The terminal (catalytic) adenosine of the HIV LTR controls the kinetics of binding and dissociation of HIV integrase strand transfer inhibitors

The kinetics of binding of a specific HIV strand transfer inhibitor to integrase variants assembled with systematic changes to the terminal 3' adenosine is described. The results indicated that the terminal deoxyribose play a critical role to retard the rate of inhibitor dissociation, either by sterically blocking inhibitor egress or by a direct interaction with the bound inhibitor.