Favorable Interactions between Enfuvirtide and 1-β- d -2,6-Diaminopurine Dioxolane In Vitro

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منابع مشابه

Favorable interactions between enfuvirtide and 1-beta-D-2,6-diaminopurine dioxolane in vitro.

We evaluated the in vitro anti-human immunodeficiency virus type 1 (HIV-1) interactions between 1-beta-D-2,6-diaminopurine dioxolane (DAPD) and enfuvirtide (T-20) against clinical isolates sensitive and resistant to reverse transcriptase and protease inhibitors. Interactions between T-20 and DAPD were synergistic to nearly additive, with combination index values ranging from 0.53 to 1.06 at 95%...

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Mechanism of Action of 1-b-D-2,6-Diaminopurine Dioxolane, a Prodrug of the Human Immunodeficiency Virus Type 1 Inhibitor 1-b-D-Dioxolane Guanosine

PHILLIP A. FURMAN,* JERRY JEFFREY, LAURA L. KIEFER, JOY Y. FENG, KAREN S. ANDERSON, KATYNA BORROTO-ESODA, EDGAR HILL, WILLIAM C. COPELAND, CHUNG K. CHU, JEAN-PIERRE SOMMADOSSI, IRINA LIBERMAN, RAYMOND F. SCHINAZI, AND GEORGE R. PAINTER Triangle Pharmaceuticals, Durham, North Carolina 27707; Department of Pharmacology, Yale School of Medicine, New Haven, Connecticut 06520-8066; Laboratory of Mol...

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Mechanism of action of 1-beta-D-2,6-diaminopurine dioxolane, a prodrug of the human immunodeficiency virus type 1 inhibitor 1-beta-D-dioxolane guanosine.

(-)-beta-D-2,6-Diaminopurine dioxolane (DAPD), is a nucleoside reverse transcriptase (RT) inhibitor with activity against human immunodeficiency virus type 1 (HIV-1). DAPD, which was designed as a water-soluble prodrug, is deaminated by adenosine deaminase to give (-)-beta-D-dioxolane guanine (DXG). By using calf adenosine deaminase a K(m) value of 15 +/- 0.7 microM was determined for DAPD, whi...

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Enfuvirtide antiretroviral therapy in HIV-1 infection

It has been over 25 years since the first diagnosis of what would be known as AIDS. Although great strides in anti-HIV therapeutics have been made, there is still a great need for antiretrovirals that are effective against drug-resistant HIV. Enfuvirtide (ENF) is the first of a new class of fusion inhibitors to be approved by the US Food and Drug Administration for use in combination with other...

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Synthesis of 6-PEtN-α-D-GalpNAc-(1–>6)-β-D-Galp-(1–>4)-β-D-GlcpNAc-(1–>3)-β-D-Galp-(1–>4)-β-D-Glcp, a Haemophilus influenzae lipopolysacharide structure, and biotin and protein conjugates thereof

BACKGROUND In bacteria with truncated lipopolysaccharide structures, i.e., lacking the O-antigen polysaccharide part, core structures are exposed to the immune system upon infection and thus their use as carbohydrate surface antigens in glycoconjugate vaccines can be considered and investigated. One such suggested structure from Haemophilus influenzae LPS is the phosphorylated pentasaccharide 6...

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ژورنال

عنوان ژورنال: Antimicrobial Agents and Chemotherapy

سال: 2003

ISSN: 0066-4804,1098-6596

DOI: 10.1128/aac.47.11.3644-3646.2003