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Druq design - Essay Example

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The human immunodeficiency virus (HIV) was first discovered in 1985.HIV is most commonly transmitted by sexual contact and needle-sharing due to the exchange of body fluids like blood and semen. The virus damages the body’s immune system resulting in AIDS (acquired immune…
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Download file to see previous pages Inside the cell, the HIV reverse transcriptase converts the viral RNA into DNA; this DNA is transported into the cell nucleus where it is inserted into the human genome by the HIV integrase enzyme. The HIV DNA may lie dormant, but is later expressed for the synthesis of new HIV proteins and enzymes. The HIV protease is active at this stage of the life cycle where its role is to cut long protein strands to form viral cores.
The development of the pathogenic effects of HIV is characterized by the interaction between viral and host factors. A broad spectrum of antiviral strategies was developed for each step of the viral replication cycle. Every stage in the life cycle, and every gene product of HIV is a potential target. Host proteins that are recognized to have an essential role in the viral life cycle are also targets of HIV therapy (Nielsen, Pedersen, & Kjems, 2005). As of 2007, more than 20 anti-HIV drugs have been approved (De Clerq, 2007). The drugs block the enzyme activity of any of the enzyme that HIV needs to replicate inside host cells: reverse transcriptase, protease, fusion inhibitors, and lately integrase inhibitors. The norm is to utilize highly active antiretroviral therapy (HAART), which combines two or three drugs to overcome the development of drug resistant targets. Nevertheless, multi-drug resistant HIV continue to develop due to the high viral mutation rates.
Integrase is the chosen target for the drug to be designed for HIV treatment; it facilitates the insertion of the double-stranded DNA copy of the HIV RNA genome into the host genome, an absolute requirement for viral replication (LaFemina, et al., 1992). Integration of the HIV DNA requires 3 processing of the final two bases of the viral DNA long terminal repeat (LTR), and DNA strand transfer activity. HIV integrase was found to be composed of several multimers with functional domains sufficient for 3 processing and ...Download file to see next pagesRead More
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