scholarly journals Aspartic Proteases ofPlasmodium falciparumas the Target of HIV‐1 Protease Inhibitors

2005 ◽  
Vol 191 (8) ◽  
pp. 1381-1382 ◽  
Author(s):  
Andrea Savarino ◽  
Roberto Cauda ◽  
Antonio Cassone
Keyword(s):  
Protease Inhibitors ◽  
Aspartic Proteases ◽  
Hiv 1

scholarly journals Antimalarial Activity of Human Immunodeficiency Virus Type 1 Protease Inhibitors

2005 ◽  
Vol 49 (7) ◽  
pp. 2983-2985 ◽  
Author(s):  
Sunil Parikh ◽  
Jiri Gut ◽  
Eva Istvan ◽  
Daniel E. Goldberg ◽  
Diane V. Havlir ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitors ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Antimalarial Activity ◽  
Aspartic Proteases ◽  
Immunodeficiency Virus ◽  
Plasmepsin Ii ◽  
Hiv 1

ABSTRACT Aspartic proteases play key roles in the biology of malaria parasites and human immunodeficiency virus type 1 (HIV-1). We tested the activity of seven HIV-1 protease inhibitors against cultured Plasmodium falciparum. All compounds inhibited the development of parasites at pharmacologically relevant concentrations. The most potent compound, lopinavir, was active against parasites (50% inhibitory concentration [IC50], 0.9 to 2.1 μM) at concentrations well below those achieved by ritonavir-boosted lopinavir therapy. Lopinavir also inhibited the P. falciparum aspartic protease plasmepsin II at a similar concentration (IC50, 2.7 μM). These findings suggest that use of HIV-1 protease inhibitors may offer clinically relevant antimalarial activity.

An oral high dose of cholecalciferol restores vitamin D status in deficient postmenopausal HIV-1 infected women independently of protease inhibitors therapy

2015 ◽  
Author(s):  
Jessica Pepe ◽  
Ivano Mezzaroma ◽  
Alessandra Fantauzzi ◽  
Mario Falciano ◽  
Alessandra Salotti ◽  
...  
Keyword(s):  
Vitamin D ◽  
Protease Inhibitors ◽  
High Dose ◽  
Vitamin D Status ◽  
Hiv 1

A convergent synthesis of the spiroketal moiety of the HIV-1 protease inhibitors didemnaketals

Tetrahedron ◽  
2002 ◽  
Vol 58 (9) ◽  
pp. 1697-1708 ◽  
Author(s):  
Yan Xing Jia ◽  
Xin Li ◽  
Bin Wu ◽  
Xue Zhi Zhao ◽  
Yong Qiang Tu
Keyword(s):  
Protease Inhibitors ◽  
Convergent Synthesis ◽  
Hiv 1

scholarly journals Substrate Envelope-Designed Potent HIV-1 Protease Inhibitors to Avoid Drug Resistance

2013 ◽  
Vol 20 (9) ◽  
pp. 1116-1124 ◽  
Author(s):  
Madhavi N.L. Nalam ◽  
Akbar Ali ◽  
G.S. Kiran Kumar Reddy ◽  
Hong Cao ◽  
Saima G. Anjum ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Protease Inhibitors ◽  
Hiv 1 ◽  
Substrate Envelope

Design and Evaluation of Novel Piperidine HIV-1 Protease Inhibitors with Potency against DRV-resistant Variants

2021 ◽  
pp. 113450
Author(s):  
Mei Zhu ◽  
Huiyu Zhou ◽  
Ling Ma ◽  
Biao Dong ◽  
Jinming Zhou ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Hiv 1

ChemInform Abstract: HIV-1 Protease Inhibitors Based on Acyclic Carbohydrates.

