scholarly journals HIV protease inhibitors and onset of cardiovascular diseases: A central role for oxidative stress and dysregulation of the ubiquitin–proteasome system

2014 ◽  
Vol 1842 (2) ◽  
pp. 256-268 ◽  
Author(s):  
Kathleen M.S.E. Reyskens ◽  
M. Faadiel Essop
Keyword(s):  
Oxidative Stress ◽  
Cardiovascular Diseases ◽  
Protease Inhibitors ◽  
Ubiquitin Proteasome System ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Ubiquitin Proteasome

scholarly journals HIV Protease Inhibitors Apoptotic Effect in SH-SY5Y Neuronal Cell Line

2016 ◽  
Vol 39 (4) ◽  
pp. 1463-1470 ◽  
Author(s):  
Paola Maura Tricarico ◽  
Rafael Freitas de Oliveira Franca ◽  
Sabrina Pacor ◽  
Valentina Ceglia ◽  
Sergio Crovella ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Cell Line ◽  
Protease Inhibitors ◽  
Heme Oxygenase ◽  
Neuroblastoma Cell ◽  
Neuroblastoma Cell Line ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Cellular Models ◽  
The Impact

Background: Prophylactic treatment regimens to prevent mother-to-child HIV transmission include protease inhibitors Lopinavir and Ritonavir. Lopinavir and Ritonavir have been reported to be able to induce intracellular oxidative stress in diverse cellular models, however scarce informations are available about protease inhibitor effects of in the central nervous system (CNS). In our study we evaluated the impact of protease inhibitors on a cell neuronal model. Methods: We treated a neuroblastoma cell line (SH-SY5Y) with increasing doses of Lopinavir and Ritonavir (0.1-1-10-25-50 µM), used alone or in combination, evaluating the impact of these drugs in terms of mitochondrial activity, with MTT cell proliferation assay; mRNA expression of heme oxygenase (HemeOH) and reactive oxygen species (ROS) levels with 2',7'-dichlorofluorescin diacetate (H2DCFDA) in order to assess oxidative stress; apoptotic cell death with flow cytometry. Results: We observed that Lopinavir and Ritonavir treatment, at 25 and/or 50 µM concentrations, induced mitochondrial damage, increase of heme oxygenase RNA expression levels and ROS generation, followed by apoptosis in SH-SY5Y. Conclusions: Our in vitro model demonstrates a damaging effect of HIV protease inhibitors on the neuroblastoma cell line, thus partially mimicking the impact of these drugs on the CNS of children born to HIV positive mothers undergone to antiretroviral treatment.

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

Aminodiol HIV protease inhibitors. 2. 1,1-Dimethyl-2-hydroxyethyl carbamate derivatives with enhanced potency

1995 ◽  
Vol 5 (5) ◽  
pp. 459-464 ◽  
Author(s):  
G.S. Bisacchi ◽  
S. Ahmad ◽  
M. Alam ◽  
A. Ashfaq ◽  
J. Barrish ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors

Evaluation of furofuran as a P2 ligand for symmetry-based HIV protease inhibitors

1996 ◽  
Vol 6 (23) ◽  
pp. 2847-2852 ◽  
Author(s):  
Xiaoqi Chen ◽  
Lin Li ◽  
Dale J. Kempf ◽  
Hing Sham ◽  
Norman E. Wideburg ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors

scholarly journals Additivity in the Analysis and Design of HIV Protease Inhibitors

2009 ◽  
Vol 52 (3) ◽  
pp. 737-754 ◽  
Author(s):  
Robert N. Jorissen ◽  
G. S. Kiran Kumar Reddy ◽  
Akbar Ali ◽  
Michael D. Altman ◽  
Sripriya Chellappan ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Analysis And Design
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