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Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).

Abstract：

:Sustained proliferative capacity and gene dysregulation are hallmarks of cancer. In mammalian cells, cyclin-dependent kinases (CDKs) control critical cell cycle checkpoints and key transcriptional events in response to extracellular and intracellular signals leading to proliferation. Significant clinical activity for the treatment of hormone receptor positive metastatic breast cancer has been demonstrated by palbociclib, ribociclib and abemaciclib, dual CDK4/6 inhibitors recently FDA-approved. SY-1365, a CDK7 inhibitor has shown initial encouraging data in phase I for solid tumors treatment. These results have rejuvenated the CDKs research field. This review provides an overview of relevant advances on CDK inhibitor research since 2015 to 2019, with special emphasis on transcriptional CDK inhibitors, new emerging strategies such as target protein degradation and compounds under clinical evaluation.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Sánchez-Martínez C,Lallena MJ,Sanfeliciano SG,de Dios A

doi

10.1016/j.bmcl.2019.126637

subject

Has Abstract

pub_date

2019-10-15 00:00:00

pages

126637

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(19)30582-7

journal_volume

29

pub_type

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