background: gp41 of hiv (human immunodeficiency virus) is a protein that mediates fusion between viral and cellular membranes. the agent, t-20, which has been approved for hiv inhibition, can restrain gp41 function in the fusion process; nevertheless, it has disadvantages like instability, high cost of production and injection form to be delivered twice a day. methods: several molecules like nb...

The role of the GABA transporter in acute toxicity in chick retina due to metabolic inhibition was investigated by the use of several substrate (nipecotic acid, THPO) and nonsubstrate (SKF 89976A, NO711) GABA transport inhibitors. Metabolic stress-induced acute toxicity in the retina is characterized by swelling of distinct populations of retinal neurons and selective release of GABA into the m...

1. The application of metabolic inhibitors to nerve-muscle synapses on 'white' and 'red' fibres in the retractor unguis muscles of P. americana and B. giganteus resulted in a dramatic increase in the spontaneous miniature potential discharge and was accompanied by a summation of the miniature potentials to form 'composite' potentials. 2. Axon terminals associated with 'white' muscle fibres resp...

One approach to target the long-term metabolic toxicity and disfiguring body-shape changes associated with antiretroviral therapy is to switch one component of a regimen to an alternative drug, usually from a different class of antiretrovirals. Most commonly, substitutions have involved protease inhibitors, but the thymidine analogue nucleosides, especially stavudine, have been investigated mor...

11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) plays a key role in converting intracellular cortisone to physiologically active cortisol, which is implicated in the development of several phenotypes of metabolic syndrome. Inhibition of 11β-HSD1 activity with selective inhibitors has beneficial effects on various conditions, including diabetes, dyslipidemia and obesity, and therefore constit...