Voltage-dependent calcium channel subunit alpha-2/delta-1 is a
protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metab ...
that in humans is encoded by the ''CACNA2D1''
gene
In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. The molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protei ...
.
This gene encodes a member of the alpha-2/delta subunit family, a protein in the voltage-dependent calcium channel complex.
Calcium channels mediate the influx of calcium ions into the cell upon membrane depolarization and consist of a complex of alpha-1, alpha-2/delta, beta, and gamma subunits in a 1:1:1:1 ratio. Research on a highly similar protein in rabbit suggests the protein described in this record is cleaved into alpha-2 and delta subunits. Alternate transcriptional
splice variant
Alternative splicing, alternative RNA splicing, or differential splicing, is an alternative splicing process during gene expression that allows a single gene to produce different splice variants. For example, some exons of a gene may be included ...
s of this gene have been observed, but have not been thoroughly characterized.
In mammals, alpha-2/delta proteins exist in four subtypes coded by four separate but closely related genes, CACNA2D1,
CACNA2D2,
CACNA2D3 and
CACNA2D4.
Recently, alpha-2/delta1 proteins, in addition to calcium channels, have been found to interact directly with
N-methyl-D-aspartate type glutamate receptors (NMDAR),
AMPA type glutamate receptors (AMPAR) and the extracellular adhesion protein,
thrombospondin.
Gabapentinoids
Alpha-2/delta proteins are believed to be the molecular target of the
gabapentinoid
Gabapentinoids, also known as α2δ ligands, are a class of drugs that are chemically chemical derivative, derivatives of the inhibitory neurotransmitter gamma-Aminobutyric acid (GABA) (i.e., GABA analogues) which Voltage-dependent calcium cha ...
s
gabapentin
Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat neuropathic pain and also for partial seizures of epilepsy. It is a commonly used medication for the treatment of neuropath ...
and
pregabalin
Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, generalized anx ...
, which are used to treat
epilepsy
Epilepsy is a group of Non-communicable disease, non-communicable Neurological disorder, neurological disorders characterized by a tendency for recurrent, unprovoked Seizure, seizures. A seizure is a sudden burst of abnormal electrical activit ...
and
neuropathic pain
Neuropathic pain is pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuo ...
.
Only alpha-2/delta subtypes 1 and 2 (but not 3 and 4) are substrates for gabapentinoid drug binding.
See also
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Voltage-dependent calcium channel
Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ion channels found in the membrane of excitable cells (''e.g.'' muscle, glial cells, neurons) with a permeability t ...
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Gabapentinoid drugs
References
Further reading
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External links
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Ion channels
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