☆ 4.8 Article

Nahuoic Acid A Produced by a Streptomyces sp Isolated From a Marine Sediment Is a Selective SAM-Competitive Inhibitor of the Histone Methyltransferase SETD8

ORGANIC LETTERS (2013)

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Journal

ORGANIC LETTERS
Volume 15, Issue 2, Pages 414-417

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol303416k

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Categories

Chemistry, Organic

Funding

  1. NSERC
  2. CCSRI
  3. CIHR
  4. Eli Lilly Canada
  5. Genome Canada
  6. GlaxoSmithKline
  7. Ontario Ministry of Economic Development and Innovation
  8. Novartis Research Foundation
  9. Pfizer
  10. Abbott
  11. Takeda
  12. Wellcome Trust

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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.

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