Comparative analysis of anti-human immunodeficiency virus type 1 activities of dideoxynucleoside analogs in resting and activated peripheral blood mononuclear cells.

Antimicrobial Agents and Chemotherapy
T ShirasakaH Mitsuya

Abstract

We determined the anti-human immunodeficiency virus type 1 (anti-HIV-1) activities of various dideoxy-nucleoside analogs by using phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMs) and resting PBMs (R-PBMs) as target cells. The comparative order of anti-HIV-1 activity in PHA-PBMs was azidothymidine (AZT) > dideoxycytidine (ddC) > dideoxythymidinene (d4T) > dideoxyinosine (ddI) and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) > 2'-beta-fluoro-dideoxyadenosine (F-ara-ddA), while that in R-PBMs was ddC > ddI, PMEA, and F-ara-ddA, >> AZT and d4T. A pronucleotide, bis-(S-acetylthioethanol)phosphotriester-ddAMP, which bypasses the anabolic monophosphorylation step for the intracellular delivery of ddAMP, was highly active both in PHA-PBMs and R-PBMs. These data may have basic and clinical relevance in the design of anti-HIV chemotherapy, particularly combination chemotherapy with dideoxynucleosides, and in the development of active pronucleotides.

References

Sep 28, 1990·Science·H MitsuyaS Broder
Jan 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·T ShirasakaH Mitsuya
Apr 25, 2008·Current Protocols in Immunology·D D RichmanH Mitsuya

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Citations

Sep 22, 2001·Molecular Immunology·S Z SackM D Scharff
Mar 25, 2008·Journal of Acquired Immune Deficiency Syndromes : JAIDS·Julie B DumondAngela D M Kashuba
Jul 27, 2004·Antimicrobial Agents and Chemotherapy·Jesús Saavedra-LozanoOctavio Ramilo
Apr 23, 2008·Current Protocols in Nucleic Acid Chemistry·Suzanne Peyrottes, Christian Périgaud
May 30, 2003·The Annals of Pharmacotherapy·Shellee A Grim, Frank Romanelli

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