Overview of CDK9 as a target in cancer research Morales, Fátima Giordano, Antonio CDK9 Molecular modelling Antitumor Anticancer Drug development Cyclin Kinase This work was supported by the Fund for Sbarro Health Research Organization (SHRO) and for the Italian Association for Cancer Research (Associazione Italiana per la Ricerca sul Cancro, AIRC). The award of a postdoctoral grant from the Martín Escudero Foundation CDK9 is a protein in constant development in cancer therapy. Herein we present an overview of the enzyme as a target for cancer therapy. We provide data on its characteristics and mechanism of action. In recent years, CDK9 inhibitors that have been designed with molecular modeling have demonstrated good antitumoral activity in vitro. Clinical studies of the drugs flavopiridol, dinaciclib, seliciclib, SNS-032 and RGB-286638 used as CDK9 inhibitors are also reviewed, with their additional targets and their relative IC 50 values. Unfortunately, treatment with these drugs remains unsuccessful and involves many adverse effects. We could conclude that there are many small molecules that bind to CDK9, but their lack of selectivity against other CDKs do not allow them to get to the clinical use. However, drug designers currently have the tools needed to improve the selectivity of CDK9 inhibitors and to make successful treatment available to patients. 2024-09-23T12:34:13Z 2024-09-23T12:34:13Z 2016-03-09 journal article Morales, F., & Giordano, A. (2016). Overview of CDK9 as a target in cancer research. Cell Cycle, 15(4), 519–527. https://doi.org/10.1080/15384101.2016.1138186 https://hdl.handle.net/10481/94924 10.1080/15384101.2016.1138186 eng http://creativecommons.org/licenses/by-nc-nd/4.0/ open access Attribution-NonCommercial-NoDerivatives 4.0 Internacional Taylor & Francis