HIV protease inhibitors block human preadipocyte differentiation, but not via the PPARgamma/RXR heterodimer

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HIV protease inhibitors block human preadipocyte differentiation, but not via the PPARgamma/RXR heterodimer.

A recent prospective clinical study has shown that antiviral therapy with HIV protease inhibitors (PIs) is associated with a syndrome of peripheral fat wasting (lipodystrophy) and disordered glucose and lipid metabolism (Carr et al. 1999). We have studied the effects of indinavir and saquinavir, two HIV protease inhibitors, on cultured primary human preadipocytes and report that these compounds...

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HIV protease inhibitors are inhibitors but not substrates of the human breast cancer resistance protein (BCRP/ABCG2).

Breast cancer resistance protein (BCRP) is a recently discovered ATP-binding cassette drug transporter. Hence, the full spectrum of therapeutic agents that interact with BCRP remains to be elucidated. Because human immunodeficiency virus protease inhibitors (HPIs) are well known P-glycoprotein (P-gp) substrates, and there is an overlap in substrate specificity between P-gp and BCRP, this study ...

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HIV protease inhibitors block adipogenesis and increase lipolysis in vitro.

AIDS therapies employing HIV protease inhibitors (PIs) are associated with changes in fat metabolism. However, the cellular mechanisms affected by PIs are not clear. Thus, the affects of PIs on adipocyte differentiation were examined in vitro using C3H10T1/2 stem cells. In these cells the PIs, nelfinavir, saquinavir, and ritonavir, reduced triglyceride accumulation, lipogenesis, and expression ...

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Screening Efficacy of Available HIV Protease Inhibitors on COVID-19 Protease

Background and Aim: Advent of COVID-19 attracted the attentions of researchers to develop drugs for its treatment. Besides efforts on developing new drugs, screening available drugs for efficacy on COVID-19 could be an urgent action of initiating its pharmacotherapy. In this study, efficacy of HIV protease inhibitors on COVID-19 protease has been examined. Methods: Molecular docking based scree...

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HIV-1 protease inhibitors.

Treatment of human immunodeficiency virus type 1 (HIV-1) infection with regimens that include protease inhibitors (PIs) has contributed to marked improvements in HIV-related disease progression and mortality. Five PIs are approved by the US Food and Drug Administration and have potent activity in vitro. PIs with 2 nucleoside analogue reverse transcriptase inhibitors have demonstrated prolonged ...

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ژورنال

عنوان ژورنال: Journal of Endocrinology

سال: 2000

ISSN: 0022-0795,1479-6805

DOI: 10.1677/joe.0.164r007