A small-molecule inhibitor shows that pirin regulates migration of melanoma cells

Isao Miyazaki, Siro Simizu, Hideo Okumura, Satoshi Takagi, Hiroyuki Osada

Research output: Contribution to journalArticle

55 Citations (Scopus)

Abstract

The discovery of small molecules that bind to a specific target and disrupt the function of proteins is an important step in chemical biology, especially for poorly characterized proteins. Human pirin is a nuclear protein of unknown function that is widely expressed in punctate subnuclear structures in human tissues. Here, we report the discovery of a small molecule that binds to pirin. We determined how the small molecule bound to pirin by solving the cocrystal structure. Either knockdown of pirin or treatment with the small molecule inhibited melanoma cell migration. Thus, inhibition of pirin by the small molecule has led to a greater understanding of the function of pirin and represents a new method of studying pirin-mediated signaling pathways.

Original languageEnglish
Pages (from-to)667-673
Number of pages7
JournalNature Chemical Biology
Volume6
Issue number9
DOIs
Publication statusPublished - 2010 Sep
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Biology
  • Cell Biology

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