Important note: Information in this article was accurate in 1998. The state of the art may have changed since the publication date.
PRNewswire - Thursday October 8, 1998
"To our knowledge, this is the first study demonstrating the potency of such derivatives," stated Dr. Rakesh Vig, lead author on the study. None of the compounds studied exhibited any detectable toxicity meaning they probably will not have any negative side-effects in humans.
The clinical potential of this derivative compound is being evaluated in detailed preclinical studies. The derivative is currently under development for future clinical trials. It is anticipated that these studies will potentially provide the basis for the design of more potent anti-HIV drugs.
The mechanism that Institute scientists used to create this drug derivative is also noteworthy because it is one of the most complete computer models of the HIV virus in the world. A description of this model and the research that lead to its creation will be published this month in the prestigious drug discovery and chemistry journal, Bioorganic & Medicinal Chemistry (ref 2). To create the model, Institute scientists basically combined all known HIV model coordinates into one all-encompassing model which they use to predict which drugs might be effective against the AIDS virus. With knowledge gained from this model, scientists are now able to better understand the complex makeup of HIV, in particular a substance called reverse transcriptase which the virus uses to survive. Using this model, they can design drugs which bind to the virus even if that virus has mutations which make other drugs ineffective. This new breakthrough in the fight against AIDS is likely to stimulate new research since it describes how powerful anti-AIDS drugs can be developed by using a computer model.
The Hughes Institute is a non-profit research organization located in Roseville, MN dedicated to combating cancer, AIDS and diseases of the immune system. References:
1. Vig R, Venkatachalam TK, Uckun FM. D4T-5'-[p-bromophenyl methoxyalaninyl phosphate] as a potent and non-toxic anti-HIV agent. Antiviral Chemistry & Chemotherapy, 9(5), 1998
2. Vig R, Mao C, Venkatachalam TK, Tuel-Ahlgren L, Sudbeck EA, Uckun FM. Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase. Bioorganic & Medical Chemistry, 10:1789-1997, 1998.
SOURCE: Hughes Institute
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