Identification of the Metabolic Profile of the α-Tubulin-Binding Natural Product (-)-Pironetin

Sara K. Coulup, David S. Huang, Henry L. Wong, Gunda I. Georg

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

Pironetin, the only crystallographically confirmed natural product to target α-tubulin, displays potent cytotoxic activity against sensitive and resistant A2780 ovarian cancer cell lines but is only marginally active in vivo. We now report that pironetin has a short half-life (<7 min) in human liver microsomes, suggesting that its limited in vivo efficacy is due to rapid metabolism. Further, we describe the discovery of epoxypironetin as pironetin's major metabolite in human liver microsomes.

Original languageEnglish (US)
Pages (from-to)1684-1689
Number of pages6
JournalJournal of medicinal chemistry
Volume62
Issue number3
DOIs
StatePublished - Feb 14 2019

PubMed: MeSH publication types

  • Journal Article
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

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