2. Academic Validation
  3. Identification of vibsanin A analog as a novel HSP90 inhibitor

Identification of vibsanin A analog as a novel HSP90 inhibitor

  • Bioorg Med Chem. 2020 Jan 15;28(2):115253. doi: 10.1016/j.bmc.2019.115253.
Kazuki Miura 1,  Wataru Matsuki 1,  Akihiro Ogura 1,  Ken-Ichi Takao 1,  Siro Simizu 2
Affiliations

Affiliations

  • 1 Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan.
  • 2 Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan. Electronic address: simizu@applc.keio.ac.jp.
PMID: 31859027 DOI: 10.1016/j.bmc.2019.115253
Abstract

Vibsanin A is the first natural product isolated from Viburnum awabuki and has several biological activities. We have reported that a vibsanin A analog, obtained from process of total synthesis of vibsanin A, has anti-proliferative activity against human Cancer cell lines. In this study, we evaluated anti-proliferative effect of the vibsanin A analogs against various human Cancer cell lines and examined molecular target of the analog in human cells. Among the vibsanin A analogs, vibsanin A analog C (VAC) showed anti-proliferative effect against various Cancer cell lines, and the anti-proliferative activity was strongest among the vibsanin A analogs. Additionally, VAC fluctuated amounts of HSP90-related proteins in cells and inhibited HSP90-mediated protein refolding of luciferase in vitro. These results suggest that the anti-proliferative activity of VAC is due to HSP90 inhibition, and VAC has a potential as novel anti-cancer drug as HSP90 Inhibitor.

Keywords

Anti-cancer activity; HSP90 inhibitor; Natural product; Vibsanin A.

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