Cuny, Hartmut and Yu, Rilei and Tae, Han-Shen and Kompella, Shiva N and Adams, David J (2018) α-Conotoxins active at α3-containing nicotinic acetylcholine receptors and their molecular determinants for selective inhibition. British Journal of Pharmacology, 175. pp.1855-1868. ISSN 1476-5381 (OA)
Full text not available from this repository.Abstract
Neuronal α3-containing nicotinic acetylcholine receptors (nAChRs) in the peripheral nervous system (PNS) and non-neuronal tissues are implicated in a number of severe disease conditions ranging from cancer to cardiovascular diseases, and chronic pain. However, despite the physiological characterization of mouse models and cell lines, the precise pathophysiology of nAChRs outside the central nervous system (CNS) remains not well understood, in part because there is a lack of subtype-selective antagonists. α-Conotoxins isolated from cone snail venom exhibit characteristic individual selectivity profiles for nAChRs and, therefore, are excellent tools to study the determinants for nAChR-antagonist interactions. Given that human α3β4 subtype selective α-conotoxins are scarce and this is a major nAChR subtype in the PNS, the design of new peptides targeting this nAChR subtype is desirable. Recent studies using α-conotoxins RegIIA and AuIB, in combination with nAChR site-directed mutagenesis and computational modeling have shed light onto specific nAChR residues which determine selectivity for the human α3β2 and α3β4 subtypes. Recent publications describing other α-conotoxins confirm that subtype-selective nAChR antagonists often work through common mechanisms by interacting with the same structural components and sites on the receptor.
| Item Type: | Article |
|---|---|
| Subjects: | R Medicine > R Medicine (General) |
| Depositing User: | Repository Administrator |
| Date Deposited: | 11 May 2017 04:46 |
| Last Modified: | 20 Aug 2018 01:24 |
| URI: | https://eprints.victorchang.edu.au/id/eprint/588 |
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