• CaV2.1

    Current–voltage relationships of CaV2.1: Patchliner compared to manual patch clamp.

    Hermann et al. (2013)

CaV2.1 | voltage-dependent, P type, alpha 1A subunit calcium channel

Family:
Calcium channels

Subgroups:
L-Type (CaV1.1–CaV1.4), P/Q-Type (CaV2.1), N-Type (CaV2.2), R-Type (CaV2.3), T-Type (CaV3.1–CaV3.3)

Topology:
Six transmembrane alpha helices (S1–S6), total of four homologous domains make up the tetrameric alpha subunit structure

Assembling:
One large alpha subunit forms a functional channel, accessory subunits ( α1, α2δ, β1-4, and γ) are crucial for robust expression, they functionally modulate the alpha subunit

CaV2.1: Background Information

CaV2.1, also known as brain calcium channel I, gives rise to P and/or Q-type calcium currents and is predominantly expressed in neuronal tissue. Localized to the presynaptic membrane of many types of neurons, CaV2.1 ion channels are involved in triggering neurotransmitter release via both, vesicle release and postsynaptic calcium entry.

Gene:
CACNA1A

Human Protein:
UniProt O00555

Tissue:
Brain

Function/ Application:
Pre-synaptic Ca2+ influx and neurotransmitter release in neurons, fast synaptic transmission

Pathology:
Migraine (FHM-1), ataxia (EA-2, SCA6), Benign paroxysmal torticollis of infancy, hemiplegia

Interaction:
β4 subunit CACNB4, α2δ subunits, calmodulin, CaBP1, VILIP, mint, CASK, Syntaxin, SNAP25

Modulator:
Kuratoxin, ω-agatoxin IIIA, ω-conotoxin MVIIC, ω-agatoxin-IVA, roscovitine

Assays:
Patch Clamp: whole cell, room temperature

Particularities:
CaV channels often show a rundown phenomenon. Adequate intra- and extrcellular solutions are essential for a good data quality.

Recommended Reviews:
Catterall WA, Perez-Reyes E, Snutch TP, Striessnig J (2005). "International Union of Pharmacology. XLVIII. Nomenclature and structure-function relationships of voltage-gated calcium channels". Pharmacol Rev. 57 (4): 411–25.

Publications

2013 - Establishment of a Secondary Screening Assay for P/Q-Type Calcium Channel Blockers

icon pl   Patchliner publication in Combinatorial Chemistry & High Throughput Screening (2013) 16(3):233-243

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