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Future Med Chem ; 9(16): 1939-1962, 2017 10.
Article in English | MEDLINE | ID: mdl-29076761

ABSTRACT

Selective abrogation of cyclin-dependent kinases (CDK) activity is a highly promising strategy in cancer treatment. The atypical CDK, CDK5 has long been known for its role in neurodegenerative diseases, and is becoming an attractive drug target for cancer therapy. Myriads of recent studies have uncovered that aberrant expression of CDK5 contributes to the oncogenic initiation and progression of multiple solid and hematological malignancies. CDK5 is also implicated in the regulation of cancer stem cell biology. In this review, we present the current state of knowledge of CDK5 as a druggable target for cancer treatment. We also provide a detailed outlook of designing selective and potent inhibitors of this enzyme.


Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cyclin-Dependent Kinase 5/metabolism , Cell Cycle , Cyclin-Dependent Kinase 5/antagonists & inhibitors , Humans , Molecular Structure , Molecular Targeted Therapy/methods , Neoplastic Stem Cells/drug effects , Neoplastic Stem Cells/metabolism , Protein Binding , Protein Conformation , Structure-Activity Relationship
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