title: HIV entry inhibitors: a new generation of antiretroviral drugs.
abstract: AIDS is presently treatable, and patients can have a good prognosis due to the success of highly active antiretroviral therapy (HAART), but it is still not curable or preventable. High toxicity of HAART, and the emergence of drug resistance add to the imperative to continue research into new strategies and interventions. Considerable progress in the understanding of HIV attachment and entry into host cells has suggested new possibilities for rationally designing agents that interfere with this process. The approval and introduction of the fusion inhibitor enfuvirtide (Fuzeon) for clinical use signals a new era in AIDS therapeutics. Here we review the crucial steps the virus uses to achieve cell entry, which merit attention as potential targets, and the compounds at pre-clinical and clinical development stages, reported to effectively inhibit cell entry.
authors.affiliation: Department of Applied Biochemistry and Immunology, Institute of Molecular Biology and Biotechnology, Vassilika Vouton, Heraklion, Crete, Greece. krambo@imbb.forth.gr
authors.forename: Elias
authors.initials: E
authors.lastname: Krambovitis
authors.forename: Filippos
authors.initials: F
authors.lastname: Porichis
authors.forename: Demetrios A
authors.initials: DA
authors.lastname: Spandidos
mesh_terms: D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy; D000818:Animals; D019380:Anti-HIV Agents / Q000494:pharmacology* / Q000627:therapeutic use; D015496:CD4-Positive T-Lymphocytes / Q000187:drug effects; D024882:Drug Resistance, Viral; D000077560:Enfuvirtide; D015699:HIV Envelope Protein gp120 / Q000187:drug effects; D015700:HIV Envelope Protein gp41 / Q000494:pharmacology* / Q000627:therapeutic use; D023581:HIV Fusion Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D015497:HIV-1 / Q000502:physiology*; D006801:Humans; D010446:Peptide Fragments / Q000494:pharmacology* / Q000627:therapeutic use; D019713:Receptors, CCR5 / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D015699:HIV Envelope Protein gp120; D015700:HIV Envelope Protein gp41; D023581:HIV Fusion Inhibitors; D010446:Peptide Fragments; D019713:Receptors, CCR5; C474741:peptide T1249; D000077560:Enfuvirtide