Developments of Polo-like Kinase 1 (Plk1) Inhibitors as Anti-Cancer Agents

Author(s): Shanshan Li, Yingjie Zhang, Wenfang Xu

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 13 , Issue 14 , 2013

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Polo-like kinases (Plks) are a family of serine/threonine kinases with a highly conserved N-terminal Ser/Thr kinase catalytic domain and a C-terminal region that play crucial roles in cell cycle progression. Plk1, playing a key role in multiple steps of mitotic progression, is the most studied member of the family. It is overexpressed in a wide spectrum of cancer types and is a promising target in oncology. Most of Plk1 inhibitors competitively bind to the ATP-binding site, which is characterized with unique features. Other inhibitors target regions outside the ATP pocket. In this review some pre-clinical or clinical Plk1 inhibitors are reported, focusing on SAR studies and biological activities, including the kinase activity, in vitro and in vivo anti-tumor efficacy. Those studies exhibited the inhibitors’ significant therapeutic effects. Moreover, combination therapies of these Plk1 inhibitors with other anticancer drugs resulted with synergistic effects.

Keywords: Antitumor activity, clinical, inhibitors, Polo-like kinases, pre-clinical, selectivity, SAR.

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Article Details

Year: 2013
Page: [2014 - 2025]
Pages: 12
DOI: 10.2174/13895575113136660103
Price: $65

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