Title : Telaprevir is a substrate and moderate inhibitor of P-glycoprotein, a strong inductor of ABCG2, but not an activator of PXR in vitro.

Pub. Date : 2014 Feb

PMID : 24332840






6 Functional Relationships(s)
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1 Telaprevir is a substrate and moderate inhibitor of P-glycoprotein, a strong inductor of ABCG2, but not an activator of PXR in vitro. telaprevir ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
2 The in vitro potency of telaprevir to inhibit P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP, ABCG2) was assessed and its substrate characteristics for P-gp, BCRP and the multidrug resistance-associated proteins (MRPs, ABCCs) 1-3 were evaluated. telaprevir ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
3 The in vitro potency of telaprevir to inhibit P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP, ABCG2) was assessed and its substrate characteristics for P-gp, BCRP and the multidrug resistance-associated proteins (MRPs, ABCCs) 1-3 were evaluated. telaprevir ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
4 The in vitro potency of telaprevir to inhibit P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP, ABCG2) was assessed and its substrate characteristics for P-gp, BCRP and the multidrug resistance-associated proteins (MRPs, ABCCs) 1-3 were evaluated. telaprevir ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
5 The in vitro potency of telaprevir to inhibit P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP, ABCG2) was assessed and its substrate characteristics for P-gp, BCRP and the multidrug resistance-associated proteins (MRPs, ABCCs) 1-3 were evaluated. telaprevir ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens
6 In LS180 cells, telaprevir strongly induced mRNA expression of ABCG2 (4.3-fold at 30 mumol/L) and weakly induced ABCB11, CYP2C19 and UGT1A3. telaprevir ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens