Inhibitors of HIV-1 Entry and Integration: Recent Developments and Impact on Treatment
Anil K. Sharma, Varghese George, Ranjini Valiathan, Sudheesh Pilakka-Kanthikeel and Suresh Pallikkuth
Affiliation: Microbiology and Immunology, University of Miami Miller School of Medicine, 1580 NW 10th Avenue, BCRI 708, Miami, FL 33136, USA.
Advances in the drug development against HIV-1 have lead to the identification of new compounds which
could be used to target cellular entry and nuclear integration of virus in addition to drugs that commonly target reverse
transcriptase and protease. These additional targets have added a new dimension to fight against HIV. Cellular entry of
HIV is a multistep procedure involving a range of cellular and molecular interactions between virus envelope protein and
receptors expressed on the surface of the target cells, thus providing many opportunities to block infection. Some of these
entry inhibitors are currently being used in the clinic and more compounds are under various stages of development. Integration
of the HIV-1 DNA is required and essential to maintain the viral DNA in the infected cell. The design and discovery
of integrase inhibitors were first focused at targeting the catalytic site of integrase that selectively acting on strand
transfer and thus inhibits integration of virus DNA with host cell genome. Thus, entry and integrase inhibitors present a
real added value in combined treatment against HIV infection. This review discusses the recent development in the discovery
of inhibitors of HIV entry and integration along with some of recent patents in the field.
Keywords: ART, entry inhibitors, HIV, HIV-1, HIV patents, HIV treatment, integrase inhibitors, Raltegravir.
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