Nahuoic acid A produced by a Streptomyces sp. isolated from a marine sediment is a selective SAM-competitive inhibitor of the histone methyltransferase SETD8

Org Lett. 2013 Jan 18;15(2):414-7. doi: 10.1021/ol303416k. Epub 2012 Dec 28.

Abstract

The histone lysine monomethyltransferase SETD8 is an epigenetic regulator of cell cycle progression. Nahuoic acid A (1), a polyketide produced in culture by a Streptomyces sp. obtained from a tropical marine sediment, is the first known selective SAM-competitive inhibitor of SETD8. The structure of nahuoic acid A (1) has been elucidated by chemical transformation and detailed analysis of spectroscopic data.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Geologic Sediments / chemistry*
  • Histone-Lysine N-Methyltransferase / antagonists & inhibitors*
  • Molecular Structure
  • Nuclear Magnetic Resonance, Biomolecular
  • Polyketides / chemistry
  • Polyketides / isolation & purification*
  • Polyketides / pharmacology*
  • Streptomyces / chemistry*

Substances

  • Polyketides
  • nahuoic acid A
  • Histone-Lysine N-Methyltransferase