Boosting of HIV Protease Inhibitors by Ritonavir in the Intestine: The Relative Role of Cytochrome P450 and P-Glycoprotein Inhibition Based on Caco-2 Monolayers versus In Situ Intestinal Perfusion in Mice

2012 ◽  
Vol 40 (8) ◽  
pp. 1473-1477 ◽  
Author(s):  
Nico Holmstock ◽  
Pieter Annaert ◽  
Patrick Augustijns
Keyword(s):  
Cytochrome P450 ◽  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Relative Role ◽  
P Glycoprotein ◽  
In Situ Intestinal Perfusion ◽  
Glycoprotein Inhibition

Comparative Effects on Intestinal Absorption in Situ by P-glycoprotein-Modifying HIV Protease Inhibitors

2004 ◽  
Vol 21 (10) ◽  
pp. 1862-1866 ◽  
Author(s):  
Martin Richter ◽  
Nóra Gyémánt ◽  
Joséf Molnár ◽  
Andreas Hilgeroth
Keyword(s):  
Intestinal Absorption ◽  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
P Glycoprotein

Changes in Pharmacokinetics of Anti-HIV Protease Inhibitors during Pregnancy: The Role of CYP3A and P-glycoprotein

2005 ◽  
Vol 316 (3) ◽  
pp. 1202-1209 ◽  
Author(s):  
Anita A. Mathias ◽  
Lillian Maggio-Price ◽  
Yurong Lai ◽  
Anshul Gupta ◽  
Jashvant D. Unadkat
Keyword(s):  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
P Glycoprotein ◽  
Anti Hiv

Significance of P-glycoprotein for the pharmacology and clinical use of HIV protease inhibitors

AIDS ◽  
2000 ◽  
Vol 14 (3) ◽  
pp. 235-236 ◽  
Author(s):  
P. Clayette ◽  
S. Jorajuria ◽  
D. Dormont
Keyword(s):  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Clinical Use ◽  
P Glycoprotein

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.

scholarly journals Brain injury caused by HIV protease inhibitors: Role of lipodystrophy and insulin resistance

2012 ◽  
Vol 95 (1) ◽  
pp. 19-29 ◽  
Author(s):  
Sunita Gupta ◽  
Alecia G. Knight ◽  
Boriss Y. Losso ◽  
Donald K. Ingram ◽  
Jeffrey N. Keller ◽  
...  
Keyword(s):  
Insulin Resistance ◽  
Brain Injury ◽  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors

Significance of P-glycoprotein for the pharmacology and clinical use of HIV protease inhibitors

AIDS ◽  
2000 ◽  
Vol 14 (3) ◽  
pp. 237-242 ◽  
Author(s):  
Maarten T. Huisman ◽  
Johan W. Smit ◽  
Alfred H. Schinkel
Keyword(s):  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Clinical Use ◽  
P Glycoprotein
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