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Venom peptides as a rich source of cav2.2 channel blockers.

ABSTRACT: Ca(v)2.2 is a calcium channel subtype localized at nerve terminals, including nociceptive fibers, where it initiates neurotransmitter release. Ca(v)2.2 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 ?2?1 subunit. It is therefore not surprising that toxins that inhibit Ca(v)2.2 are analgesic. Venomous animals, such as cone snails, spiders, snakes, assassin bugs, centipedes and scorpions are rich sources of remarkably potent and selective Ca(v)2.2 inhibitors. However, side effects in humans currently limit their clinical use. Here we review Ca(v)2.2 inhibitors from venoms and their potential as drug leads.

SUBMITTER: Sousa SR

PROVIDER: S-EPMC3640536 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature

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Venom peptides as a rich source of cav2.2 channel blockers.

Sousa Silmara R SR Vetter Irina I Lewis Richard J RJ

Toxins 20130204 2

Ca(v)2.2 is a calcium channel subtype localized at nerve terminals, including nociceptive fibers, where it initiates neurotransmitter release. Ca(v)2.2 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(v)2.2 are analgesic. Venomous animals, such as cone snails, spiders, snakes, assassin bugs, centipedes and ...[more]

PMID: 23381143

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