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OverviewDue 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]. Full Product DetailsAuthor: Ernst JuckerPublisher: Birkhauser Verlag AG Imprint: Birkhauser Verlag AG Edition: Softcover reprint of the original 1st ed. 1998 Volume: 51 Dimensions: Width: 17.00cm , Height: 1.80cm , Length: 24.40cm Weight: 0.586kg ISBN: 9783034897983ISBN 10: 3034897987 Pages: 326 Publication Date: 12 November 2011 Audience: College/higher education , Professional and scholarly , Postgraduate, Research & Scholarly , Professional & Vocational Format: Paperback Publisher's Status: Active Availability: Manufactured on demand  We will order this item for you from a manufactured on demand supplier. Table of ContentsDevelopment of HIV protease inhibitors: A survey.- Insulin resistance, impaired glucose tolerance and non-insulin-dependent diabetes, pathologic mechanisms and treatment: Current status and therapeutic possibilities.- Peptide drug delivery into the central nervous system.- Abnormalities of protein kinases in neurodegenerative diseases.- Biomimicry as a basis for drug discovery.- Serotonin in migraine: Theories, animal models and emerging therapies.- The application of high-throughput screening to novel lead discovery.- Index Vol. 51.- Index of titles, Vol. 1–51.- Author and paper index, Vol. 1–51.ReviewsAuthor InformationTab Content 6Author Website:Countries AvailableAll regions |
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