title: Development of Selective Cyclin-Dependent Kinase 4 Inhibitors for Antineoplastic Therapies.
abstract: 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.
authors.affiliation: School of Chemistry and Pharmaceutical Engineering, Qilu University of Technology, 3501 Daxue Road, Jinan 250353, China.
authors.forename: Haixing
authors.initials: H
authors.lastname: Guan
authors.affiliation: School of Chemistry and Pharmaceutical Engineering, Qilu University of Technology, 3501 Daxue Road, Jinan 250353, China.
authors.forename: Yongli
authors.initials: Y
authors.lastname: Du
authors.affiliation: School of Chemistry and Pharmaceutical Engineering, Qilu University of Technology, 3501 Daxue Road, Jinan 250353, China.
authors.forename: Weiwei
authors.initials: W
authors.lastname: Han
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China.
authors.forename: Jingkang
authors.initials: J
authors.lastname: Shen
authors.affiliation: Clinical Pharmacy Laboratory, Huashan Hospital, Fudan University, 12 Wu Lu Mu Qi M Road, Shanghai 200040, China.
authors.forename: Qunyi
authors.initials: Q
authors.lastname: Li
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D051358:Cyclin-Dependent Kinase 4 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; C495900:CDK4 protein, human; D051358:Cyclin-Dependent Kinase 4
keywords: Anti-cancer agents; cell cycle; clinical trials; cyclin-dependent kinases 4; selective inhibitors; structure activity relationship
  (SAR)