Polo-box domain: a versatile mediator of polo-like kinase function
نویسندگان
چکیده
منابع مشابه
Putting a bit into the polo-box domain of polo-like kinase 1
Polo-like kinase 1 (Plk1) plays key roles in regulating various mitotic processes that are critical for cellular proliferation. A growing body of evidence suggests that Plk1 overexpression is tightly associated with the development of human cancers. Interestingly, various types of cancer cells are shown to be addicted to a high level of Plk1, and the reversal of Plk1 addiction appears to be an ...
متن کاملInhibition of polo-like kinase 1 by blocking polo-box domain-dependent protein-protein interactions.
The serine/threonine kinase Polo-like kinase 1 (Plk1) is overexpressed in many types of human cancers, and has been implicated as an adverse prognostic marker for cancer patients. Plk1 localizes to its intracellular anchoring sites via its polo-box domain (PBD). Here we show that Plk1 can be inhibited by small molecules which interfere with its intracellular localization by inhibiting the funct...
متن کاملIdentification of a novel Polo-like kinase 1 inhibitor that specifically blocks the functions of Polo-Box domain
Polo-like kinase 1 (Plk1) is a promising target for cancer therapy due to its essential role in cell division. In addition to a highly conserved kinase domain, Plk1 also contains a Polo-Box domain (PBD), which is essential for Plk1's subcellular localization and mitotic functions. We adopted a fluorescence polarization assay and identified a new Plk1 PBD inhibitor T521 from a small-molecule com...
متن کاملExploring the Binding Nature of Pyrrolidine Pocket-Dependent Interactions in the Polo-Box Domain of Polo-Like Kinase 1
BACKGROUND Over the years, a great deal of effort has been focused on the design and synthesis of potent, linear peptide inhibitors targeting the polo-like kinase 1 (Plk1), which is critically involved in multiple mitotic processes and has been established as an adverse prognostic marker for tumor patients. Plk1 localizes to its intracellular anchoring sites via its polo-box domain, and inhibit...
متن کاملIdentification of high affinity polo-like kinase 1 (Plk1) polo-box domain binding peptides using oxime-based diversification.
In an effort to develop improved binding antagonists of the polo-like kinase 1 (Plk1) polo-box domain (PBD), we optimized interactions of the known high affinity 5-mer peptide PLHSpT using oxime-based post solid-phase peptide diversification of the N-terminal Pro residue. This allowed us to achieve up to two orders of magnitude potency enhancement. An X-ray crystal structure of the highest affi...
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ژورنال
عنوان ژورنال: Cellular and Molecular Life Sciences
سال: 2010
ISSN: 1420-682X,1420-9071
DOI: 10.1007/s00018-010-0279-9