cvt-313 and dinaciclib

CVT-313 is a potent CDK2 inhibitor that was identified by screening a purine-analogue library and is currently in preclinical studies. Since this molecule has the potential to be developed as a CDK2 inhibitor for cancer therapy, the potency of CVT-313 to bind and stabilize CDK2 was evaluated, together with its ability to inhibit aberrant cell proliferation. CVT-313 increased the melting temperature of CDK2 by 7°C in thermal stabilization studies, thus indicating its protein-stabilizing effect. CVT-313 inhibited the growth of human lung carcinoma cell line A549 in a dose-dependent manner, with an IC

Topics: A549 Cells; Adenosine Triphosphate; Antineoplastic Agents; Binding Sites; Cell Proliferation; Cloning, Molecular; Crystallography, X-Ray; Cyclic N-Oxides; Cyclin-Dependent Kinase 2; Dose-Response Relationship, Drug; Escherichia coli; Gene Expression; Genetic Vectors; Humans; Indolizines; Models, Molecular; Protein Binding; Protein Conformation, alpha-Helical; Protein Conformation, beta-Strand; Protein Interaction Domains and Motifs; Protein Kinase Inhibitors; Purines; Pyridinium Compounds; Recombinant Proteins; Roscovitine