ArticleThe EMBO journal1996
The IVS6 segment of the L-type calcium channel is critical for the action of dihydropyridines and phenylalkylamines.
Article in The EMBO journal, 1996. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 124 citations in OpenAlex.
- Inhibition of CaV1.4 channels by CaV3 channel antagonists ML218 and Z944.The Journal of general physiology · 2026Article
- Voltage gated sodium and calcium channels: Discovery, structure, function, and Pharmacology.Channels (Austin, Tex.) · 2023Review
- Modulation of L-type calcium channels in Alzheimer's disease: A potential therapeutic target.Computational and structural biotechnology journal · 2023Review
- Phenylalkylamines in calcium channels: computational analysis of experimental structures.Journal of computer-aided molecular design · 2020Article
- Elucidation of molecular kinetic schemes from macroscopic traces using system identification.PLoS computational biology · 2017Article
- Molecular simulations study of novel 1,4-dihydropyridines derivatives with a high selectivity for Cav3.1 calcium channel.Protein science : a publication of the Protein Society · 2015Article
- Structural Basis for Pharmacology of Voltage-Gated Sodium and Calcium Channels.Molecular pharmacology · 2015Review
- Bioelectric patterning during oogenesis: stage-specific distribution of membrane potentials, intracellular pH and ion-transport mechanisms in Drosophila ovarian follicles.BMC developmental biology · 2015Article
- Pharmacological Inhibition of Voltage-gated Ca(2+) Channels for Chronic Pain Relief.Current neuropharmacology · 2013Article
- Molecular determinants for activation of human ether-à-go-go-related gene 1 potassium channels by 3-nitro-n-(4-phenoxyphenyl) benzamide.Molecular pharmacology · 2011Article
- TTX, cations and spider venom modify avian muscle tone in vitro.Journal of venom research · 2011Article
- Structural model for phenylalkylamine binding to L-type calcium channels.The Journal of biological chemistry · 2009Article
- Engineering proteins for custom inhibition of Ca(V) channels.Physiology (Bethesda, Md.) · 2009Review
- Structural model for dihydropyridine binding to L-type calcium channels.The Journal of biological chemistry · 2009Article
- The organic cation transporter, OCTN1, expressed in the human heart, potentiates antagonism of the HERG potassium channel.Journal of cardiovascular pharmacology · 2009Article
- A genetic screen for dihydropyridine (DHP)-resistant worms reveals new residues required for DHP-blockage of mammalian calcium channels.PLoS genetics · 2008Article
- Calcicludine binding to the outer pore of L-type calcium channels is allosterically coupled to dihydropyridine binding.Biochemistry · 2007Article
- Maturation of rat cerebellar Purkinje cells reveals an atypical Ca2+ channel current that is inhibited by omega-agatoxin IVA and the dihydropyridine (-)-(S)-Bay K8644.The Journal of physiology · 2007Article
- The L-type calcium channel in the heart: the beat goes on.The Journal of clinical investigation · 2005Review
- Reverse engineering the L-type Ca2+ channel alpha1c subunit in adult cardiac myocytes using novel adenoviral vectors.Biochemical and biophysical research communications · 2005Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The current through the L-type calcium channel is inhibited and stimulated by distinct dihydropyridines at very low concentrations. The molecular determinants for the high affinity block and stimulation were investigated using chimeras between the class C and E calcium channels. Mutation of three amino acids in the last putative transmembrane segment (IVS6) of the alpha1C subunit decreased the affinity for (+)isradipine 100-fold without significantly affecting the basic properties of the expressed channel. Mutation of two of these three amino acids completely abolished the stimulatory effect of the calcium channel agonist Bay K 8644. These mutations only slightly affected the blocking efficacy of mibefradil and the phenylalkylamine devapamil. Three distinct but adjacently located amino acids mediated the high affinity block by devapamil. These results suggest that the IVS6 segment of the alpha1C subunit is critical for the high affinity interaction between the L-type calcium channel and the calcium channel agonist Bay K 8644 and the two antagonists isradipine and devapamil.
Indexed as
Identifiers
8665843PMC450166W209805056What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.