ArticleACS chemical biology2012
The CDK9 C-helix exhibits conformational plasticity that may explain the selectivity of CAN508.
Article in ACS chemical biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 59 citations in OpenAlex.
- Structure-Based Design of Potent and Selective MerTK Inhibitors by Modulating the Conformation of αC Helix.Journal of medicinal chemistry · 2025Article
- CDK9 inhibitors for the treatment of solid tumors.Biochemical pharmacology · 2024Review
- Article
- 3,4,3'-Tri-RSC advances · 2022Article
- CDK9 inhibitors in cancer research.RSC medicinal chemistry · 2022Review
- Pharmacophore-based virtual screening, synthesis, biological evaluation, and molecular docking study of novel pyrrolizines bearing urea/thiourea moieties with potential cytotoxicity and CDK inhibitory activities.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Novel pyrrolizines bearing 3,4,5-trimethoxyphenyl moiety: design, synthesis, molecular docking, and biological evaluation as potential multi-target cytotoxic agents.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- CDK9: A Comprehensive Review of Its Biology, and Its Role as a Potential Target for Anti-Cancer Agents.Frontiers in oncology · 2021Review
- 2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors.Scientific reports · 2018Article
- Structure-based discovery of cyclin-dependent protein kinase inhibitors.Essays in biochemistry · 2017Review
- Antitumor effects of cyclin dependent kinase 9 inhibition in esophageal adenocarcinoma.Oncotarget · 2017Article
- Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.Journal of medicinal chemistry · 2016Article
- Efficient soluble expression of active recombinant human cyclin A2 mediated by E. coli molecular chaperones.Protein expression and purification · 2015Article
- Discovery of novel 5-fluoro-MedChemComm · 2015Article
- Determining the Functions of HIV-1 Tat and a Second Magnesium Ion in the CDK9/Cyclin T1 Complex: A Molecular Dynamics Simulation Study.PloS one · 2015Article
- Cyclin dependent kinase-9 mediated transcriptional de-regulation of cMYC as a critical determinant of endocrine-therapy resistance in breast cancers.Breast cancer research and treatment · 2014Article
- Computational study and peptide inhibitors design for the CDK9 - cyclin T1 complex.Journal of molecular modeling · 2013Article
- Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.Journal of medicinal chemistry · 2013Article
- Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.Journal of medicinal chemistry · 2013Article
- The CDK9 tail determines the reaction pathway of positive transcription elongation factor b.Structure (London, England : 1993) · 2012Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
CDK9 is the kinase of positive transcription elongation factor b and facilitates the transition of paused RNA polymerase II to processive transcription elongation. CDK9 is a validated target for the treatment of cancer, cardiac hypertrophy, and human immunodeficiency virus. Here we analyze different CDK9/cyclin T variants to identify a form of the complex amenable to use in inhibitor design. To demonstrate the utility of this system, we have determined the crystal structures of CDK9/cyclin T and CDK2/cyclin A bound to the CDK9-specific inhibitor CAN508. Comparison of the structures reveals CDK9-specific conformational changes and identifies a CDK9-specific hydrophobic pocket, adjacent to the αC-helix. By comparison with a previously published structure of CDK9/cyclin T/human immunodeficiency virus TAT we find that the CDK9 αC-helix has a degree of conformational variability that has the potential to be exploited for inhibitor design.
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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.