Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 9, Issue 11, Pages 1016-1037Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/156802609789630910
Keywords
HIV-1 IN; diketo acids; HIV inhibitors; AIDS; IN inhibitors; peptides; oligonucleotides
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Funding
- Center for Cancer Research, an Intramural Division of the National Cancer Institute, National Institutes of Health
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Integrase (IN) is the newest validated target against AIDS and retroviral infections. The remarkable activity of raltegravir (Isentress (R)) led to its rapid approval by the FDA in 2007 as the first IN inhibitor. Several other IN strand transfer inhibitors (STIs) are in development with the primary goal to overcome resistance due to the rapid occurrence of IN mutations in raltegravir-treated patients. Thus, many scientists and drug companies are actively pursuing clinically useful IN inhibitors. The objective of this review is to provide an update on the IN inhibitors reported in the last two years, including second generation STI, recently developed hydroxylated aromatics, natural products, peptide, antibody and oligonucleotide inhibitors. Additionally, the targeting of IN cofactors such as LEDGF and Vpr will be discussed as novel strategies for the treatment of AIDS.
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