Progress in Drug Research - Couverture souple

Couverture souple

ISBN 10 : 3034897987 ISBN 13 : 9783034897983

Editeur : Birkhäuser, 2011

Synopsis

Due tothedevelopmentofdrugresistanceandotherlimitationsinthe treat­ ment of AIDS patients with reverse transcriptase (RT) inhibitors like zidovu­ dineandothers, itbecamenecessarytoexploreantiviralagentsactingontar­ getsotherthan RT. Inthepastfewyears, hundredsofHIVproteaseinhibitoLs have been synthesized and tested. Among these protease inhibitors, saquinavir, ritonavir, indinavir and nelfinavir have been marketed during 1995-1997. In this review, emphasis is placed on the development of HIV protease inhibitors as antiviral agents against HIV, structure-activity rela­ tionship (SAR) analysis ofsaquinavirand relatedcompounds, comparisonof four marketed HIV protease inhibitors, and future prospect in developing new anti-HIV drugs. 2 Introduction HIV protease inhibitors 3 HIV protease as a target for chemotherapy HIV protease was first suggested as a potential target for AIDS therapy by Kramer et a1. in 1986 [5]. HIV protease is a proteolytic enzyme responsible for cleaving large numbers of amino acid sequences. This enzyme regulates conversionoftheselargeaminoacid sequencesintobiologicallyactive struc­ tural and functional protein products. Specifically, HIV protease is responsi­ the enzymatic processing of the gagand gag-pol genes of HIV, which ble for encode for functional core proteins and viral enzymes (reverse transcriptase, ribonuclease H, integrase, and HIV protease). The polyproteins encoded by the gagand gag-pol genes undergo post-translational processing by HIV pro­ tease to form functional protein products as the viral particles budding out from infected cells. Therefore, inhibition of HIV protease by a protease inhibitor results in the release ofimmature, noninfectious viral particles [4].

Détails de l'édition

• Éditeur: Birkhäuser
• Date d'édition: 2011
• Langue: anglais
• ISBN 10: 3034897987
• ISBN 13: 9783034897983
• Reliure: Broché
• Nombre de pages: 340
• Éditeur: Jucker Ernst
• Coordonnées du fabricant: Springer Nature Customer Service Center GmbH; ProductSafety@springernature.com; ; Europaplatz 3; Heidelberg; 69115; Allemagne