To test this hypothesis, we first synthesized several aromatic enediyne derivatives ❋ Ajoy Basak Et Al. (2009)
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. ❋ Ajoy Basak Et Al. (2009)
The table shows the IC50 values for inhibition of recombinant proprotein convertases furin, PC5 and PC7 by various aromatic enediyne compounds. ❋ Ajoy Basak Et Al. (2009)
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 ❋ Ajoy Basak Et Al. (2009)
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. ❋ Ajoy Basak Et Al. (2009)
This is the first report of PC-inhibitory activity of an enediyne compound ❋ Ajoy Basak Et Al. (2009)
They have shown that specifically designed enediyne derivatives can degrade proteins under suitable conditions ❋ Ajoy Basak Et Al. (2009)
Most aromatic enediyne compounds are chemically highly reactive and can easily generate upon heating reactive bis-radical species ❋ Ajoy Basak Et Al. (2009)
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 ❋ Ajoy Basak Et Al. (2009)
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 ❋ Ajoy Basak Et Al. (2009)
Basak A, Dasgupta S (2009) Design and synthesis of enediyne-peptide conjugates and their inhibiting activity against chymotrypsin. ❋ Ajoy Basak Et Al. (2009)
This study revealed for the first time that fully nonpeptide aromatic and heterocyclic enediyne compounds can inhibit furin activity in vitro with IC50 in low to medium micromolar ranges depending on the nature of the structure and type of substituent present. ❋ Ajoy Basak Et Al. (2009)
The gradient used was as described in Chemical syntheses and full characterizations of various aryl enediyne compounds ❋ Ajoy Basak Et Al. (2009)
In the proposed mechanism for the early stage of 10-membered enediyne biosynthesis, CalE8 produces a carbonyl-conjugated polyene with the assistance of ❋ M. Kotaka (2009)
Moreover, computational docking suggested that the substrate-binding channel binds a polyene substrate that contains a single cis double bond at the C4 / C5 position, raising the possibility that the C4 = C5 double bond in the enediyne moiety could be generated by the iterative polyketide synthase. ❋ M. Kotaka (2009)
Together, the results revealed a hotdog fold thioesterase distinct from the common type I and type II thioesterases associated with polyketide biosynthesis and provided interesting insight into the enediyne ❋ M. Kotaka (2009)
The biosynthesis of the enediyne moiety of the antitumor natural product calicheamicin involves an iterative polyketide synthase ❋ M. Kotaka (2009)
In vitro enzyme assay of PCs against Boc-RVRR-MCA substrate (50 µM), in the absence and presence of various synthetic aromatic enediyne compounds ( ❋ Ajoy Basak Et Al. (2009)
