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KMID : 1145520200060020081
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Journal of Radiopharmaceuticals and Molecular Probes
2020 Volume.6 No. 2 p.81 ~ p.87
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Synthesis and evaluation of inhibitors for Polo-box domain of Polo-like kinase 1
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Ryu Eun-Kyoung
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Abstract
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Polo-like kinase 1 (Plk1) is a key protein in mitosis and has been validated as a target for tumor therapy. It is well known to highly overexpress in many kinds of tumor, which has been implicated as a potential biomarker for tumor treatment and diagnosis. Plk1 consists of two domains, the N-terminus kinase domain and the C-terminus polo-box domain (PBD). The inhibitors have been developed for PBD of Plk1, which were shown a high level of affinity and selectivity for Plk1 that led to mitotic arrest and apoptotic cell death. This review discusses the inhibitors for PBD of Plk1 that are suitable for in vivo tumor treatment. They can be further extended for developing in vivo imaging probes for early diagnosis of tumor.
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KEYWORD
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Polo-like kinase 1, Polo-box domain, inhibitor, Tumor, Treatment, Diagnosis
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