RT info:eu-repo/semantics/article
T1 TSAO compounds: The comprehensive story of a unique family of HIV-1 specific inhibitors of reverse transcriptase
A1 Camarasa Rius, María José
A1 San Félix García, Ana
A1 Velázquez Díaz, Sonsoles
A1 Pérez Pérez, María Jesús
A1 Gago Badenas, Federico
A1 Balzarini, Jan
K1 Reverse transcriptase
K1 Non-nucleoside RT inhibitors
K1 TSAO compounds
K1 Resistance
K1 Dimerization
K1 Ciencia
K1 Farmacología
K1 Science
K1 Pharmacology
AB 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.
PB Bentham Science Publishers
YR 2004
FD 2004
LK http://hdl.handle.net/10017/5047
UL http://hdl.handle.net/10017/5047
LA eng
DS MINDS@UW
RD 25-abr-2024