Abstract
AbstractIn this review, evidence is presented from a number of research groups over the past two decades that show that (5Z)‐7‐oxozeaenol, an initially biologically uninteresting fungal metabolite, is a remarkably selective and potent kinase inhibitor with important antiproliferative and anti‐inflammatory properties. Taken together, this research shows (5Z)‐7‐oxozeaenol to be a surprisingly selective and competitive ATP binder in which the aromatic ring of the resorcylic lactone mimics the adenine ring of ATP; that it binds covalently to a conserved cysteine at a metabolically unstable cis‐enone Michael acceptor; the conformational importance of the macrocycle, which depends on the absolute stereochemistry and hydrogen bonding properties of the 8,9‐diol; and the success of medicinal chemistry in stabilizing the cis‐enone.
Published Version
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