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
نویسندگان
چکیده
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 Molecular Genetics, National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina 27709; Center for Drug Discovery, Department of Pharmaceutical and Biomedical Sciences, The University of Georgia College of Pharmacy, Athens, Georgia 30602; Department of Clinical Pharmacology and The Liver Center, University of Alabama at Birmingham, Birmingham, Alabama 35294; and Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia 30322, and Veterans Affairs Medical Center, Decatur, Georgia 30033
منابع مشابه
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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