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Medicinal Chemistry of HIV Integrase InhibitorsMedicinal Chemistry of HIV Integrase Inhibitors

When AIDS was first discovered in the 1980s, an individual's prognosis was grim, with a life expectancy on the order of 10 years. With development of effective antiviral drugs, this has increased up to 50 years. The HIV virus encodes several enzymes that are drug targets. The first effective drugs that were developed inhibit reverse transcriptase.


The structure to the left is the first HIV integrase that has made it's way to market, raltegravir (Isentress).

Structure of the first HIV integrase inhibitor to market, raltegravir (PDB entry RLT)

Drag the structure with the mouse to rotate

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Arthur Cox