Venom peptides as a rich source of Cav2.2 channel blockers
In: Toxins. Multidisciplinary Digital Publishing Institute (MDPI): Basel. e-ISSN 2072-6651, meer
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| Author keywords |
Cav2.2; voltage-gated calcium channels; nociception; neurotransmitter; ?-conotoxins; venom peptides |
| Auteurs | | Top |
- Sousa, S.
- Vetter, I., meer
- Lewis, R.
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| Abstract |
Cav2.2 is a calcium channel subtype localized at nerve terminals, including nociceptive fibers, where it initiates neurotransmitter release. Cav2.2 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 Cav2.2 are analgesic. Venomous animals, such as cone snails, spiders, snakes, assassin bugs, centipedes and scorpions are rich sources of remarkably potent and selective Cav2.2 inhibitors. However, side effects in humans currently limit their clinical use. Here we review Cav2.2 inhibitors from venoms and their potential as drug leads. |
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