2lz5

From Proteopedia

(Difference between revisions)

Current revision

Solution structure of a Novel Alpha-Conotoxin TxIB

Structural highlights

2lz5 is a 1 chain structure with sequence from Conus textile. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	Solution NMR, 20 models
Ligands:
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

CA1B_CONTE Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This conotoxin is a subtype-specific blocker of alpha-6/alpha-3-beta-2-beta-3 (CHRNA6/CHRNA3-CHRNB2-CHRNB3) nAChRs nicotinic acetylcholine receptors (nAChRs) (IC(50)=28.4 nM).^[1] ^[2]

Publication Abstract from PubMed

Alpha6beta2 nicotinic acetylcholine receptors (nAChRs) expressed by dopaminergic neurons in the CNS are potential therapeutic targets for the treatment of several neuropsychiatric diseases, including nicotine addiction and Parkinson's disease. However, recent studies indicate that the alpha6 subunit can also associate with the beta4 subunit to form alpha6beta4 nAChRs that are difficult to pharmacologically distinguish from alpha6beta2, alpha3beta4 and alpha3beta2 subtypes. The current study characterized a novel 16 amino acid alpha-conotoxin (alpha-CTx) TxIB from Conus textile whose sequence is GCCSDPPCRNKHPDLC-amide as deduced from gene cloning. The peptide and an analog with an additional C-terminal glycine were chemically synthesized and tested on rat nAChRs heterologously expressed in Xenopus laevis oocytes. alpha-CTx TxIB blocked alpha6/alpha3beta2beta3 nAChR with an IC50 of 28 nM. In contrast, the peptide showed little or no block of other tested subtypes at concentrations up to 10 muM. The three-dimensional solution structure of alpha-CTx TxIB was determined using NMR spectroscopy. alpha-CTx TxIB represents a uniquely selective ligand for probing the structure and function of alpha6beta2 nAChRs.

Characterization of a Novel alpha-Conotoxin from Conus textile that Selectively Targets Alpha6/alpha3beta2betab3 Nicotinic Acetylcholine Receptors.,Luo S, Zhangsun D, Wu Y, Zhu X, Hu Y, McIntyre M, Christensen S, Akcan M, Craik DJ, McIntosh JM J Biol Chem. 2012 Nov 26. PMID:23184959^[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Luo S, Zhangsun D, Wu Y, Zhu X, Hu Y, McIntyre M, Christensen S, Akcan M, Craik DJ, McIntosh JM. Characterization of a Novel alpha-Conotoxin from Conus textile that Selectively Targets Alpha6/alpha3beta2betab3 Nicotinic Acetylcholine Receptors. J Biol Chem. 2012 Nov 26. PMID:23184959 doi:10.1074/jbc.M112.427898
↑ Li X, Wang S, Zhu X, Zhangsun D, Wu Y, Luo S. Effects of Cyclization on Activity and Stability of α-Conotoxin TxIB. Mar Drugs. 2020 Mar 29;18(4):180. PMID:32235388 doi:10.3390/md18040180
↑ Luo S, Zhangsun D, Wu Y, Zhu X, Hu Y, McIntyre M, Christensen S, Akcan M, Craik DJ, McIntosh JM. Characterization of a Novel alpha-Conotoxin from Conus textile that Selectively Targets Alpha6/alpha3beta2betab3 Nicotinic Acetylcholine Receptors. J Biol Chem. 2012 Nov 26. PMID:23184959 doi:10.1074/jbc.M112.427898

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2lz5"

@@ Line 1: / Line 1: @@
 ==Solution structure of a Novel Alpha-Conotoxin TxIB==
-<StructureSection load='2lz5' size='340' side='right'caption='[[2lz5]], [[NMR_Ensembles_of_Models | 20 NMR models]]' scene=''>
+<StructureSection load='2lz5' size='340' side='right'caption='[[2lz5]]' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[2lz5]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2LZ5 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=2LZ5 FirstGlance]. <br>
+<table><tr><td colspan='2'>[[2lz5]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Conus_textile Conus textile]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2LZ5 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2LZ5 FirstGlance]. <br>
-</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 20 models</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=2lz5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2lz5 OCA], [http://pdbe.org/2lz5 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2lz5 RCSB], [http://www.ebi.ac.uk/pdbsum/2lz5 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2lz5 ProSAT]</span></td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NH2:AMINO+GROUP'>NH2</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=2lz5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2lz5 OCA], [https://pdbe.org/2lz5 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2lz5 RCSB], [https://www.ebi.ac.uk/pdbsum/2lz5 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2lz5 ProSAT]</span></td></tr>
 </table>
+== Function ==
+[https://www.uniprot.org/uniprot/CA1B_CONTE CA1B_CONTE] Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This conotoxin is a subtype-specific blocker of alpha-6/alpha-3-beta-2-beta-3 (CHRNA6/CHRNA3-CHRNB2-CHRNB3) nAChRs nicotinic acetylcholine receptors (nAChRs) (IC(50)=28.4 nM).<ref>PMID:23184959</ref> <ref>PMID:32235388</ref>
 <div style="background-color:#fffaf0;">
 == Publication Abstract from PubMed ==
@@ Line 20: / Line 23: @@
 __TOC__
 </StructureSection>
+[[Category: Conus textile]]
 [[Category: Large Structures]]
-[[Category: Akcan, M]]
+[[Category: Akcan M]]
-[[Category: Christensen, S]]
+[[Category: Christensen S]]
-[[Category: Craik, D]]
+[[Category: Craik D]]
-[[Category: Hu, Y]]
+[[Category: Hu Y]]
-[[Category: Luo, S]]
+[[Category: Luo S]]
-[[Category: McIntosh, J]]
+[[Category: McIntosh J]]
-[[Category: McIntyre, M]]
+[[Category: McIntyre M]]
-[[Category: Wu, Y]]
+[[Category: Wu Y]]
-[[Category: Zhangsun, D]]
+[[Category: Zhangsun D]]
-[[Category: Zhu, X]]
+[[Category: Zhu X]]
-[[Category: Alpha-conotoxin]]
-[[Category: Alpha-helix]]
-[[Category: Amidated c-terminus]]
-[[Category: Disulfide bond]]
-[[Category: Toxin]]

2lz5

From Proteopedia

Current revision

Solution structure of a Novel Alpha-Conotoxin TxIB

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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