Cyclins and cyclin-dependent kinases (CDKs) play versatile roles in promoting the hallmarks of cancer. Therefore, cyclins CDKs have been widely studied targeted cancer treatment, with four CDK4/6 inhibitors being approved by FDA many other examined clinical trials. The specific purpose this review is to delineate role therapeutic potential Cyclin K cancers. Studies shown that regulates essentia...

BACKGROUND Protein kinases play a central role in tumor progression, regulating fundamental processes such as angiogenesis, proliferation and metastasis. Such enzymes are an increasingly important class of drug target with small molecule kinase inhibitors being a major focus in drug development. However, balancing drug specificity and efficacy is problematic with off-target effects and toxicity...

The present work deals with design, synthesis, mechanistic study and biological evaluation of novel, diverse compounds as potential inhibitors of cyclin-dependent kinase 2 (CDK2). Multi-complex-based method has been suggested to generate a comprehensive pharmacophore map of cyclin-dependent kinase 2 (CDK2) based on a collection of 13 crystal structures of human CDK2 inhibitor complex. The propo...

Cdc25A, a phosphatase essential for G1-S transition, associates with, dephosphorylates, and activates the cell cycle kinase cyclin E-cdk2. p21CIP1 and p27 are cyclin-dependent kinase (cdk) inhibitors induced by growth-suppressive signals such as p53 and transforming growth factor beta (TGF-beta). We have identified a cyclin binding motif near the N terminus of Cdc25A that is similar to the cycl...

Treatment of MCF-7 cells with the peroxisome proliferator-activated receptor (PPAR) agonists ciglitazone or 15-deoxy12,14-prostaglandin J2 resulted in a concentrationand time-dependent decrease of cyclin D1 and estrogen receptor (ER) proteins, and this was accompanied by decreased cell proliferation and G1-G03S-phase progression. Downregulation of cyclin D1 and ER by PPAR agonists was inhibited...