Current Enzyme Inhibition - Volume 10, Issue 2, 2014

Poly(ADP-ribosyl)ation is one of the most pertinent post translational modifications involved in regulation of chromatin structure, cell cycle progression, tissue development and differentiation and other vital biological phenomena. The enzymes that catalyze the synthesis and degradation of poly(ADP) ribose polymers are PARP and PARG, respectively. The role of PARP has been implicated in development of various diseases Read More

Natural proteinaceous protease inhibitors inhibit through nonproductive binding to proteases and steric blockage of active sites. These complexes are among the most structurally complementary protein-protein interactions. To see if complementarity is correlated to activity, we scored the shape complementarity in 15 serine protease-inhibitor complexes through in silico docking and compared the scores against their repor Read More

Despite the explosion in structural biologythe multi-dimensional complexity of the structure determination process of biomolecules like proteins significantly poses hindrances to drug development and study of interaction of ligands to the target. Since virtual screening has come up as a potential tool in the process of drug discovery the availability of macromolecular structures has limitations. Moreover, when more than Read More

Tuberculosis (TB) remains to be one of the major public health concerns worldwide. The continuing emergence of Mtb strains resistant to known drugs makes the campaign for successful TB control and treatment very difficult to accomplish. It is therefore imperative to search for newer chemical entities that could inhibit the growing number of putative drug targets for the development of more efficient anti-tubercular dr Read More

Lipase inhibitors have a high pharmacological interest because they could help in the therapy of diseases in which lipases play an important role such as obesity. Extracts from two Algerian spontaneous plants: Oudneya africana and Pulicaria crispa, were screened for potential lipase inhibitory activity. The enzymatic inhibition produced by these plants extracts is described here for the first time. Additionally, the antioxidant activi Read More

Lipase inhibitors are drugs used to reduce the activity of lipase found in the intestine. These inhibitors are used for the treatment of obesity and cardiovascular diseases. The purpose of this work was to explore in vitro the enzymatic and antioxidant activities of secondary metabolites extracts such as, phenolic compounds, flavonoids and tannins obtained with various extraction solvent systems: methanol/water, acetone/water Read More

Eighty four endophytic fungi were isolated from Ocimum sanctum. Secondary metabolites extracted from these endophytic fungi were tested for the inhibitors of enzymes responsible for the glycaemic index and polyol pathway. Six isolates were positive for both α-glucosidase and α-amylase inhibitors. Secondary metabolites from four endophytic fungal isolates inhibited aldose reductase enzyme extracted from rat lens. Crud Read More

Colchicine is a toxic alkaloid known for its therapeutic applications. In addition to the inhibition of microtubule polymerization, colchicine has been reported to inhibit many key enzymes. Here we provide evidence for colchicine binding and inhibiting ζ-crystallin purified from camel eye lens. Indeed, we demonstrated the molecular interaction between colchicine and ζ-crystallin using fluorescence quenching. Moreover, colchic Read More

Dextransucrase isolated from Weissella cibaria JAG8 was subjected to active site mapping analysis by using lysine specific inhibitor viz. pyridoxal-5’-phosphate (PLP) and 2,4,6-trinitrobenzenesulphonic acid (TNBS) gave 98.5% and 98.7% inhibition in enzyme activity at 25 mM concentration respectively. The -NH2 lysine derivative of enzymeinhibitor complex with PLP and TNBS gave absorbance maxima at 325 and 369 nm, re Read More