Inhibitors of the Human Immunodeficiency Virus Protease

摘要: HIV protease inhibitors (PIs) were first introduced into clinical practice in 1996, and their use has resulted major benefits for human immunodeficiency virus (HIV) -infected people terms of better viral suppression, improved immune restoration, reduced morbidity, longer survival. This chapter focuses on the biochemical molecular basis inhibition HIV-1 aspartic (PR), virological PI resistance, implications therapeutics infections proposes research that is still needed order to further improve PIs offer medicine. Drug-resistant viruses have been described all developed date. Some strains recovered from extensively treated patients display cross-resistance a variety PIs. Additionally, structural data highly resistant PR containing 10 resistance mutations revealed an expansion active site, as result separation flaps by much A, while this distance only 4 A case wild-type PR. The degree suppression replication interaction between exposure drug inherent susceptibility infecting such drug, within diverse environments tissues. study efflux transporters role penetration into, distribution within, so-called sanctuary sites may lead ways making these compartments more susceptible antiretrovirals (ARVs).