A kinetic model for comparing proteolytic processing activity and inhibitor resistance potential of mutant HIV-1 proteases.

A kinetic model is presented for the comparison of potential proteolytic processing activities of wild-type and mutant human immunodeficiency virus proteases in the presence and absence of protease inhibitors. The protease processing of gag substrate in the immature virions is assessed by the kinetic parameters, kcat, Km and Ki. The relationship of the estimated potential processing activities to the viability of the HIV mutants and their tendencies to resist inhibitors also are discussed. A fully developed model has the potential to stimulate the results of inhibitor resistance either in vivo or in cell culture.