Cyclin-Dependent Kinases 4 (CDK4) belongs to a family of serine-threonine protein kinase and plays key regulatory role in G1-phase of cell cycle progression. Compelling evidences have shown that targeting CDK4 pathway is an attractive proposition for tumor therapy. Recent progresses of selective small molecule CDK4 inhibitors in cancer therapy have endorsed the field to be interested and attractive. In this review, we will discuss the recent developments of CDK4 inhibitors on several aspects such as the structure of CDK4, the working mechanism of CDK4 inhibitors, the structure activity relationships (SARs) of the selective CDK4 inhibitors and the latest developments of the selective CDK4 inhibitors in clinical trials.
Keywords: Anti-cancer agents, cell cycle, clinical trials, cyclin-dependent kinases 4, selective inhibitors, structure activity relationship (SAR).