Progress in Drug Research (Paperback, Softcover reprint of the original 1st ed. 1998)

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].

General

Imprint:	Birkhauser Verlag AG
Country of origin:	Switzerland
Series:	Progress in Drug Research, 51
Release date:	November 2011
First published:	1998
Authors:	Ernst Jucker
Dimensions:	244 x 170 x 18mm (L x W x T)
Format:	Paperback
Pages:	326
Edition:	Softcover reprint of the original 1st ed. 1998
ISBN-13:	978-3-03-489798-3
Categories:	Books > Medicine > Nursing & ancillary services > Pharmacy / dispensing Books > Medicine > Other branches of medicine > Pharmacology > General
LSN:	3-03-489798-7
Barcode:	9783034897983

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