title: Nahuoic acid A produced by a Streptomyces sp. isolated from a marine sediment is a selective SAM-competitive inhibitor of the histone methyltransferase SETD8.
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.
authors.affiliation: Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, BC, Canada V6T 1Z1.
authors.forename: David E
authors.initials: DE
authors.lastname: Williams
authors.forename: Doralyn S
authors.initials: DS
authors.lastname: Dalisay
authors.forename: Fengling
authors.initials: F
authors.lastname: Li
authors.forename: James
authors.initials: J
authors.lastname: Amphlett
authors.forename: Wisanu
authors.initials: W
authors.lastname: Maneerat
authors.forename: Miguel Angel Garcia
authors.initials: MA
authors.lastname: Chavez
authors.forename: Yan Alexander
authors.initials: YA
authors.lastname: Wang
authors.forename: Teatulohi
authors.initials: T
authors.lastname: Matainaho
authors.forename: Wenyu
authors.initials: W
authors.lastname: Yu
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Brown
authors.forename: Cheryl H
authors.initials: CH
authors.lastname: Arrowsmith
authors.forename: Masoud
authors.initials: M
authors.lastname: Vedadi
authors.forename: Raymond J
authors.initials: RJ
authors.lastname: Andersen
mesh_terms: D019015:Geologic Sediments / Q000737:chemistry*; D011495:Histone-Lysine N-Methyltransferase / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D061065:Polyketides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D013302:Streptomyces / Q000737:chemistry*
chemical_list: D061065:Polyketides; C580730:nahuoic acid A; D011495:Histone-Lysine N-Methyltransferase