HIV-1 Integrase Inhibitors: 2007-2008 Update

In recent years, HIV-1 integrase (IN) has become an attractive target for designing anti-retroviral agents. The first IN inhibitor approved for clinical use, raltegravir, has validated the pharmacological viability of IN inhibitors and signals the advent of a new generation of antiretroviral drugs. The development of raltegravir and other successful lead IN inhibitors has also influenced the IN inhibitor design strategy. This has led to the identification of several potent inhibitors in these last two years. Further, an increased understanding of IN structural biology has opened up novel approaches to inhibiting IN, such as targeting its multimerization or interaction with cellular cofactors. This review covers recent developments in the field of IN inhibitor design from 2007 to 2008. (C) 2010 Wiley Periodicals, Inc. Med Res Rev, 30, No. 6, 890-954, 2010