Calcicludine

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Calcicludine (CaC) is a protein toxin from the venom of the green mamba that inhibits high-voltage-activated calcium channels, especially L-type calcium channels.

Source

Calcicludine is a toxin in the venom of the green mamba (Dendroaspis angusticeps).

Chemistry

Calcicludine is a 60-amino acid polypeptide with six cysteines forming three disulfide bridges. Calcicludine structurally resembles dendrotoxin, but works differently, since even at high concentrations, calcicludine has no effect on dendrotoxin-sensitive potassium channels in chicken and rat neurons.[1]

Target

Calcicludine is a blocker of high-voltage-activated calcium channels (L-, N- and P-type channels). It has highest affinity to the L-type calcium channel (IC₅₀ = 88nM[2]). However, sensitivity of the drug on the channel depends on the species and the tissue. For example, the IC₅₀ for block of L-type calcium channels on a cerebellar granule cell is 0.2 nM, but the IC₅₀ of the block of rat peripheral DRG neuronal L-type channels is around 60-80 nM.[1]

Mode of Action

Calcicludine has a unique mode of action, which is still incompletely understood. It has been suggested to act by a partial pore block or an effect on channel gating.[2]

Toxicity

Calcicludine has been shown to work on rat cardiac cells and rat cerebellum granule cells.[1]

References

[1]: Calcicludine, A Venom Peptide of the Kunitz-Type Protease Inhibitor Family, is a Potent Blocker of High-Threshold Ca 2+ Channels with a High Affinity for L-Type Channels in Cerebellar Granule Neurons, Schweitz et al., 1994
[2]: Block of Voltage-dependent Calcium Channel by the Green Mamba Toxin Calcicludine, Stotz et al., 1999

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Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .