Trifunctional Saxitoxin Conjugates for Covalent Labeling of Voltage-Gated Sodium Channels.

ABSTRACT: Voltage-gated sodium ion channels (Na_V s) are integral membrane protein complexes responsible for electrical signal conduction in excitable cells. Methods that enable selective labeling of Na_V s hold potential value for understanding how channel regulation and post-translational modification are influenced during development and in response to diseases and disorders of the nervous system. We have developed chemical reagents patterned after (+)-saxitoxin (STX) - a potent and reversible inhibitor of multiple Na_V isoforms - and affixed with a reactive electrophile and either a biotin cofactor, fluorophore, or 'click' functional group for labeling wild-type channels. Our studies reveal enigmatic structural effects of the probes on the potency and efficiency of

SUBMITTER: Finkelstein DS 

PROVIDER: S-EPMC10863845 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature