HIV-1 reverse transcriptase: a therapeutical target in the spotlight.
Human Immunodeficiency Virus type 1 Reverse Transcriptase (HIV-1 RT) is one of the most important targets for treatment of Acquired Immune Deficiency Syndrome (AIDS). It catalyzes the reverse transcription of HIV-RNA into a double stranded DNA, and the knowledge of its substrate specificity and catalytic mechanism has guided the development of several inhibitors widely used on current HIV/AIDS therapy. However, mutations in HIV-1 RT structure can lead to the emergence of drug-resistant virus strains. The goal of this review is to summarize relevant structural features of HIV-1 RT and its inhibitors in such a way that this cost-effective target in the development of new antiretroviral drugs is particularly highlighted.
Castro
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HC
Laboratório de Bioquímica e Modelagem Molecular (LaBioMol), Departamento de Biologia Celular e Molecular, IB, Universidade Federal Fluminense (UFF), Outeiro Sao Joao Batista, Niterói, RJ, 24001-970, Brazil. hcastrorangel@yahoo.com.br
Loureiro
N I V
NI
Pujol-Luz
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M
Souza
A M T
AM
Albuquerque
M G
MG
Santos
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DO
Cabral
L M
LM
Frugulhetti
I C
IC
Rodrigues
C R
CR
D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy; D054303:HIV Reverse Transcriptase / Q000737:chemistry / Q000187:drug effects* / Q000235:genetics; D015497:HIV-1 / Q000201:enzymology* / Q000235:genetics / Q000502:physiology; D006801:Humans; D008958:Models, Molecular; D011487:Protein Conformation; D018894:Reverse Transcriptase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D014779:Virus Replication
D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase