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Synthesis and evaluation of inhibitors for Polo-box domain of Polo-like kinase 1

  • Eun Kyoung Ryu (Research Center for Bioconvergence Analysis, Korea Basic Science Institute)
  • Received : 2020.12.15
  • Accepted : 2020.12.29
  • Published : 2020.12.31

Abstract

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.

Keywords

Acknowledgement

이 논문은 한국연구재단 중견연구자지원사업(2020R1A2C1009289)의 지원에 의하여 이루어졌으며 다른 이해관계는 없음을 밝힙니다.

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