In vitro susceptibility of clinical isolates of HIV-1 to XM323, a non-peptidyl HIV protease inhibitor

AIDS ◽  
1994 ◽  
Vol 8 (6) ◽  
pp. 753-756 ◽  
Author(s):  
Dean L. Winslow ◽  
Douglas Mayers ◽  
Helen Scarnati ◽  
James Lane ◽  
Arlene Bincsik ◽  
...  
Keyword(s):  
Protease Inhibitor ◽  
Clinical Isolates ◽  
Hiv Protease ◽  
Hiv Protease Inhibitor ◽  
In Vitro Susceptibility ◽  
Hiv 1

A C2 Symmetry-Based HIV Protease Inhibitor, A77003, Irreversibly Inhibits Infectivity of HIV-1 In Vitro

1994 ◽  
Vol 10 (6) ◽  
pp. 735-743 ◽  
Author(s):  
SEIJI KAGEYAMA ◽  
DAVID T. HOEKZEMA ◽  
YOHKO MURAKAWA ◽  
EIJI KOJIMA ◽  
TAKUMA SHIRASAKA ◽  
...  
Keyword(s):  
Protease Inhibitor ◽  
Hiv Protease ◽  
Hiv Protease Inhibitor ◽  
Hiv 1

In vitro anti-HIV-1 activity of HIV protease inhibitor KNI-272 in resting and activated cells: implications for its combined use with AZT or ddI

1995 ◽  
Vol 28 (1) ◽  
pp. 25-38 ◽  
Author(s):  
Sudhichai Chokekijchai ◽  
Takuma Shirasaka ◽  
John N. Weinstein ◽  
Hiroaki Mitsuya
Keyword(s):  
Protease Inhibitor ◽  
Hiv Protease ◽  
Hiv Protease Inhibitor ◽  
Combined Use ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals TMC310911, a Novel Human Immunodeficiency Virus Type 1 Protease Inhibitor, ShowsIn Vitroan Improved Resistance Profile and Higher Genetic Barrier to Resistance Compared with Current Protease Inhibitors

2011 ◽  
Vol 55 (12) ◽  
pp. 5723-5731 ◽  
Author(s):  
Inge Dierynck ◽  
Herwig Van Marck ◽  
Marcia Van Ginderen ◽  
Tim H. M. Jonckers ◽  
Madhavi N. L. Nalam ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitor ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Clinical Isolates ◽  
Immunodeficiency Virus ◽  
Hiv 1 ◽  
Selection Of

ABSTRACTTMC310911 is a novel human immunodeficiency virus type 1 (HIV-1) protease inhibitor (PI) structurally closely related to darunavir (DRV) but with improved virological characteristics. TMC310911 has potent activity against wild-type (WT) HIV-1 (median 50% effective concentration [EC50], 14 nM) and a wide spectrum of recombinant HIV-1 clinical isolates, including multiple-PI-resistant strains with decreased susceptibility to currently approved PIs (fold change [FC] in EC50, >10). For a panel of 2,011 recombinant clinical isolates with decreased susceptibility to at least one of the currently approved PIs, the FC in TMC310911 EC50was ≤4 for 82% of isolates and ≤10 for 96% of isolates. The FC in TMC310911 EC50was ≤4 and ≤10 for 72% and 94% of isolates with decreased susceptibility to DRV, respectively.In vitroresistance selection (IVRS) experiments with WT virus and TMC310911 selected for mutations R41G or R41E, but selection of resistant virus required a longer time than IVRS performed with WT virus and DRV. IVRS performed with r13025, a multiple-PI-resistant recombinant clinical isolate, and TMC310911 selected for mutations L10F, I47V, and L90M (FC in TMC310911 EC50= 16). IVRS performed with r13025 in the presence of DRV required less time and resulted in more PI resistance-associated mutations (V32I, I50V, G73S, L76V, and V82I; FC in DRV EC50= 258). The activity against a comprehensive panel of PI-resistant mutants and the limitedin vitroselection of resistant viruses under drug pressure suggest that TMC310911 represents a potential drug candidate for the management of HIV-1 infection for a broad range of patients, including those with multiple PI resistance.

scholarly journals The HIV protease inhibitor, ritonavir, dysregulates human platelet function in vitro

2018 ◽  
Vol 169 ◽  
pp. 96-104 ◽  
Author(s):  
Shannon G. Loelius ◽  
Katie L. Lannan ◽  
Neil Blumberg ◽  
Richard P. Phipps ◽  
Sherry L. Spinelli
Keyword(s):  
Protease Inhibitor ◽  
Platelet Function ◽  
Human Platelet ◽  
Hiv Protease ◽  
Hiv Protease Inhibitor

scholarly journals Modeling Metabolic Effects of the HIV Protease Inhibitor Ritonavir In Vitro

2007 ◽  
Vol 171 (5) ◽  
pp. 1724-1725 ◽  
Author(s):  
Jeffrey Laurence ◽  
Rozbeh Modarresi ◽  
Xinwen Wang ◽  
Qizhi Yao ◽  
Changyi Chen
Keyword(s):  
Protease Inhibitor ◽  
Hiv Protease ◽  
Metabolic Effects ◽  
Hiv Protease Inhibitor

In Vitro Interaction of the HIV Protease Inhibitor Ritonavir with Herbal Constituents: Changes in P-gp and CYP3A4 Activity

2004 ◽  
Vol 11 (4) ◽  
pp. 262-277 ◽  
Author(s):  
Jignesh Patel ◽  
Balasubrahmanyam Buddha ◽  
Surajit Dey ◽  
Dhananjay Pal ◽  
Ashim K Mitra
Keyword(s):  
Protease Inhibitor ◽  
Hiv Protease ◽  
Cyp3a4 Activity ◽  
Hiv Protease Inhibitor ◽  
In Vitro Interaction

scholarly journals In vitro anti-human immunodeficiency virus (HIV) activity of XM323, a novel HIV protease inhibitor.

1993 ◽  
Vol 37 (12) ◽  
pp. 2606-2611 ◽  
Author(s):  
M J Otto ◽  
C D Reid ◽  
S Garber ◽  
P Y Lam ◽  
H Scarnati ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitor ◽  
Hiv Protease ◽  
Hiv Protease Inhibitor ◽  
Immunodeficiency Virus
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