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HIV-1 Integrase

According to the Joint United Nations Programme on HIV/AIDS, 40 million people are estimated to be living with HIV/AIDS. Of these, 37 million are adults and 2.5 million are children under 15. An estimated 5 million people acquired the human immunodeficiency virus (HIV) in 2003, including 4.2 million adults and 700,000 children under 15. During 2003, AIDS caused the deaths of an estimated 3 million people, including 2.5 million adults and 500,000 children under 15.

Integration of viral DNA into the host chromosome is a necessary process in the HIV replication cycle. The key steps of DNA integration are associated with the viral integrase protein, which, along with protease and reverse transcriptase, is one of three enzymes encoded by HIV. Unlike protease and reverse transcriptase, for which several classes of inhibitors have been developed, progress with the development of integrase inhibitors has been slow. A major obstacle has been the absence of good lead compounds that can serve as the starting point for structure based design.

Quantum Pharmaceuticals aims to identify novel lead compounds, which have binding affinities of not more than about 10-8 mol/l and good drug-likeness properties. We will use only our proprietary technology.

Newly found leads will be used as scaffolds for developing novel drug candidates, which will improve the process of AIDS treatment.




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