Current development on HIV-1 protease inhibitors

Although a number of potent and selective inhibitors have been developed and approved as drugs for the treatment of HIV infection, efforts still needed in order to develop new inhibitors that are more potent, have unique resistance patterns, and minimal side effects. This review focuses to the HIV-1...

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Bibliographic Details
Main Authors: Arusksakunwong O., Promsri S., Wittayanarakul K., Nimmanpipug P., Lee V.S., Wijitkosoom A., Sompornpisut P., Hannongbua S.
Format: Review
Language:English
Published: 2014
Online Access:http://www.scopus.com/inward/record.url?eid=2-s2.0-51949109972&partnerID=40&md5=6446436a7e1a1ddf0312325abcda335b
http://cmuir.cmu.ac.th/handle/6653943832/5165
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Institution: Chiang Mai University
Language: English
Description
Summary:Although a number of potent and selective inhibitors have been developed and approved as drugs for the treatment of HIV infection, efforts still needed in order to develop new inhibitors that are more potent, have unique resistance patterns, and minimal side effects. This review focuses to the HIV-1 protease (HIV-1 PR), the enzyme belongs to the family of aspartic acid based on the identification of the Asp-Thr-Gly catalytic triad. In the fast part, general features of the HIV-1 PR as well as its structure and functions were given. Afterwards, the review was targeted to discovery, characteristic, activity and emergence of drug resistant of the nine FDA (Food and Drug Administration) approval inhibitors, indinavir, saquinavir, nelfinavir, ritonavir, lopinavir, amprenavir, tipranavir, atazanavir and fosamprenavir. In addition, the two promising inhibitors (brecanavir, darunavir), which are currently under development, as well as a competitive non-peptide based inhibitors (water soluble C60 derivatives) were also introduced. © 2007 Bentham Science Publishers Ltd.