Abstract
The highly active antiretroviral therapy (HAART) can cause a metabolic syndrome consisting of lipodystropy/lipoatrophy, dyslipidemia, and type 2 diabetes mellitus with an increased cardiovascular risk. The pathogenetic bases of HAART-associated lipodystrophy are poorly known. A genetic screen was used to evaluate proteins that are modulated in HIV-1-infected patients with or without lipodystrophy syndrome, that are routinely treated with HAART regimens. The most significant modulation was represented by FAP48 expression. Stable over-expression of FAP48 was able to alter, in vitro, adipogenesis, acting both on calcineurin and glucocorticoid pathways. Finally, we demonstrated that FAP48 over-expression was able to influence the capacity of some HIV drugs, Saquinavir and Efavirenz, but not Stavudine, Amprenavir, and Indinavir to inhibit adipocyte formation. In conclusion, this molecule could be a potential target for novel therapeutic approaches to the HAART related lipodystrophy in HIV patients.
Copyright © 2012 Wiley Periodicals, Inc.
MeSH terms
-
Adaptor Proteins, Signal Transducing / genetics
-
Adaptor Proteins, Signal Transducing / metabolism*
-
Adipocytes / drug effects*
-
Adipocytes / metabolism
-
Adipocytes / pathology
-
Alkynes
-
Animals
-
Antiretroviral Therapy, Highly Active / adverse effects
-
Benzoxazines / adverse effects
-
Benzoxazines / pharmacology
-
Calcineurin / genetics
-
Calcineurin / metabolism
-
Carbamates / adverse effects
-
Carbamates / pharmacology
-
Cell Differentiation / drug effects
-
Cell Line
-
Cyclopropanes
-
Furans
-
Gene Expression / drug effects
-
Glucocorticoids / metabolism
-
HIV-1 / drug effects
-
HIV-1 / physiology
-
HIV-Associated Lipodystrophy Syndrome / chemically induced
-
HIV-Associated Lipodystrophy Syndrome / metabolism*
-
Humans
-
Indinavir / adverse effects
-
Indinavir / pharmacology
-
Mice
-
Saquinavir / adverse effects
-
Saquinavir / pharmacology
-
Signal Transduction / drug effects
-
Stavudine / adverse effects
-
Stavudine / pharmacology
-
Sulfonamides / adverse effects
-
Sulfonamides / pharmacology
-
Transfection
Substances
-
Adaptor Proteins, Signal Transducing
-
Alkynes
-
Benzoxazines
-
Carbamates
-
Cyclopropanes
-
Furans
-
GLMN protein, human
-
Glucocorticoids
-
Sulfonamides
-
amprenavir
-
Indinavir
-
Stavudine
-
Calcineurin
-
efavirenz
-
Saquinavir