Current Enzyme Inhibition - Volume 12, Issue 1, 2016

The first generation of Nitric Oxide Synthases inhibitors was synthesized in the late 1980’s and early 1990’s; they were mainly amino acid derivatives, binding to the same residues within the enzyme heme-active site with respect to the natural substrate L-Arg, and showed no or scarce selectivity. In 1994, the N-(3-(aminomethyl)-benzyl) acetamidine (1400W), a highly selective compound for human iNOS versus both hu Read More

Nitric oxide is being explored for the treatment of neuropsychiatric disorders since decades. The molecule has shown to alter different neurotransmitters comprising norepinephrine, serotonin, glutamate and dopamine and thus plays an important role in the neurobiology of major depression. A large number of studies have depicted a dual-nature of this molecule in the pathophysiology of major depression and rela Read More

Nitric Oxide (NO) is the smallest known molecule in the mammalian biological signaling system. It is well established in the field of molecular biology as an endothelium derived growth factor. It is biosynthesized from L-arginine by three enzyme isoforms - endothelial NOS (eNOS or NOS3), neuronal NOS (nNOS or NOS1) and inducible NOS (iNOS or NOS2). In last two decades, all these enzyme isoforms were investigated to u Read More

It has been observed that the overproduction of Nitric Oxide (NO) causes disfunction of several organs and affects lactate level. Hence, attempts have been made to design and develop potent inhibitors for Nitric Oxide Synthases (NOSs), the enzymes which are responsible for its production. NOSs exist mainly in three different isoforms: neuronal, inducible, and endothelial, designated as nNOS, iNOS, and eNOS, respectively. F Read More

NO is a key signaling molecule that has a wide range of biological functions including vasodilation and neurotransmission, and is implicated in several pathological conditions. Therefore, modulation of NO is a desired step in curbing the NO-associated disease processes. Targetting NOS proteins and inhibiting their activity to reduce NO production is a major approach since the inception of NOS inhibitor research. Although Read More