ChemInform ◽  
2010 ◽  
Vol 29 (49) ◽  
pp. no-no
Author(s):  
B. SAMUELSSON ◽  
ET AL. ET AL.
Keyword(s):  
Protease Inhibitors ◽  
Hiv 1

scholarly journals Major drug resistance mutations to HIV-1 protease inhibitors (PI) among patients exposed to PI class failing antiretroviral therapy in São Paulo State, Brazil

PLoS ONE ◽  
2019 ◽  
Vol 14 (10) ◽  
pp. e0223210
Author(s):  
Giselle de Faria Romero Soldi ◽  
Isadora Coutinho Ribeiro ◽  
Cintia Mayumi Ahagon ◽  
Luana Portes Ozório Coelho ◽  
Gabriela Bastos Cabral ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Antiretroviral Therapy ◽  
Protease Inhibitors ◽  
Sao Paulo ◽  
Resistance Mutations ◽  
Paulo State ◽  
Drug Resistance Mutations ◽  
São Paulo State ◽  
Major Drug ◽  
Hiv 1

scholarly journals Novel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants

2020 ◽  
Vol 11 (6) ◽  
pp. 1196-1204
Author(s):  
Mei Zhu ◽  
Yue Dou ◽  
Ling Ma ◽  
Biao Dong ◽  
Fan Zhang ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Hiv 1 ◽  
Enhance Activity

scholarly journals Multiple Mutations in the Human Immunodeficiency Virus Protease Gene Are Responsible for Decreased Susceptibility to Protease Inhibitors

1995 ◽  
Vol 6 (2) ◽  
pp. 80-88 ◽  
Author(s):  
R. W. King ◽  
S. Garber ◽  
D. L. Winslow ◽  
C. Reid ◽  
L. T. Bacheler ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitors ◽  
Clinical Isolate ◽  
Protease Gene ◽  
Human Immunodeficiency Virus Protease ◽  
Fold Reduction ◽  
Antiretroviral Drug ◽  
Immunodeficiency Virus ◽  
Hiv 1

The protease (PR) of the human immunodeficiency virus (HIV) is essential for replication of the virus, and accordingly has become an attractive target for the development of an antiretroviral drug. We have previously reported that passage of HIV-1 in the presence of increasing concentrations of the C-2 symmetrical, linear diol P9941 resulted in the isolation of virus with a valine-to-alanine change at position 82 (V82A) of the PR, and reduced sensitivity to certain PR inhibitors. In this study, we passaged four different variants of HIV-1 in increasing concentrations of XM323, and isolated variants with reduced sensitivity to inhibitors of PR. Twenty-three passages of HIV-1 (RF) in the presence of XM323 resulted in a variant that exhibited an approximately 100-fold reduction in susceptibility to XM323 and that contained V82F and I84V changes. When two other viruses, HIV-1 (RF41D2) and HIV-1(RF41E4), previously derived from HIV-1 (RF) by passage in the presence of P9941, were passaged in the presence of XM323, variants with V82A/L97V and M46L/V82A/L97V changes, respectively, were obtained. The M46L/V82A/L97V variant showed a 6-fold reduction in sensitivity to XM323, whereas the susceptibility of the V82A/L97V mutant remained unchanged. Seventeen passages of a clinical isolate of HIV-1, HIV-1 (Pat.E), in the presence of XM323 produced a V82F/L97V mutant with an approximately 9-fold reduction in sensitivity to XM323.

scholarly journals A randomized trial of therapeutic drug monitoring of protease inhibitors in antiretroviral-experienced, HIV-1-infected patients

AIDS ◽  
2009 ◽  
Vol 23 (3) ◽  
pp. 357-368 ◽  
Author(s):  
Lisa M Demeter ◽  
Hongyu Jiang ◽  
A Lisa Mukherjee ◽  
Gene D Morse ◽  
Robin DiFrancesco ◽  
...  
Keyword(s):  
Therapeutic Drug Monitoring ◽  
Randomized Trial ◽  
Protease Inhibitors ◽  
Drug Monitoring ◽  
Therapeutic Drug ◽  
Hiv 1
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