Voltage Gated Calcium Channel Related Drug Discovery Products
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
The Voltage-Gated Calcium Channel (VGCC) represents a diverse family of transmembrane proteins, orchestrating the influx of calcium ions contingent upon membrane depolarization. As critical regulators of calcium signaling, these channels underpin myriad physiological processes, including neurotransmitter release, muscle contraction, and the modulation of gene expression. Consequently, the VGCC family has garnered significant scientific attention, precipitating a concerted effort to delineate the nuances of their structure and function, as well as to scrutinize their potential as pharmacological targets for the mitigation of various pathological conditions.
To meet the needs of voltage gated calcium channel drug discovery, Creative Biolabs can provide a wide variety of related assays and products:
- Voltage Gated Calcium Channel Assays
- Ion Channel Cell Lines
- Ion Channel Membranes
- Membrane Protein Tools
Overview of Voltage Gated Calcium Channel
The Voltage-Gated Calcium Channel family is classified into distinct subtypes, namely the L-type (Cav1), P/Q-type (Cav2.1), N-type (Cav2.2), R-type (Cav2.3), and T-type (Cav3) channels, each exhibiting unique biophysical properties, tissue distribution, and responsiveness to pharmacological intervention. VGCCs are composed of a central, pore-forming α1-subunit, in conjunction with auxiliary α2δ, β, and γ subunits, which collectively modulate channel function, trafficking, and membrane localization. The α1-subunits are characterized by four homologous domains (DI-DIV), each encompassing six transmembrane segments (S1-S6), with the S4 segment serving as the voltage sensor, and the intervening loops between S5 and S6 defining the ion-selective pore. Upon membrane depolarization, VGCCs undergo a series of conformational transitions, transitioning from a closed to an open and subsequently an inactivated state, a process integral to the regulation of calcium signaling.
Voltage Gated Calcium Channel Drug Discovery
The VGCCs encompass an array of distinct subtypes, each exhibiting unique properties and tissue distribution patterns, thereby presenting a panoply of opportunities for targeted pharmacological intervention. Research in the realm of VGCC-targeted drug discovery has mainly focused on small molecule modulators, allosteric modulation, auxiliary subunits, and peptide-based therapeutics.
Small molecule modulators: Advances in medicinal chemistry have facilitated the generation of isoform-selective small molecules, which exhibit greater potency and reduced off-target liabilities compared to non-selective agents. These small molecules encompass agonists, antagonists, and allosteric modulators, targeting specific subtypes of VGCCs.
Peptide-based therapeutics: Peptide-based approaches offer a promising alternative to small molecule modulators. These peptides, derived from natural sources or rationally designed, can selectively target specific VGCC subtypes, providing greater specificity and reduced off-target effects.
Gene therapy: The advent of gene therapy has opened new avenues for VGCC-targeted interventions. By modulating the expression of specific VGCC subunits, this approach holds promise for the treatment of conditions where aberrant VGCC activity contributes to the pathophysiology.
Nanoparticle-mediated delivery: Nanoparticle-based drug delivery systems have garnered attention for their potential to enhance the bioavailability, stability, and tissue-specific targeting of VGCC modulators. By encapsulating small molecules or peptides within nanoparticles, these systems may overcome some of the limitations associated with conventional drug delivery.
