Biomaterial Database

Enfuvirtide, the first fusion inhibitor to treat HIV infection. 2005

Eva Poveda, and Verónica Briz, and Vincent Soriano

Department of Infectious Diseases, Hospital Carlos III, Madrid, Spain.

Entry inhibitors are a new class of drugs for the treatment of HIV infection. Enfuvirtide is the first compound of this family to be approved for clinical use. It blocks HIV fusion to host cells. It is a synthetic peptide that mimics an HR2 fragment of gp41, blocking the formation of a six-helix bundle structure which is critical in the fusion process. Enfuvirtide is a good therapeutic option as rescue therapy in combination with other active antiretrovirals and works against different HIV-1 variants, including all group M subtypes and group O. However, it is not active against HIV-2. The main mechanism of resistance to enfuvirtide depends of the selection of changes in a 10-amino acid domain between residues 36 to 45 in the HR1 region of gp41. Single and double mutations in this region have been shown to result in high-level resistance to enfuvirtide. A negative impact of enfuvirtide-resistance mutations on viral fitness has been postulated, since resistance mutations tend to disappear soon after drug discontinuation and because immunologic benefits have been noticed despite virologic failure in patients undergoing enfuvirtide treatment.

UI	MeSH Term	Description	Entries
D008969	Molecular Sequence Data	Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.	Sequence Data, Molecular,Molecular Sequencing Data,Data, Molecular Sequence,Data, Molecular Sequencing,Sequencing Data, Molecular
D010446	Peptide Fragments	Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.	Peptide Fragment,Fragment, Peptide,Fragments, Peptide
D006678	HIV	Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.	AIDS Virus,HTLV-III,Human Immunodeficiency Viruses,Human T-Cell Lymphotropic Virus Type III,Human T-Lymphotropic Virus Type III,LAV-HTLV-III,Lymphadenopathy-Associated Virus,Acquired Immune Deficiency Syndrome Virus,Acquired Immunodeficiency Syndrome Virus,Human Immunodeficiency Virus,Human T Cell Lymphotropic Virus Type III,Human T Lymphotropic Virus Type III,Human T-Cell Leukemia Virus Type III,Immunodeficiency Virus, Human,Immunodeficiency Viruses, Human,Virus, Human Immunodeficiency,Viruses, Human Immunodeficiency,AIDS Viruses,Human T Cell Leukemia Virus Type III,Lymphadenopathy Associated Virus,Lymphadenopathy-Associated Viruses,Virus, AIDS,Virus, Lymphadenopathy-Associated,Viruses, AIDS,Viruses, Lymphadenopathy-Associated
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077560	Enfuvirtide	A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS.	DP 178,DP-178,DP178,Fuzeon,Pentafuside,Peptide T20,T20 Peptide,T20, Peptide
D000595	Amino Acid Sequence	The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.	Protein Structure, Primary,Amino Acid Sequences,Sequence, Amino Acid,Sequences, Amino Acid,Primary Protein Structure,Primary Protein Structures,Protein Structures, Primary,Structure, Primary Protein,Structures, Primary Protein
D015658	HIV Infections	Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).	HTLV-III Infections,HTLV-III-LAV Infections,T-Lymphotropic Virus Type III Infections, Human,HIV Coinfection,Coinfection, HIV,Coinfections, HIV,HIV Coinfections,HIV Infection,HTLV III Infections,HTLV III LAV Infections,HTLV-III Infection,HTLV-III-LAV Infection,Infection, HIV,Infection, HTLV-III,Infection, HTLV-III-LAV,Infections, HIV,Infections, HTLV-III,Infections, HTLV-III-LAV,T Lymphotropic Virus Type III Infections, Human
D015700	HIV Envelope Protein gp41	Transmembrane envelope protein of the HUMAN IMMUNODEFICIENCY VIRUS which is encoded by the HIV env gene. It has a molecular weight of 41,000 and is glycosylated. The N-terminal part of gp41 is thought to be involved in CELL FUSION with the CD4 ANTIGENS of T4 LYMPHOCYTES, leading to syncytial formation. Gp41 is one of the most common HIV antigens detected by IMMUNOBLOTTING.	Envelope Protein gp41, HIV,HIV Transmembrane Protein gp41,HTLV-III gp41,env Protein gp41, HIV,gp41(HIV),gp41 Envelope Protein, HIV
D023581	HIV Fusion Inhibitors	Inhibitors of the fusion of HIV to host cells, preventing viral entry. This includes compounds that block attachment of HIV ENVELOPE PROTEIN GP120 to CD4 RECEPTORS.	Fusion Inhibitors, HIV,HIV Cell Fusion Inhibitor,HIV Entry Inhibitor,HIV Entry Inhibitors,HIV Fusion Inhibitor,HIV Fusion Protein Inhibitor,HIV Cell Fusion Inhibitors,HIV Fusion Protein Inhibitors,Entry Inhibitor, HIV,Entry Inhibitors, HIV,Fusion Inhibitor, HIV,Inhibitor, HIV Entry,Inhibitor, HIV Fusion
D024882	Drug Resistance, Viral	The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation.	Antiviral Drug Resistance,Antiviral Drug Resistances,Drug Resistances, Viral