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JAC Advance Access originally published online on January 6, 2003
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Journal of Antimicrobial Chemotherapy (2003) 51, 207-211
© 2003 The British Society for Antimicrobial Chemotherapy

Leading Article

HIV protease inhibitors: antiretroviral agents with anti-inflammatory, anti-angiogenic and anti-tumour activity

Paolo Monini, Cecilia Sgadari, Giovanni Barillari and Barbara Ensoli*

Laboratory of Virology, Department of Retrovirus Infection, Istituto Superiore di Sanità, Viale Regina Elena 299, Roma, Italy

Keywords: HIV, protease inhibitors

The first 150 words of the full text of this article appear below.

Despite mild toxicity and adverse effects, human immunodeficiency virus (HIV) protease inhibitors (PIs), used in combination with reverse transcriptase nucleoside inhibitors (NRTIs), have turned AIDS into a chronic, manageable disease. Such combination therapy, known as highly active antiretroviral therapy (HAART), efficiently suppresses HIV replication leading to immune restoration in HIV-infected patients. HIV PIs act by blocking the HIV aspartyl protease, a viral enzyme that cleaves the HIV gag and gag-pol polyprotein backbone at nine specific cleavage sites to produce shorter, functional proteins. Three of the nine cleavage reactions occur between a phenylalanine or a tyrosine and a proline. Strikingly, none of the known mammalian endopeptidases cleaves before a proline; for this reason, most HIV PIs have been designed to mimic the phenylalanine–proline peptide bond. This confers a remarkable specificity of action to HIV PIs and, with short-term treatment, they show only mild side-effects and a tolerable toxicity.1

Unexpectedly, however, the . . . [Full Text of this Article]


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