Lopinavir-NO, a nitric oxide-releasing HIV protease inhibitor, suppresses the growth of melanoma cells in vitro and in vivo

2019 ◽  
Vol 37 (5) ◽  
pp. 1014-1028 ◽  
Author(s):  
Svetlana Paskas ◽  
Emanuela Mazzon ◽  
Maria Sofia Basile ◽  
Eugenio Cavalli ◽  
Yousef Al-Abed ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Protease Inhibitor ◽  
Melanoma Cells ◽  
Hiv Protease ◽  
Hiv Protease Inhibitor ◽  
Nitric Oxide Releasing

In vitro and in vivo prevention of HIV protease inhibitor-induced insulin resistance by a novel small molecule insulin receptor activator

2004 ◽  
Vol 92 (6) ◽  
pp. 1234-1245 ◽  
Author(s):  
Mingshan Cheng ◽  
Seiyu Chen ◽  
Steven R. Schow ◽  
Vara Prasad Manchem ◽  
Wayne R. Spevak ◽  
...  
Keyword(s):  
Insulin Resistance ◽  
Protease Inhibitor ◽  
Insulin Receptor ◽  
Small Molecule ◽  
Hiv Protease ◽  
Hiv Protease Inhibitor ◽  
Receptor Activator ◽  
Prevention Of Hiv

scholarly journals Pharmacokinetic interactions between 20(S)-ginsenoside Rh2 and the HIV protease inhibitor ritonavir in vitro and in vivo

2013 ◽  
Vol 34 (10) ◽  
pp. 1349-1358 ◽  
Author(s):  
Jian Shi ◽  
Bei Cao ◽  
Wei-bin Zha ◽  
Xiao-lan Wu ◽  
Lin-sheng Liu ◽  
...  
Keyword(s):  
Protease Inhibitor ◽  
Hiv Protease ◽  
Ginsenoside Rh2 ◽  
Hiv Protease Inhibitor ◽  
Pharmacokinetic Interactions

scholarly journals 536 In vitro and in vivo efficacy of nitric oxide-releasing antiviral therapeutic agents

2016 ◽  
Vol 136 (5) ◽  
pp. S95
Author(s):  
K.A. McHale ◽  
K. Balogh ◽  
H. Wang ◽  
S. Hollenbach ◽  
N. Christensen ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Therapeutic Agents ◽  
In Vivo Efficacy ◽  
Nitric Oxide Releasing

scholarly journals ABT-378, a Highly Potent Inhibitor of the Human Immunodeficiency Virus Protease

1998 ◽  
Vol 42 (12) ◽  
pp. 3218-3224 ◽  
Author(s):  
Hing L. Sham ◽  
Dale J. Kempf ◽  
Akhteruzammen Molla ◽  
Kennan C. Marsh ◽  
Gondi N. Kumar ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitor ◽  
Response To Therapy ◽  
Hiv Protease ◽  
Healthy Human ◽  
Human Volunteers ◽  
Immunodeficiency Virus ◽  
Potent Protease Inhibitor

ABSTRACT The valine at position 82 (Val 82) in the active site of the human immunodeficiency virus (HIV) protease mutates in response to therapy with the protease inhibitor ritonavir. By using the X-ray crystal structure of the complex of HIV protease and ritonavir, the potent protease inhibitor ABT-378, which has a diminished interaction with Val 82, was designed. ABT-378 potently inhibited wild-type and mutant HIV protease (Ki = 1.3 to 3.6 pM), blocked the replication of laboratory and clinical strains of HIV type 1 (50% effective concentration [EC50], 0.006 to 0.017 μM), and maintained high potency against mutant HIV selected by ritonavir in vivo (EC50, ≤0.06 μM). The metabolism of ABT-378 was strongly inhibited by ritonavir in vitro. Consequently, following concomitant oral administration of ABT-378 and ritonavir, the concentrations of ABT-378 in rat, dog, and monkey plasma exceeded the in vitro antiviral EC50 in the presence of human serum by >50-fold after 8 h. In healthy human volunteers, coadministration of a single 400-mg dose of ABT-378 with 50 mg of ritonavir enhanced the area under the concentration curve of ABT-378 in plasma by 77-fold over that observed after dosing with ABT-378 alone, and mean concentrations of ABT-378 exceeded the EC50 for >24 h. These results demonstrate the potential utility of ABT-378 as a therapeutic intervention against AIDS.

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
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