Current Enzyme Inhibition - Volume 5, Issue 3, 2009

Disulfide reductases are involved in many functions in the cell, in particular, maintaining the intracellular redox balance. Many classes of these enzymes exist, and their inhibition has served as an effective therapy against different types of human diseases. The involvement of disulfide reductases in various cellular processes is reviewed, and therapeutic strategies against pathogenic bacteria, parasitic infections, and hu Read More

Somatic angiotensin-converting enzyme (ACE) - well known for its role in cardiovascular pathophysiology - has an unusual, two-domain, double active-site structure. The two domains (designated N and C) are 55% identical and each contains a similar active site with overlapping but distinct substrate preferences. While both convert angiotensin I to angiotensin II in vitro, current evidence suggests the C domain site predomin Read More

Diacylglycerol kinases (DGKs), a family of lipid kinases, convert diacylglycerol (DG) to phosphatidic acid (PA). Acting as a second messenger, DG activates protein kinase C (PKC). PA, a signaling lipid, regulates diverse functions involved in physiological responses. Since DGK modulates two lipid second messengers, DG and PA, regulation of DGK could induce related cellular responses. Currently, there are 10 mammalian isoforms Read More

SHIP (SH2 domain containing inositol phosphatases) was identified as a 145kDa multi-domain cytosolic protein expressed specifically in hematopoietic cells that negatively regulates cell growth, survival and proliferation. Aberrant SHIP function is associated with many disease pathologies. There are two aspects to SHIP function: the catalytic function mediated by the central catalytic domain and the non-catalyti Read More

Hydrolysis of D-valyl-L-leucyl-L-arginine 4-nitroanilide (120-640 μM) by rat tissue kallikrein (rK1) (3.15 nM) was studied in both the absence and the presence of increasing concentrations of aprotinin (10.4-34.6 nM), a serine protease inhibitor also known as basic pancreatic trypsin inhibitor, which inhibits trypsin, chymotrypsin, plasmin and kallikrein. The data indicate that the inhibition of rK1 by aprotinin is a parabolic competitive in Read More

Free radicals are causative factor for aminoglycoside induced tissue injury. Fixed dose combination therapy of ceftazidime plus tobramycin reduces liver toxicity than single therapy of tobramycin. The objective of present study was designed to determine the activity of antioxidant enzymes as well as some biochemical parameters along with MDA level by the administration of tobramycin and its fixed dose combination (FDC) wit Read More