Polo-like Kinase 4 Inhibition: A Strategy for Cancer Therapy?
نویسندگان
چکیده
منابع مشابه
Polo-like kinase 4 inhibition: a strategy for cancer therapy?
In this issue of Cancer Cell, Mason and colleagues describe the development of a Polo-like kinase 4 (PLK4) inhibitor (CFI-400945), with promising activity against tumors formed in mice from patient-derived tumor tissue. A clinical trial has been initiated, but questions remain as to whether PLK4 is the only relevant therapeutic target.
متن کاملTargeting Polo-like kinase in cancer therapy.
Polo-like kinases (Plk) function in mitosis and maintaining DNA integrity. There are four family members, of which Plk1 represents a target for anticancer therapy. Plk1 is only expressed in dividing cells with peak expression during G2/M. Plk1 functions in multiple steps of mitosis, and is overexpressed in many tumor types. Mitotic arrest and inhibition of proliferation, apoptosis, and tumor gr...
متن کاملPolo-like kinase 1 as target for cancer therapy
Polo-like kinase 1 (Plk1) is an interesting molecule both as a biomarker and as a target for highly specific cancer therapy for several reasons. Firstly, it is over-expressed in many cancers and can serve as a biomarker to monitor treatment efficacy of Plk1 inhibitors. Furthermore, the Plk1 enzyme is expressed only in dividing cells and is a major regulator of the cell cycle. It controls entry ...
متن کاملPolo-like kinase 4 shapes up.
Polo-like kinase 4 (Plk4) is a master regulator of centriole duplication and targets to centrioles through the association of its cryptic polo box domain with centriole receptors. In this issue of Structure, Shimanovskaya and colleagues unveil a new dimeric architecture of Plk4's cryptic polo box that reveals a conserved mechanism for centriole targeting of the kinase.
متن کاملAutoinhibition and relief mechanism for Polo-like kinase 4.
Polo-like kinase 4 (Plk4) is a master regulator of centriole duplication, and its hyperactivity induces centriole amplification. Homodimeric Plk4 has been shown to be ubiquitinated as a result of autophosphorylation, thus promoting its own degradation and preventing centriole amplification. Unlike other Plks, Plk4 contains three rather than two Polo box domains, and the function of its third Po...
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ژورنال
عنوان ژورنال: Cancer Cell
سال: 2014
ISSN: 1535-6108
DOI: 10.1016/j.ccr.2014.07.017