Current Topics in Medicinal Chemistry - Volume 3, Issue 13, 2003

The replication cycle of human immunodeficiency virus (HIV) is divided into an early and a late phase. Most of the steps of the cycle have been targeted in antiviral therapy, although the drugs currently available for clinical use are only effective against two replication enzymes of the virus, either against the reverse transcriptase or against the viral protease. The introduction of combination anti-retroviral therapy changed th Read More

The field of antiretroviral therapy has witnessed remarkable progress during the past 15 years. There are now over a dozen approved therapeutic agents for infection with the human immunodeficiency virus (HIV), a pathogen that once caused nearly uniformly fatal illness. These agents usually target two essential enzymes of the virus, the reverse transcriptase and the protease. The era of potent antiretroviral therapy, also ter Read More

Control of AIDS requires development of special therapeutic strategies in order to reduce the level of monocyte / macrophage HIV infection, to prevent spread of HIV within the monocyte / macrophage reservoir, to maintain a therapeutically effective drug concentration in sanctuaries such as the brain and to overcome the problem of cellular resistance mechanisms. A popular approach towards this end has been the develo Read More

Replication of human immunodeficiency virus 1 (HIV-1) uses a viral reverse transcriptase (RT) to convert its positive-strand RNA into double stranded DNA, which is then integrated into host genome. Reverse transcription is a complex event involving p66 and p51 RT subunits but also several viral proteins including Nef, Tat, Vif, IN, NCp7 and p55gag. Viral RNA itself forms a primer / template complex by association with Read More

In order to combat the human immunodeficiency virus (HIV), diverse strategies have been developed to research on compounds which can be developed as therapeutic agents. Screening of natural products derived from numerous species has afforded metabolites with significant antiviral activity against the HIV. The marine environment representing approximately half of the global biodiversity offers an enormous resource Read More

Antiretroviral therapy with potent combinations of drugs has been responsible for a significant decline in the occurrences of AIDS defining conditions and death in the developed world. However, therapy requires lifelong use and is complicated by relatively high failure rates, significant toxicities, adherence difficulties and the development of resistance. The combination of these complications of therapy and the availabili Read More