Design of HIV Protease Inhibitors Targeting Protein Backbone: An Effective Strategy for Combating Drug Resistance

2008 ◽  
Vol 41 (1) ◽  
pp. 78-86 ◽  
Author(s):  
Arun K. Ghosh ◽  
Bruno D. Chapsal ◽  
Irene T. Weber ◽  
Hiroaki Mitsuya
Keyword(s):  
Drug Resistance ◽  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Effective Strategy ◽  
Protein Backbone

scholarly journals Reviewing HIV-1 Gag Mutations in Protease Inhibitors Resistance: Insights for Possible Novel Gag Inhibitor Designs

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3243 ◽  
Author(s):  
Chinh Tran-To Su ◽  
Darius Wen-Shuo Koh ◽  
Samuel Ken-En Gan
Keyword(s):  
Drug Resistance ◽  
Protease Inhibitors ◽  
Structural Changes ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Resistance Mutations ◽  
Drug Resistance Mutations ◽  
Viral Maturation ◽  
Inhibitor Resistance

HIV protease inhibitors against the viral protease are often hampered by drug resistance mutations in protease and in the viral substrate Gag. To overcome this drug resistance and inhibit viral maturation, targeting Gag alongside protease rather than targeting protease alone may be more efficient. In order to successfully inhibit Gag, understanding of its drug resistance mutations and the elicited structural changes on protease binding needs to be investigated. While mutations on Gag have already been mapped to protease inhibitor resistance, there remain many mutations, particularly the non-cleavage mutations, that are not characterized. Through structural studies to unravel how Gag mutations contributes to protease drug resistance synergistically, it is thus possible to glean insights to design novel Gag inhibitors. In this review, we discuss the structural role of both novel and previously reported Gag mutations in PI resistance, and how new Gag inhibitors can be designed.

Bis-Tetrahydrofuran: A Privileged Ligand for Darunavir and a New Generation of HIV Protease Inhibitors that Combat Drug Resistance.

ChemInform ◽  
2006 ◽  
Vol 37 (48) ◽  
Author(s):  
Arun K. Ghosh ◽  
Perali Ramu Sridhar ◽  
Nagaswamy Kumaragurubaran ◽  
Yasuhiro Koh ◽  
Irene T. Weber ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
New Generation

Bis-Tetrahydrofuran: a Privileged Ligand for Darunavir and a New Generation of HIV Protease Inhibitors That Combat Drug Resistance

ChemMedChem ◽  
2006 ◽  
Vol 1 (9) ◽  
pp. 939-950 ◽  
Author(s):  
Arun K. Ghosh ◽  
Perali Ramu Sridhar ◽  
Nagaswamy Kumaragurubaran ◽  
Yasuhiro Koh ◽  
Irene T. Weber ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
New Generation

Determining and Overcoming Resistance to HIV Protease Inhibitors

2004 ◽  
Vol 4 (2) ◽  
pp. 137-152 ◽  
Author(s):  
Jana Prejdova ◽  
Milan Soucek ◽  
Jan Konvalinka
Keyword(s):  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors

A QSAR Study of HIV Protease Inhibitors Using Theoretical Descriptors

2010 ◽  
Vol 6 (4) ◽  
pp. 269-282 ◽  
Author(s):  
Subhash C. Basak ◽  
Denise Mills ◽  
Rajni Garg ◽  
Barun Bhhatarai
Keyword(s):  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Qsar Study
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