Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113244
Abstract: Cyclin-dependent kinases (CDKs) are a family of Ser/Thr kinases involved in cell cycle and transcriptional regulation. CDK9 regulates transcriptional elongation and this unique property has made it a potential target for several diseases. Due to… read more here.
Keywords: cdk9 inhibitors; cdk9; structure based; selective cdk9 ... See more keywords
Discovery and Administration Optimization of Novel Selective CDK9 Inhibitor, 1-7a-B1, for Improved Pharmacokinetics and Antitumor Efficacy In Vivo.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c00472
Abstract: Cyclin-dependent kinase 9 (CDK9) is a member of the transcriptional CDK subfamily. In this work, a de novo design strategy was used to obtain a series of novel CDK9 inhibitors. A novel selective CDK9 inhibitor… read more here.
Keywords: cdk9; cdk9 inhibitor; pharmacokinetics antitumor; improved pharmacokinetics ... See more keywords
Abstract 4295: AZ’5576, a selective CDK9 inhibitor, demonstratesin vitroandin vivoactivity in diverse preclinical models of non-Hodgkin lymphoma
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DOI: 10.1158/1538-7445.am2017-4295
Abstract: Cyclin-dependent kinase 9 (Cdk9) is a serine/threonine kinase that regulates elongation of transcription through phosphorylation of RNA polymerase II at serine 2 (pSer2-RNAPII). Transient inhibition of Cdk9 results in modulation of genes with short-lived transcripts… read more here.
Keywords: inhibitor; hodgkin lymphoma; cdk9; non hodgkin ... See more keywords
Abstract 3409: Design and characterization of highly potent and selective CDK9 heterobifunctional degraders
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-3409
Abstract: Cyclin-dependent kinase 9 (CDK9) has long been considered an attractive therapeutic target for modulating transcription in cancers of high unmet clinical need. CDK9 coordinates signaling events that regulate RNA polymerase II (Pol II) pause-release state… read more here.
Keywords: characterization highly; cdk9; selective cdk9; design characterization ... See more keywords
Selective CDK9 Inhibition by Natural Compound Toyocamycin in Cancer Cells
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DOI: 10.3390/cancers14143340
Abstract: Simple Summary By combining drug screens, transcriptomic studies, and in vitro assays, our study identified the natural product toyocamycin as a potent and selective CDK9 inhibitor. Thus, toyocamycin can be used as a new small… read more here.
Keywords: cdk9 inhibition; cancer cells; cancer; selective cdk9 ... See more keywords