><references group="xtra"/>
	[[Category: Fruchart-Gaillard, C.]]		[[Category: Fruchart-Gaillard, C.]]
	[[Category: Menez, A.]]		[[Category: Menez, A.]]
Line 30:		Line 27:
	[[Category: Secreted]]		[[Category: Secreted]]
	[[Category: Toxin]]		[[Category: Toxin]]

	~~''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Dec 23 10:06:29 2009''~~