期刊
CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 9, 期 11, 页码 1016-1037出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/156802609789630910
关键词
HIV-1 IN; diketo acids; HIV inhibitors; AIDS; IN inhibitors; peptides; oligonucleotides
资金
- Center for Cancer Research, an Intramural Division of the National Cancer Institute, National Institutes of Health
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.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据