Roscovitine, a cyclin‐dependent kinase inhibitor, affects several gating mechanisms to inhibit cardiac L‐type (Ca(V)1.2) calcium channels
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Background and purpose: L‐type calcium channels (Ca (V)1.2) play an important role in cardiac contraction. Roscovitine, a cyclin‐dependent kinase inhibitor and promising anticancer drug, has been shown to affect Ca (V)1.2 by inhibiting current amplitude and slowing activation. This research investigates the mechanism by which roscovitine inhibits Ca (V)1.2 channels. Experimental approach: Ca (V)1.2 channels were transfected into HEK 293 cells, using the calcium phosphate precipitation method, and currents were measured using the whole‐cell patch clamp technique. Key results: Roscovitine slows activation at all voltages, which precludes one previously proposed mechanism. In addition, roscovitine enhances voltage‐dependent, but not calcium‐dependent inactivation. This enhancement resulted from both an acceleration of inactivation and a slowing of the recovery from inactivation. Internally applied roscovitine failed to affect Ca (V)1.2 currents, which supports a kinase‐independent mechanism and extracellular binding site. Unlike the dihydropyridines, closed state inactivation was not affected by roscovitine. Inactivation was enhanced in a dose‐dependent manner with an IC 50=29.5±12 μ M, which is close to that for slow activation and inhibition. Conclusions and implications: We conclude that roscovitine binds to an extracellular site on Ca (V)1.2 channels to inhibit current by both slowing activation and enhancing inactivation. Purine‐based drugs could become a new option for treatment of diseases that benefit from L‐channel inhibition such as cardiac arrhythmias and hypertension. British Journal of Pharmacology (2007) 152, 386–395; doi:10.1038/sj.bjp.0707414; published online 13 August 2007
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This phenotype can be reversed by treatment with roscovitine, a cyclin-dependent kinase inhibitor and atypical L-type-channel blocker.
“This phenotype can be reversed by treatment with roscovitine, a cyclin-dependent kinase inhibitor and atypical L-type–channel blocker 2, 3, 4.”
From Using iPSC-derived neurons to uncover cellular phenotypes associated with Timothy syndrome (2011) · cites this paper as [3]
Earlier studies in cardiomyocytes from TS individuals indicated that roscovitine, a cyclin-dependent kinase blocker that also increases L-type channel inactivation, can reduce the prolongation of the cardiac AP in cells from TS individuals.
“Earlier studies in cardiomyocytes12 from TS individuals indicated that roscovitine2,3,29, a cyclin-dependent kinase blocker that also increases L-type channel inactivation, can reduce the prolongation of the cardiac AP in cells from TS individuals.”
From Using iPSC-derived neurons to uncover cellular phenotypes associated with Timothy syndrome (2011) · cites this paper as [3]
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Das, S. (2021) · Handbook of Oxidative Stress in Cancer: Therapeutic Aspects · doi:10.1007/978-981-16-1247-3_249-1 · Cited by 1 · see citing works
Therapeutic Efficacy of Roscovitine Against Cancer
Das, S. (2022) · Handbook of Oxidative Stress in Cancer: Therapeutic Aspects · doi:10.1007/978-981-16-5422-0_249
Ando, A., Kirkbride, R. C., Jones, D. C., Grimwood, J., & Chen, Z. J. (2021) · Figshare · doi:10.6084/m9.figshare.14516510
- Authors
- Yarotskyy, V, & Elmslie, K. S.
- Affiliations
- Pennsylvania State University (US)
- Corresponding author
- Elmslie, K S
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2007-10
- Volume
- 152
- Issue
- 3
- Pages
- 386-395
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- PMC
- PMC2042960
- OpenAlex
- W1510194880
- Cited by
- 49
- References
- 45
- Citations by year
- 2025: 1 · 2024: 1 · 2023: 1 · 2022: 4 · 2021: 5 · 2020: 1 · 2019: 3 · 2018: 3 · 2017: 3 · 2016: 1 · 2015: 1 · 2014: 1 · 2013: 4 · 2012: 3
- FWCI
- 1.46
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- British Journal of Pharmacology (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Health Sciences › Medicine › Cardiology and Cardiovascular Medicine › Cardiac electrophysiology and arrhythmias
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Keywords
- roscovitine, cyclin-dependent kinase inhibitors, L-type calcium channels, Cav1.2, channel gating, voltage-dependent inactivation, recovery from inactivation, extracellular binding site, cardiac arrhythmias, hypertension
- MeSH terms
- Roscovitine, Binding Sites, Calcium Phosphates, Cardiovascular Diseases, Cell Line, Electrophysiology, Humans, Chemical Precipitation, Purines, Transfection, Ion Channel Gating, Patch-Clamp Techniques, Cyclin-Dependent Kinases, Calcium Channels, L-Type, Protein Kinase Inhibitors
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