Drug Transport in the Liver

Sjöstedt, Noora; Adiwidjaja, Jeffry; Murphy, William A.; Brouwer, Kim L.R.

doi:10.1002/9781119739883.ch13

Cited by 1 publication

(1 citation statement)

References 191 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In the basolateral (sinusoidal) membrane function, uptake carriers are from OATP family, i.e., organic anion transporting polypeptide 1B1 (OATP1B1 and SLCO1B1), OATP1B3 (SLCO1B3), and OATP2B1 (SLCO2B1), as well as SLC22A family, i.e., organic cation transporter 1 (OCT1 and SLC22A1) and organic anion transporter OAT2 (SLC22A7). The basolateral membrane is also endowed with efflux transporters, such as MRP3 (ABCC3), MRP4 (ABCC4), and MRP6 (ABCC6) [ 4 ].…”

Section: Introductionmentioning

confidence: 99%

Protein Abundance of Drug Transporters in Human Hepatitis C Livers

Droździk

Łapczuk-Romańska

Wenzel

et al. 2022

IJMS

View full text Add to dashboard Cite

Transmembrane drug transport in hepatocytes is one of the major determinants of drug pharmacokinetics. In the present study, ABC transporters (P-gp, MRP1, MRP2, MRP3, MRP4, BCRP, and BSEP) and SLC transporters (MCT1, NTCP, OAT2, OATP1B1, OATP1B3, OATP2B1, OCT1, and OCT3) were quantified for protein abundance (LC-MS/MS) and mRNA levels (qRT-PCR) in hepatitis C virus (HCV)-infected liver samples from the Child–Pugh class A (n = 30), B (n = 21), and C (n = 7) patients. Protein levels of BSEP, MRP3, MCT1, OAT2, OATP1B3, and OCT3 were not significantly affected by HCV infection. P-gp, MRP1, BCRP, and OATP1B3 protein abundances were upregulated, whereas those of MRP2, MRP4, NTCP, OATP2B1, and OCT1 were downregulated in all HCV samples. The observed changes started to be seen in the Child–Pugh class A livers, i.e., upregulation of P-gp and MRP1 and downregulation of MRP2, MRP4, BCRP, and OATP1B3. In the case of NTCP, OATP2B1, and OCT1, a decrease in the protein levels was observed in the class B livers. In the class C livers, no other changes were noted than those in the class A and B patients. The results of the study demonstrate that drug transporter protein abundances are affected by the functional state of the liver in hepatitis C patients.

show abstract

Section: Introductionmentioning

confidence: 99%