Current Enzyme Inhibition - Volume 10, Issue 1, 2014

Aldose reductase (AR) is an enzyme that catalyzes the rate limiting step of the polyol pathway of glucose metabolism. Besides reducing glucose to sorbitol, it reduces a number of lipid peroxidation derived aldehydes and their glutathione conjugates. Recent studies suggest that apart from its involvement in diabetic complications, it also has a pivotal role in inflammatory diseases such as atherosclerosis, sepsis, asthma, uveitis, Read More

This review article tries to be an update of 2008 Pungitore’s review. Again, this paper tries to summarize the investigation about natural products, synthetic and non-nucleoside compounds with the ability to inhibit enzymes that play a crucial role in DNA metabolism such as replication, transcription, retro-transcription, recombination, and chromosome segregation during mitosis. The focus is placed on DNA polymerases, Read More

Various derivatives of a modified estradiol core bearing a fused γ-lactone were designed as non-estrogenic inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1). The compounds were synthesized, characterized and tested for their ability to inhibit enzyme activity (transformation of estrone into estradiol). The proliferative (estrogenic) activity of the compounds was also investigated on estrogen-sen Read More

Tramadol is an analgesic drug that binds to specific opioid receptors. It may contribute to the inhibition of neuronal re-uptake of noradrenaline. Catalase is a key enzyme for degrading H2O2 in cells and has various isoforms with different structures and kinetics properties. In this research, the effect of tramadol on the activity of catalase of Pseudomonas and mouse liver was investigated and compared. Tramadol could inhibit P Read More

The aim of this study consisted in extracting and quantifying phenolic and flavonoids compounds of five selected Algerian plants. The second step was devoted to studying the effects of phenolic compounds on the kinetics catalyzed by two enzymes belonging to the class of hydrolase (the α - amylase and the α - glucosidase) responsible for the digestion of sugars. Finally, we assessed the potential antiradical of our extracts. Th Read More

A series of phenyl alkyl ketone derivatives based phosphodiesterase 4 (PDE4) inhibitors was subjected to 2D Quantitative Structure–Activity Relationships (2D QSAR) and Hologram Quantitative Structure–Activity Relationship (HQSAR) studies. The dataset was divided into training and test sets by applying K-means clustering, and 2D QSAR models were established using stepwise linear regression analysis, replacement meth Read More