Identification of vibsanin A analog as a novel HSP90 inhibitor

Kazuki Miura, Wataru Matsuki, Akihiro Ogura, Ken ichi Takao, Siro Simizu

Research output: Contribution to journalArticle

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.

Original languageEnglish
Article number115253
JournalBioorganic and Medicinal Chemistry
Volume28
Issue number2
DOIs
Publication statusPublished - 2020 Jan 15

Fingerprint

Cells
Cell Line
Neoplasms
Viburnum
vibsanin A
Protein Refolding
Bioactivity
Biological Products
Luciferases
Human Activities
Proteins
Pharmaceutical Preparations

Keywords

  • Anti-cancer activity
  • HSP90 inhibitor
  • Natural product
  • Vibsanin A

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Identification of vibsanin A analog as a novel HSP90 inhibitor. / Miura, Kazuki; Matsuki, Wataru; Ogura, Akihiro; Takao, Ken ichi; Simizu, Siro.

In: Bioorganic and Medicinal Chemistry, Vol. 28, No. 2, 115253, 15.01.2020.

Research output: Contribution to journalArticle

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