Cav1.2 (L-type) Rat Calcium Ion Channel Binding (Dihydropyridine Site) LeadHunter Assay - TW

Background Information:

Voltage-gated calcium channels mediate calcium influx in response to membrane depolarization and regulate intracellular processes such as contraction, secretion, neurotransmission, and gene expression. They are members of a gene superfamily of transmembrane ion channel proteins that includes voltage-gated potassium and sodium channels. Pharmacology of the three families of calcium channels is quite distinct. Type L calcium channel blockers are used in the therapy of cardiovascular disease. Of these, phenylalkyamines are intracellular pore blockers, closely apposed to the dihydropyridine receptor and share some common amino acid residues. Dihydropyridines can be channel activators or inhibitors and, therefore, are thought to act allosterically to shift the channel toward the open or closed state, rather than by occluding the pore. Benzothiazepines are thought to bind to a third receptor site where the required amino acids for binding overlap extensively with those for phenylalkylamine binding.

Family:

Ion Channel

Sub Family:

Calcium

Class:

Voltage-Gated

Protein Name:

Cav1.2 (L-type)

Uniprot Number:

Q13936

Gene Name:

CACNA1C

Gene ID:

775

Gene Aliases:

Cav1.2|CACH2|CACN2|TS|LQT8

Organism:

Rat