3neq: Difference between revisions

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==Crystal structure of the chimeric muscarinic toxin MT7 with loop 3 from MT1==
==Crystal structure of the chimeric muscarinic toxin MT7 with loop 3 from MT1==
<StructureSection load='3neq' size='340' side='right' caption='[[3neq]], [[Resolution|resolution]] 1.25&Aring;' scene=''>
<StructureSection load='3neq' size='340' side='right'caption='[[3neq]], [[Resolution|resolution]] 1.25&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[3neq]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3NEQ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3NEQ FirstGlance]. <br>
<table><tr><td colspan='2'>[[3neq]] is a 2 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=3NEQ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3NEQ 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='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.25&#8491;</td></tr>
<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3fev|3fev]], [[2vlw|2vlw]], [[1ff4|1ff4]]</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><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3neq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3neq OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3neq RCSB], [http://www.ebi.ac.uk/pdbsum/3neq PDBsum]</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=3neq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3neq OCA], [https://pdbe.org/3neq PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3neq RCSB], [https://www.ebi.ac.uk/pdbsum/3neq PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3neq ProSAT]</span></td></tr>
<table>
</table>
== 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: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>  
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<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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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 MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
<div class="pdbe-citations 3neq" style="background-color:#fffaf0;"></div>
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Fruchart-Gaillard, C.]]
[[Category: Dendroaspis angusticeps]]
[[Category: Menez, A.]]
[[Category: Large Structures]]
[[Category: Menez, R.]]
[[Category: Fruchart-Gaillard C]]
[[Category: Mournier, G.]]
[[Category: Menez A]]
[[Category: Servent, D.]]
[[Category: Menez R]]
[[Category: Stura, E A.]]
[[Category: Mournier G]]
[[Category: Chimeric muscarinic toxin]]
[[Category: Servent D]]
[[Category: Green mamba]]
[[Category: Stura EA]]
[[Category: Hm1-muscarinic receptor]]
[[Category: Snake toxin]]
[[Category: Toxin]]

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