TSAO compounds: The comprehensive story of a unique family of HIV-1 specific inhibitors of reverse transcriptase
Autores
Camarasa Rius, María José; San Félix García, Ana; Velázquez Díaz, Sonsoles; Pérez Pérez, María Jesús; Gago Badenas, FedericoIdentificadores
Enlace permanente (URI): http://hdl.handle.net/10017/5047DOI: 10.2174/1568026043388600
Editor
Bentham Science Publishers
Fecha de publicación
2004Cita bibliográfica
Current Topics in Medicinal Chemistry 2004, 4, 945-963
Palabras clave
Reverse transcriptase
Non-nucleoside RT inhibitors
TSAO compounds
Resistance
Dimerization
Tipo de documento
info:eu-repo/semantics/article
Versión
info:eu-repo/semantics/publishedVersion
Versión del editor
http://dx.doi.org/10.2174/1568026043388600Derechos de acceso
info:eu-repo/semantics/openAccess
Resumen
Emergence of drug-resistant viral strains is one of the major milestones and the main cause for the failure of antiretroviral therapy. Combination of different anti-HIV agents has E become the standard clinical practice to keep the viral load at low or even undetectable levels and to prevent emergence of virus-drug resistance. Among the human immunodeficiency virus (HIV) reverse transcriptase (RT) inhibitors, the so called nonnucleoside RT inhibitors (NNRTIs) have gained a definitive place in the treatment of HIV infections in combination with nucleoside analogue RT inhibitors (NRTIs) and HIV protease inhibitors (PIs). The virus can be markedly suppressed for a relatively long period of time when exposed to multiple drug combination therapy (highly active antiretroviral therapy, HAART). TSAO derivatives are a peculiar group of highly functionalized nucleosides that belong to the so-called nonnucleoside RT inhibitors (NNRTIs). They exert their unique selectivity for HIV-1 through a specific interaction with the p51 subunit of HIV-1 RT. They are the first small molecules that seem to interfere with the dimerization process of the enzyme. This review covers the work carried out with this unique class of specific inhibitors of HIV-1 reverse transcriptase, including structure activity relationship studies (SAR), its mechanism of action, resistance studies, model of interaction with the enzyme, etc.
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