Venom Peptides as a Rich Source of Cav2.2 Channel Blockers

Toxins

Silmara R. Sousa¹  Irina Vetter¹ 

[1] Institute for Molecular Bioscience, The University of Queensland, St Lucia, Queensland, 4072, Australia;

关键词: Ca_v2.2;    voltage-gated calcium channels;    nociception;    neurotransmitter;    ω-conotoxins;    venom peptides;   

DOI  :  10.3390/toxins5020286

来源: mdpi

【 摘 要 】

Ca_v2.2 is a calcium channel subtype localized at nerve terminals, including nociceptive fibers, where it initiates neurotransmitter release. Ca_v2.2 is an important contributor to synaptic transmission in ascending pain pathways, and is up-regulated in the spinal cord in chronic pain states along with the auxiliary α2δ1 subunit. It is therefore not surprising that toxins that inhibit Ca_v2.2 are analgesic. Venomous animals, such as cone snails, spiders, snakes, assassin bugs, centipedes and scorpions are rich sources of remarkably potent and selective Ca_v2.2 inhibitors. However, side effects in humans currently limit their clinical use. Here we review Ca_v2.2 inhibitors from venoms and their potential as drug leads.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.