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Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities.
The isolation and structure elucidation of new apicidins from two Fusarium species, temperature-dependent NMR studies of apicIDin, NMR and molecular modeling based conformation of the 12-membered macrocyclic ring, and selected chemical modifications of Apicidin have been detailed in this paper.
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK.
A resorcylic acid lactone, L-783,277, isolated from a Phoma sp. (ATCC 74403) which came from the fruitbody of Helvella acetabulum, is a potent and specific inhibitor of MEK (Map kinase kinase).
Durhamycin A, a potent inhibitor of HIV Tat transactivation.
Durhamycin A was discovered as a potent inhibitor (IC(50) = 4.8 nM) of Tat transactivation of HIV transactivation in efforts to discover Tat inhibitors from natural product screening of microbial fermentation extracts.
Isolation, structure, and absolute stereochemistry of platensimycin, a broad spectrum antibiotic discovered using an antisense differential sensitivity strategy.
It was determined that potential reactivity of the enone moiety does not play a key role in the biological activity of platensimycin and cyclohexenone ring conformation renders for the stronger binding interaction with the enzyme.