2m3i

Characterization of a Novel Alpha4/6-Conotoxin TxIC from Conus textile that Potently Blocks alpha3beta4 Nicotinic Acetylcholine Receptors

spinqualitylabelsall models 2m3i Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2m3i is a 1 chain structure with sequence from Conus lividus. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: Solution NMR, 20 models Ligands: NH2 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function CA112_CONLI Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This toxin inhibits alpha-3-beta-4, alpha-6/alpha-3-beta-4, and alpha-2-beta-4 nAChRs.[UniProtKB:K8DWB5] Publication Abstract from PubMed The alpha3beta4 nAChRs are implicated in pain sensation in the PNS and addiction to nicotine in the CNS. We identified an alpha-4/6-conotoxin (CTx) TxID from Conus textile. The new toxin consists of 15 amino acid residues with two disulfide bonds. TxID was synthesized using solid phase methods, and the synthetic peptide was functionally tested on nAChRs heterologously expressed in Xenopus laevis oocytes. TxID blocked rat alpha3beta4 nAChRs with a 12.5 nM IC50, which places it among the most potent alpha3beta4 nAChR antagonists. TxID also blocked the closely related alpha6/alpha3beta4 with a 94 nM IC50 but showed little activity on other nAChR subtypes. NMR analysis showed that two major structural isomers exist in solution, one of which adopts a regular alpha-CTx fold but with different surface charge distribution to other 4/6 family members. alpha-CTx TxID is a novel tool with which to probe the structure and function of alpha3beta4 nAChRs. Characterization of a Novel alpha-Conotoxin TxID from Conus textile That Potently Blocks Rat alpha3beta4 Nicotinic Acetylcholine Receptors.,Luo S, Zhangsun D, Zhu X, Wu Y, Hu Y, Christensen S, Harvey PJ, Akcan M, Craik DJ, McIntosh JM J Med Chem. 2013 Nov 22. PMID:24200193 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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