The current status of the NNRTI family of antiretrovirals used in the HAART regime against HIV infection

• Tipo: Outra Publicação em Revista Científica Internacional
• Data: 2008

Autores

Silvia Martins (Autor) Outra; Maria Joao Ramos (Autor) FCUP; Pedro Alexandrino Fernandes (Autor) FCUP

Revista

Título: Current Medicinal Chemistry

Vol. 15 Nº 22

Páginas: 1083-1095

ISSN: 0929-8673

Editora: Bentham Science

Indexação

ISI Web of Knowledge - 55 Citações

Scopus - 62 Citações

Classificação Científica

FOS: Ciências médicas e da saúde > Medicina básica

Outras Informações

ID Authenticus: P-003-ZKR

DOI: 10.2174/092986708784221467

Abstract (EN): Acquired immunodeficiency syndrome (AIDS) remains, after 25 years of its discovery, as one of the major threats to human life. Reverse Transcriptase is an essential enzyme for virus replication, and therefore constitutes a major target in HIV-1 therapy. Among the different types of drugs targeting RT, the nonnucleoside reverse transcriptase inhibitors (NNRTIs) act by binding in an induced-fit allosteric pocket. In this review, we explore the several NNRTIs' structures and binding interactions, as well as their mechanisms of action. The conformational changes that they cause in RT and their effects on the topology of the active site are discussed. The emergence of mutant, resistant viruses is analysed, focussing on the mutations responsible for the loss of antiviral efficacy of NNRTIs. Explanations for the role of those mutations are presented. Emergent drugs in the pipeline, together with the underlying strategies for drug development, are also analysed.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 13