TSAO Derivatives: Highly Specific Inhibitors of Human Immunodeficiency Virus Type-1 (HIV-1) Replication

Maria J. Camarasa Instituto de Quíamica Méadica (C. S. I. C.). Juan de la Cierva, 3. 28006, Madrid, Spain

Maria J. Péarez-Péarez Instituto de Quíamica Méadica (C. S. I. C.). Juan de la Cierva, 3. 28006, Madrid, Spain

Sonsoles Velázquez Instituto de Quíamica Méadica (C. S. I. C.). Juan de la Cierva, 3. 28006, Madrid, Spain

Ana San-Féalix Instituto de Quíamica Méadica (C. S. I. C.). Juan de la Cierva, 3. 28006, Madrid, Spain

Rosa Alvarez Instituto de Quíamica Méadica (C. S. I. C.). Juan de la Cierva, 3. 28006, Madrid, Spain

Simon Ingate Instituto de Quíamica Méadica (C. S. I. C.). Juan de la Cierva, 3. 28006, Madrid, Spain

Maria Luisa Jimeno Instituto de Quíamica Méadica (C. S. I. C.). Juan de la Cierva, 3. 28006, Madrid, Spain

Anna Karlsson Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000, Leuven, Belgium

Erik De Clercq Karolinska Institute, Biochemical Laboratory I, S-10401, Stockholm, Sweden

Jan Balzarini Karolinska Institute, Biochemical Laboratory I, S-10401, Stockholm, Sweden

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Abstract

TSAO derivatives represent a unique class of nucleosides that are specifically targeted at HIV-1 RT. This overview is focussed on the chemical synthesis, the conformational studies, the antiviral and metabolic properties of TSAO derivatives, as well as their mechanism of antiviral action and the molecular basis of the rapid selection of resistant HIV-1 strains that emerge in cell culture in the presence of TSAO derivatives.

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TSAO Derivatives: Highly Specific Inhibitors of Human Immunodeficiency Virus Type-1 (HIV-1) Replication

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TSAO Derivatives: Highly Specific Inhibitors of Human Immunodeficiency Virus Type-1 (HIV-1) Replication

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