Molecular cloning and characterization of the human voltage-gated calcium channel alpha(2)delta-4 subunit

Mol Pharmacol. 2002 Sep;62(3):485-96. doi: 10.1124/mol.62.3.485.

Abstract

The voltage-gated calcium channel is composed of a pore-forming alpha(1) subunit and several regulatory subunits: alpha(2)delta, beta, and gamma. We report here the identification of a novel alpha(2)delta subunit, alpha(2)delta-4, from the expressed sequence tag database followed by its cloning and characterization. The novel alpha(2)delta-4 subunit gene contains 39 exons spanning about 130 kilobases and is co-localized with the CHCNA1C gene (alpha(1C) subunit) on human chromosome 12p13.3. Alternative splicing of the alpha(2)delta-4 gene gives rise to four potential variants, a through d. The open reading frame of human alpha(2)delta-4a is composed of 3363 base pairs encoding a protein with 1120 residues and a calculated molecular mass of 126 kDa. The alpha(2)delta-4a subunit shares 30, 32, and 61% identity with the human calcium channel alpha(2)delta-1, alpha(2)delta-2, and alpha(2)delta-3 subunits, respectively. Primary sequence comparison suggests that alpha(2)delta-4 lacks the gabapentin binding motifs characterized for alpha(2)delta-1 and alpha(2)delta-2; this was confirmed by a [(3)H]gabapentin-binding assay. In human embryonic kidney 293 cells, the alpha(2)delta-4 subunit associated with Ca(V)1.2 and beta(3) subunits and significantly increased Ca(V)1.2/beta(3)-mediated Ca(2+) influx. Immunohistochemical study revealed that the alpha(2)delta-4 subunit has limited distribution in special cell types of the pituitary, adrenal gland, colon, and fetal liver. Whether the alpha(2)delta-4 subunit plays a distinct physiological role in select endocrine tissues remains to be demonstrated.

MeSH terms

  • Acetates / pharmacology
  • Alternative Splicing
  • Amines*
  • Amino Acid Sequence
  • Base Sequence
  • Biological Transport
  • Blotting, Northern
  • Calcium / metabolism*
  • Calcium Channel Blockers / pharmacology
  • Calcium Channels / genetics*
  • Calcium Channels / metabolism
  • Calcium Channels, L-Type / metabolism
  • Cells, Cultured
  • Chromosome Mapping
  • Chromosomes, Human, Pair 12*
  • Cloning, Molecular
  • Cyclohexanecarboxylic Acids*
  • Exons
  • Gabapentin
  • Humans
  • Immunohistochemistry
  • Molecular Sequence Data
  • Protein Subunits
  • Sequence Homology, Amino Acid
  • Tissue Distribution
  • gamma-Aminobutyric Acid*

Substances

  • Acetates
  • Amines
  • CACNA2D4 protein, human
  • Calcium Channel Blockers
  • Calcium Channels
  • Calcium Channels, L-Type
  • Cyclohexanecarboxylic Acids
  • L-type calcium channel alpha(1C)
  • Protein Subunits
  • gamma-Aminobutyric Acid
  • Gabapentin
  • Calcium