Acyclovir is a substrate for the human breast cancer resistance protein (BCRP/ABCG2): Implications for renal tubular transport and acyclovir-induced nephrotoxicity

Patrina Gunness, Katarina Aleksa, Gideon Koren

פרסום מחקרי: פרסום בכתב עתמאמרביקורת עמיתים

12 ציטוטים ‏(Scopus)

תקציר

The human breast cancer resistance protein (BCRP/ABCG2) is widely expressed in human tissues, including the kidney. In mice, Bcrp1 (murine BCRP ortholog) mediates the transport of acyclovir into breast milk. It is plausible that acyclovir is also a substrate for the human BCRP. The objective of the study was to determine whether acyclovir is a substrate for human BCRP. Transfected human embryonic kidney (HEK293) cells (containing the wild-type ABCG2 gene) were exposed to [8- 14C]acyclovir (1 μmol/L) in the presence or absence of the BCRP inhibitor fumitremorgin C (FTC). Intracellular acyclovir accumulation was assessed using a liquid scintillation counter. Coexposure to FTC resulted in a significant (5- fold) increase in the intracellular accumulation of acyclovir. The results suggest that acyclovir is a substrate for human BCRP. The study is the first to provide direct evidence for the role of human BCRP in acyclovir transport and its potential significance with respect to renal tubular transport of acyclovir and the direct renal tubular insult induced by the drug.

שפה מקוריתאנגלית
עמודים (מ-עד)675-680
מספר עמודים6
כתב עתCanadian Journal of Physiology and Pharmacology
כרך89
מספר גיליון9
מזהי עצם דיגיטלי (DOIs)
סטטוס פרסוםפורסם - ספט׳ 2011
פורסם באופן חיצוניכן

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