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Calcicludine

 

 
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Calcicludine
 
 
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Calcicludine (CaC) is a protein toxin
Toxin

A toxin is a poisonous substance produced by living cells or organisms. For a toxic substance not produced by living organisms, "toxicant" is the more appropriate term, and "toxics" is an acceptable plural....
 from the venom of the green mamba
Green mamba

Green mamba may refer to:* Eastern green mamba* Western green mamba...
 that inhibits high-voltage-activated calcium channels, especially L-type calcium channels.

icludine is a toxin in the venom of the green mamba
Green mamba

Green mamba may refer to:* Eastern green mamba* Western green mamba...
 (Dendroaspis angusticeps).

icludine is a 60-amino acid
Amino acid

In chemistry, an amino acid is a molecule containing both amine and carboxyl functional groups. These molecules are particularly important in biochemistry, where this term refers to alpha-amino acids with the general formula H2NCHRCOOH, where R is an organic substituent....
 polypeptide with six cysteines forming three disulfide bridges. Calcicludine structurally resembles dendrotoxin
Dendrotoxin

Dendrotoxins are a class of neurotoxins produced by mamba snakes that block particular subtypes of voltage-gated potassium channels in neurons, thereby enhancing the release of acetylcholine at neuromuscular junctions....
, but works differently, since even at high concentrations, calcicludine has no effect on dendrotoxin-sensitive potassium channels in chicken and rat neurons.

icludine is a blocker of high-voltage-activated calcium channels (L-, N- and P-type channels).






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Encyclopedia


Calcicludine (CaC) is a protein toxin
Toxin

A toxin is a poisonous substance produced by living cells or organisms. For a toxic substance not produced by living organisms, "toxicant" is the more appropriate term, and "toxics" is an acceptable plural....
 from the venom of the green mamba
Green mamba

Green mamba may refer to:* Eastern green mamba* Western 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
Green mamba

Green mamba may refer to:* Eastern green mamba* Western green mamba...
 (Dendroaspis angusticeps).

Chemistry

Calcicludine is a 60-amino acid
Amino acid

In chemistry, an amino acid is a molecule containing both amine and carboxyl functional groups. These molecules are particularly important in biochemistry, where this term refers to alpha-amino acids with the general formula H2NCHRCOOH, where R is an organic substituent....
 polypeptide with six cysteines forming three disulfide bridges. Calcicludine structurally resembles dendrotoxin
Dendrotoxin

Dendrotoxins are a class of neurotoxins produced by mamba snakes that block particular subtypes of voltage-gated potassium channels in neurons, thereby enhancing the release of acetylcholine at neuromuscular junctions....
, but works differently, since even at high concentrations, calcicludine has no effect on dendrotoxin-sensitive potassium channels in chicken and rat neurons.

Target

Calcicludine is a blocker of high-voltage-activated calcium channels (L-, N- and P-type channels). It has highest affinity
Affinity

Affinity, in etymology affinity is the opposite of infinity . These two words have the same root coming from the Latin: finis = end....
 to the L-type calcium channel (IC50
IC50

The half maximal inhibitory concentration is a measure of the effectiveness of a compound in inhibiting biological or biochemical function. Often, the compound in question is a drug candidate....
 = 88nM[2]). However, sensitivity
Sensitivity

Sensitivity may refer to:* Allergy* Sensitivity * Sensitivity * Sensitivity * Sensitivity and specificity are related concepts in statistics...
 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
Granule cell

In neuroscience, granule cells refer to tiny neurons that are around 10 micrometres in diameter. Granule cells are found within the Cerebellum#Granular_Layer of the cerebellum, layer 4 of cerebral cortex, the dentate gyrus of the hippocampus, and in the olfactory bulb....
 is 0.2 nM, but the IC50 of the block of rat peripheral DRG neuronal L-type channels is around 60-80 nM.

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.

Toxicity

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