a-conotoxin ImI, a novel peptide which selectively targets neuronal nAChRs.McIntosh, J MYoshikami, DJohnson, D SMahe, ENielsen, D BRivier, J EGray, W ROlivera, B M
α-Conotoxin ImI is a 12-amino acid peptide, found in the venom of the marine snail Conus imperialis . This conotoxin is a selective antagonist of α7 nicotinic acetylcholine receptors. To produce biologically active α-ImI, disulfide bonds must be formed between Cys2–Cys8 and Cys3–Cys12...
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A nicotinic acetylcholine receptor ligand of unique specificity, alpha-conotoxin ImI. We report the isolation, characterization, and total synthesis of a small peptide ligand for nicotinic acetylcholine receptors (nAChRs). It is highly activ... JM Mcintosh,D Yoshikami,E Mahe,... - 《Journal of ...
α-Conotoxin ImI incorporating stable cystathionine bridges maintains full potency and identical three-dimensional structure. J. Am. Chem. Soc. 133, 15866–15869 (2011). Article CAS Google Scholar Knerr, P. J. et al. Synthesis and activity of thioether-containing analogues of the complement ...
A positional scan synthetic combinatorial library was constructed based on the three residues of the n-loop of z-conotoxin ImI to give a total of 10,648 possible combinations that were screened for functional activity in an α<sub>7</sub> nAChR Fluo-4/Ca<sup>2+</sup> assay, allowing ...
α-Conotoxin ImI incorporating stable cystathionine bridges maintains full potency and identical three-dimensional structure. The two disulfide bonds of α-conotoxin ImI, a peptide antagonist of the α7 nicotinic acetylcholine receptor (nAChR), were systematically replaced with isosteric redox-stable cystath...
to reject those solutions that were not in at least rough accordance with the available biochemical and mutagenesis data for long-chain alpha neurotoxins, and in the case of α-conotoxin GI, the complex was compared to the X-ray structure of the AChBP with conotoxin IMI (PDB code:2C9T)....
Taken together, the three stacked molecules of VUF9432 occupy a large volume and bury a substantial surface area in AChBP (959.9±4.8 Å2) comparable with the area buried by conotoxins IMI20 (PDB:2C9T) and PnIA19 (PDB:2BR8) (1164 Å2 and 1468 Å2, respectively). However...
Taken together, the three stacked molecules of VUF9432 occupy a large volume and bury a substantial surface area in AChBP (959.9±4.8 Å2) comparable with the area buried by conotoxins IMI20 (PDB:2C9T) and PnIA19 (PDB:2BR8) (1164 Å2 and 1468 Å2, respectively). However, the ...