title: Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay.
abstract: Cochliobolic acid (1), a novel biologically active natural product, is produced by submerged fermentation of Cochliobolus lunatus. Compound 1 was determined to be a novel polyketide possessing a substituted tetrahydrofuran ring, a conjugated polyene chain and a 1,2-diketone moiety, by interpretation of NMR, MS, and UV/vis spectroscopic data. Compound 1 inhibits the binding of TGF-alpha to the EGF receptor of the human epidermal cell line A431 in a SPA assay with an IC50 of 1.6 microM.
authors.affiliation: Xenova Ltd., Slough, B erkshire, U.K.
authors.forename: N
authors.initials: N
authors.lastname: Robinson
authors.forename: T M
authors.initials: TM
authors.lastname: Gibson
authors.forename: M I
authors.initials: MI
authors.lastname: Chicarelli-Robinson
authors.forename: L
authors.initials: L
authors.lastname: Cameron
authors.forename: P J
authors.initials: PJ
authors.lastname: Hylands
authors.forename: D
authors.initials: D
authors.lastname: Wilkinson
authors.forename: T J
authors.initials: TJ
authors.lastname: Simpson
mesh_terms: D055598:Chemical Phenomena; D002627:Chemistry, Physical; D066246:ErbB Receptors / Q000187:drug effects / Q000378:metabolism*; D005285:Fermentation; D005663:Furans / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D011090:Polyenes / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D013056:Spectrophotometry, Ultraviolet; D016211:Transforming Growth Factor alpha / Q000378:metabolism*; D013098:Xylariales / Q000737:chemistry*
chemical_list: D005663:Furans; D011090:Polyenes; D016211:Transforming Growth Factor alpha; C104549:cochliobolic acid; D066246:ErbB Receptors