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

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منابع مشابه

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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Resistance mechanism of human immunodeficiency virus type-1 protease to inhibitors: A molecular dynamic approach

Human immunodeficiency virus type 1 (HIV-1) protease inhibitors comprise an important class of drugs used in HIV treatments. However, mutations of protease genes accelerated by low fidelity of reverse transcriptase yield drug resistant mutants of reduced affinities for the inhibitors. This problem is considered to be a serious barrier against HIV treatment for the foreseeable future. In this st...

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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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Venom Components of Iranian Scorpion Hemiscorpius lepturus Inhibit the Growth and Replication of Human Immunodeficiency Virus 1 (HIV-1)

Background: During the recent years, significant progress has been achieved on development of novel anti-viral drugs. Natural products are assumed as the potential sources of novel anti-viral drugs; therefore, there are some previous studies reporting the anti-viral compounds from venomous animals. Based on the significant value for tracing of non-toxic anti-viral agents from natural resources,...

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ژورنال

عنوان ژورنال: Antimicrobial Agents and Chemotherapy

سال: 2001

ISSN: 0066-4804,1098-6596

DOI: 10.1128/aac.45.1.158-165.2001