Voltage-Gated Sodium Channel Inhibition by µ-Conotoxins.

ABSTRACT: µ-Conotoxins are small, potent pore-blocker inhibitors of voltage-gated sodium (Na_V) channels, which have been identified as pharmacological probes and putative leads for analgesic development. A limiting factor in their therapeutic development has been their promiscuity for different Na_V channel subtypes, which can lead to undesirable side-effects. This review will focus on four areas of µ-conotoxin research: (1) mapping the interactions of µ-conotoxins with different Na_V channel subtypes, (2) µ-conotoxin structure-activity relationship studies, (3) observed species selectivity of µ-conotoxins and (4) the effects of µ-conotoxin disulfide connectivity on activity. Our aim is to provide a clear overview of the current status of µ-conotoxin research.

SUBMITTER: McMahon KL 

PROVIDER: S-EPMC10819908 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature