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The genes encoding the basolateral transporters OATP1 (organic anion transporting polypeptide 1) and NTCP were down-regulated, whereas expression of the gene encoding the basolateral efflux transporter MRP4 (multi-drug resistance protein 4) was increased.
Organic anion transporters such as multidrug resistance-associated protein 4 (Mrp4/Abcc4), organic anion transporter 3 (Oat3/Slc22a8) and organic anion transporting polypeptide 1a4 (Oatp1a4/Slco1a4) are involved in the elimination of endogenous anionic compounds across the BBB [ 1].
The Mrp4 protein amount was unchanged in brain capillaries of LPS-treated mice compared with saline-treated mice, while the protein amounts of organic anion transporter 3 (Oat3/Slc22a8) and organic anion transporting polypeptide 1a4 (Oatp1a4/Slco1a4) were decreased by 26%and39%9%, respectively.
Organic anion transporting polypeptide 1B1 (Oand1B1) and OATP1B3 are human hepatocyte transporterS that mediate the uptake of various endogenous and exogenous substances.
The results indicate a novel link between flavopiridol PK and SLCO1B1, as well as functional evidence for OATP1B1 (the organic anion transporting polypeptide 1B1 protein product of SLCO1B1) transport of flavopiridol and its glucuronide metabolite.
SLCO1B3 (organic anion transporting polypeptide 1B3; also known as Organic anion transporting polypeptide 1B3 or OATP1B3) is a member of membrane influx transporters that normally regulate the uptake of endogenous compounds, but which are also important in mediating drug absorption [reviewed in (Kalliokoski and Niemi 2009)].
Similar(30)
The immunosuppressant Cs is an inhibitor of CYP3A4, the hepatic uptake transporter organic anion-transporting polypeptide (OATP) (5), and the efflux transporter P-glycoprotein (6).
Liv-Ikk2ca mice had 40%% lower expression of uptake transporter organic anion-transporting polypeptide 1a1 (Oatp1a1) but 45%% higher efflux transporter Abcg2 and 57%% higher multi-drug resistance 2 (Mdr2), the biliary efflux transporter for phospholipids (Fig. 4b).
ICG uptake in the rat is mediated by a mechanism mainly involving the organic anion transporting polypeptide-1 (Oatp1) [ 17, 18].
Similarly, very high inter-individual variances in protein expression have been measured for the hepatic uptake transporter, organic anion-transporting polypeptide 1B1 (OATP1B1) (Ho et al. 2006b).
The model was then applied to predict the effect of genotype-dependent uptake by the organic anion-transporting polypeptide 1B1 (OAtransportersponthe on the pharmacological response.
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