ArticleThe Journal of biological chemistry2009
A novel class of cyclin-dependent kinase inhibitors identified by molecular docking act through a unique mechanism.
Article in The Journal of biological chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
15 citing papers in PubMed, 20 citations in OpenAlex.
- Design, synthesis and evaluation of acetylcholine-antitumor lipid hybrids led to identification of a potential anticancer agent disrupting the CDK4/6-Rb pathway in lung cancer.RSC medicinal chemistry · 2025Article
- Repurposing Tranexamic Acid as an Anticancer Agent.Frontiers in pharmacology · 2021Article
- A composite docking approach for the identification and characterization of ectosteric inhibitors of cathepsin K.PloS one · 2017Article
- Cyclin-Dependent Kinase Inhibitors as Anticancer Therapeutics.Molecular pharmacology · 2015Article
- Novel agents that downregulate EGFR, HER2, and HER3 in parallel.Oncotarget · 2015Article
- Targeting cyclin-dependent kinases in human cancers: from small molecules to Peptide inhibitors.Cancers · 2015Review
- Structure-based discovery of the first allosteric inhibitors of cyclin-dependent kinase 2.Cell cycle (Georgetown, Tex.) · 2014Article
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- A chrysin derivative suppresses skin cancer growth by inhibiting cyclin-dependent kinases.The Journal of biological chemistry · 2013Article
- Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents.Molecular cancer therapeutics · 2013Article
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- Discovery of antimicrobial ribonucleotide reductase inhibitors by screening in microwell format.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- Effects of an Indolocarbazole-Derived CDK4 Inhibitor on Breast Cancer Cells.Journal of Cancer · 2011Article
- CDKN1C negatively regulates RNA polymerase II C-terminal domain phosphorylation in an E2F1-dependent manner.The Journal of biological chemistry · 2010Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
Abstract
The cyclin-dependent kinase (Cdk) family is emerging as an important therapeutic target in the treatment of cancer. Cdks 1, 2, 4, and 6 are the key members that regulate the cell cycle, as opposed to Cdks that control processes such as transcription (Cdk7 and Cdk9). For this reason, Cdks 1, 2, 4, and 6 have been the subject of extensive cell cycle-related research, and consequently many inhibitors have been developed to target these proteins. However, the compounds that comprise the current list of Cdk inhibitors are largely ATP-competitive. Here we report the identification of a novel structural site on Cdk2, which is well conserved between the cell cycle Cdks. Small molecules identified by a high throughput in silico screen of this pocket exhibit cytostatic effects and act by reducing the apparent protein levels of cell cycle Cdks. Drug-induced cell cycle arrest is associated with decreased Rb phosphorylation and decreased expression of E2F-dependent genes. Multiple lines of evidence indicate that the primary mechanism of action of these compounds is the direct induction of Cdk1, Cdk2, and Cdk4 protein aggregation.
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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.