“To test this hypothesis, we first synthesized several aromatic enediyne derivatives”
“In a recent study Jones et al. examined the viability of proteins as targets of thermally and photo-activated enediyne derivatives and confirmed at the molecular level.”
“The table shows the IC50 values for inhibition of recombinant proprotein convertases furin, PC5 and PC7 by various aromatic enediyne compounds.”
“Among the compounds tested, a 12-membered 1, 4-diaza enediyne heterocyclic ring compound with bis-benzyl substituent (AB-2) has been found to exhibit highest inhibitory activities against both furin and PC7 with IC”
“Kar M, Mandal S (2005) Dependence of reactivity of a novel 2,6-diamino pyridine-based enediyne on the extent of salt formation with external acids: a possible implication in pH based drug design.”
“This is the first report of PC-inhibitory activity of an enediyne compound”
“They have shown that specifically designed enediyne derivatives can degrade proteins under suitable conditions”
“Most aromatic enediyne compounds are chemically highly reactive and can easily generate upon heating reactive bis-radical species”
“Except for minor protease activating effect of AB-3 towards PC7, all other enediyne compounds exhibited inhibitory effects towards furin, PC5 and PC7 with IC”
“Due to this unique ability to cyclize and produce reactive bis-radicals, several enediyne derivatives have been designed as reactive species especially for DNA degradation”
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