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Spider Venom Nav1.7 Inhibitors for Pain Relief

Spider Venom Nav1.7 Inhibitors for Pain Relief

Paperback

Chemistry

ISBN10: 6630131037
ISBN13: 9786630131031
Publisher: Scholars' Press
Published: Jul 1 2026
Pages: 156
Weight: 0.48
Height: 0.36 Width: 6.00 Depth: 9.00
Language: English
This book describes the discovery and engineering of spider venom peptides that selectively inhibit the Nav1.7 sodium channel, a validated target for chronic pain relief. It begins with the identification of two novel toxins, -TRTX-Ca1a and -TRTX-Ca2a, from the Thai zebra tarantula Cyriopagopus albostriatus. Both peptides show potent, dose-dependent analgesia in rodent pain models. The authors then demonstrate that inactive HNTX-I can be transformed into a potent Nav1.7 blocker by introducing conserved residues, creating a 36 nM inhibitor. Finally, through systematic alanine scanning and molecular docking of HNTX-III, they engineer the optimized variant H4, which achieves an IC₅₀ of 7 nM, >1400-fold selectivity over cardiac and muscle sodium channels, and superior analgesic efficacy compared to morphine in inflammatory and neuropathic pain models. The book illustrates a complete arc from natural venom prospecting to rational peptide engineering and preclinical validation for safer pain therapeutics.

Also from

Zhang, Yunxiao

Also in

Chemistry