Endoplasmic Reticulum Stress Links Dyslipidemia to Inhibition of Proteasome Activity and Glucose Transport by HIV Protease Inhibitors

2005 ◽  
Vol 67 (6) ◽  
pp. 1909-1919 ◽  
Author(s):  
Rex A. Parker ◽  
Oliver P. Flint ◽  
Ruth Mulvey ◽  
Carolina Elosua ◽  
Faye Wang ◽  
...  
Keyword(s):  
Endoplasmic Reticulum ◽  
Endoplasmic Reticulum Stress ◽  
Protease Inhibitors ◽  
Glucose Transport ◽  
Proteasome Activity ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors

scholarly journals The HIV protease inhibitor saquinavir impairs lipid metabolism and glucose transport in cultured adipocytes

2002 ◽  
Vol 172 (1) ◽  
pp. 155-162 ◽  
Author(s):  
S Ranganathan ◽  
PA Kern
Keyword(s):  
Lipid Metabolism ◽  
Glucose Metabolism ◽  
Protease Inhibitors ◽  
Glucose Transport ◽  
Inhibitory Effect ◽  
Cellular Protein ◽  
Hiv Protease ◽  
Hiv Protease Inhibitors ◽  
Direct Effects ◽  
Related Drug

Treatment of HIV infection using protease inhibitors is frequently associated with lipodystrophy and impaired lipid and glucose metabolism. We examined the effect of saquinavir, one of the protease inhibitors, on lipid metabolism and glucose transport in cultured adipocytes. Saquinavir inhibited lipoprotein lipase (LPL) activity in 3T3-F442A and 3T3-L1 adipocytes. The inhibition of LPL was 81% at a concentration of 20 microg/ml. Another closely related drug, indinavir, had a small inhibitory effect. Saquinavir also inhibited the biosynthesis of lipids from [(14)C]-acetate. Saquinavir increased the lipolysis. Saquinavir had no significant effect on the cellular protein synthesis or protein content. Saquinavir increased the basal glucose transport threefold and decreased insulin-stimulated glucose transport by 35%. These studies suggest that some HIV protease inhibitors have direct effects on lipid and glucose metabolism. This inhibition of lipogenesis and glucose transport may explain some of the lipodystrophy, dyslipidemia and disturbed glucose metabolism with the clinical use of these drugs.

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
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