Open AccessModulation of human BCRP (ABCG2) activity by anti-HIV drugs
Author(s) -
Johanna Weiß,
Jessica Rose,
Caroline Henrike Storch,
Nahal KetabiKiyanvash,
A. Sauer,
Walter E. Haefeli,
Thomas Efferth
Publication year - 2006
Publication title -
journal of antimicrobial chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.124
H-Index - 194
eISSN - 1460-2091
pISSN - 0305-7453
DOI - 10.1093/jac/dkl474
Subject(s) - pharmacology , efavirenz , ritonavir , saquinavir , indinavir , nevirapine , atazanavir , amprenavir , abacavir , abcg2 , lamivudine , nelfinavir , didanosine , emtricitabine , stavudine , zidovudine , atp binding cassette transporter , chemistry , virology , medicine , transporter , viral load , biochemistry , human immunodeficiency virus (hiv) , hiv 1 protease , virus , antiretroviral therapy , hepatitis b virus , gene , protease , enzyme , viral disease
The safety and effectiveness of highly active antiretroviral therapy (HAART) is challenged by viral resistance to antiretrovirals and the frequent occurrence of drug interactions which may limit the access of these drugs to the target sites. In particular, drug distribution and elimination may be modified by active efflux transporters. While P-glycoprotein is well evaluated in this regard, the interaction of antiretrovirals with the ABC transporter BCRP (ABCG2) is far from being elucidated. The aim of this study was therefore to investigate the influence of all important anti-HIV drugs on BCRP activity in vitro in one assay to allow unrestricted comparison of the results.
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