2. Academic Validation
  3. MKI-1, a Novel Small-Molecule Inhibitor of MASTL, Exerts Antitumor and Radiosensitizer Activities Through PP2A Activation in Breast Cancer

MKI-1, a Novel Small-Molecule Inhibitor of MASTL, Exerts Antitumor and Radiosensitizer Activities Through PP2A Activation in Breast Cancer

  • Front Oncol. 2020 Sep 29;10:571601. doi: 10.3389/fonc.2020.571601.
Ah-Young Kim 1,  Yi Na Yoon 1 2,  Jiyeon Leem 3,  Jee-Young Lee 4,  Kwan-Young Jung 5,  Minsung Kang 1,  Jiyeon Ahn 1,  Sang-Gu Hwang 1,  Jeong Su Oh 3,  Jae-Sung Kim 1 2
Affiliations

Affiliations

  • 1 Division of Radiation Biomedical Research, Korea Institute of Radiological and Medical Sciences, Seoul, South Korea.
  • 2 Radiological and Medico-Oncological Sciences, University of Science and Technology, Daejeon, South Korea.
  • 3 Department of Integrative Biotechnology, Sungkyunkwan University, Suwon, South Korea.
  • 4 New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, South Korea.
  • 5 Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Daejeon, South Korea.
PMID: 33117702 DOI: 10.3389/fonc.2020.571601
Abstract

Although MASTL (microtubule-associated serine/threonine kinase-like) is an attractive target for Anticancer treatment, MASTL inhibitors with antitumor activity have not yet been reported. In this study, we have presented a novel MASTL inhibitor, MKI-1, identified through in silico screening and in vitro analysis. Our data revealed that MKI-1 exerted antitumor and radiosensitizer activities in in vitro and in vivo models of breast Cancer. The mechanism of action of MKI-1 occurred through an increase in PP2A activity, which subsequently decreased the c-Myc protein content in breast Cancer cells. Moreover, the activity of MKI-1 in the regulation of MASTL-PP2A was validated in a mouse oocyte model. Our results have demonstrated a new small-molecule inhibitor of MASTL, MKI-1, which exerts antitumor and radiosensitizer activities through PP2A activation in breast Cancer in vitro and in vivo.

Keywords

MASTL; PP2A; antitumor; breast cancer; radiosensitizer.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-137552
    98.13%, MASTL 抑制剂
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