Lens epithelium-derived growth factor (LEDGF/p75) plays an essential role in the HIV-1
replication. It acts by tethering integrase (IN) into the host cellular chromatin. Due to its significance
of the IN-LEDGF/p75 interaction affords a novel therapeutic approach for the design of new classes of
antiretroviral agents. To date, many small molecules have been found to be the inhibitors of INLEDGF/
p75 interaction. This review summarizes recent advances in the development of potential
structure-based IN-LEDGF/p75 interaction inhibitors. The work will be helpful to shed light on the
antiretroviral drug development pipeline in the next future.
Keywords: HIV-1; integrase; LEDGF/p75; integrase-LEDGF/p75 interaction inhibitors .
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