Rationally Designed α-Conotoxin Analogues Maintained Analgesia Activity and Weakened Side Effects.

ABSTRACT: A lack of specificity is restricting the further application of conotoxin from Conus bullatus (BuIA). In this study, an analogue library of BuIA was established and virtual screening was used, which identified high α7 nicotinic acetylcholine receptor (nAChR)-selectivity analogues. The analogues were synthesized and tested for their affinity to functional human α7 nAChR and for the regulation of intracellular calcium ion capacity in neurons. Immunofluorescence, flow cytometry, and patch clamp results showed that the analogues maintained their capacity for calcium regulation. The results of the hot-plate model and paclitaxel-induced peripheral neuropathy model indicated that, when compared with natural BuIA, the analgesia activities of the analogues in different m

SUBMITTER: Liu C 

PROVIDER: S-EPMC6358911 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature