Results 151 to 160 of about 2,031 (173)
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A novel fluorescence‐based functional assay for human OATP1A2 and OATP1C1 identifies interaction between third‐generation P‐gp inhibitors and OATP1A2

The FEBS Journal, 2019
Organic anion‐transporting polypeptide 1A2 (OATP1A2), expressed in the human blood–brain barrier, promotes drug uptake from the blood and hence can be exploited for central nervous system‐targeted drug delivery. The thyroid transporter OATP1C1, expressed in the choroid plexus and in astrocytes, is also a potential pharmacological target. Based on their
Éva Bakos   +6 more
openaire   +3 more sources

Inhibitory Effects of Cranberry Juice and Its Components on Intestinal OATP1A2 and OATP2B1: Identification of Avicularin as a Novel Inhibitor

Journal of Agricultural and Food Chemistry, 2022
Organic anion-transporting polypeptide (OATP) 1A2 and OATP2B1 mediate the intestinal absorption of drugs. This study aimed to identify fruit juices or fruit juice components that inhibit OATPs and assess the risk of associated food-drug interactions. Inhibitory potency was assessed by examining the uptake of [3H]estrone 3-sulfate and [3H]fexofenadine ...
Tokio Morita   +2 more
exaly   +3 more sources

Reabsorption of bile acids regulated by FXR-OATP1A2 is the main factor for the formation of cholesterol gallstone

American Journal of Physiology-Gastrointestinal and Liver Physiology, 2020
For the first time, our results indicate that the axis of farnesoid X receptor-organic anion transporter polypeptide 1A2 that physiologically regulates the reabsorption of bile acids might play an important role in the regulation of the composition of bile acids and make contribution to the development of cholelithiasis.
Jingli Cai   +6 more
openaire   +2 more sources

Molecular cloning and functional characterization of the bovine (Bos taurus) organic anion transporting polypeptide Oatp1a2 (Slco1a2)

Comparative Biochemistry and Physiology Part B: Biochemistry and Molecular Biology, 2004
We describe the cloning, functional characterization and tissue localization of a novel membrane transporter of the OATP/Oatp-gene family obtained from liver and kidney of cattle (Bos taurus). The carrier protein exhibits highest sequence identity to the human OATP1A2 (previously called OATP-A) and is, therefore, named bovine Oatp1a2.
Joachim, Geyer   +3 more
openaire   +2 more sources

Constituents of Passiflora incarnata, but Not of Valeriana officinalis, Interact with the Organic Anion Transporting Polypeptides (OATP)2B1 and OATP1A2

Planta Medica, 2021
AbstractHerbal medication used in the treatment of sleep disorders and anxiety often contain extracts of Valeriana officinalis or Passiflora incarnata. Valerenic acid in V. officinalis and apigenin, orientin, and vitexin in P. incarnata are thought to contribute to their therapeutic effect.
Anima M. Schäfer   +4 more
openaire   +2 more sources

Alteration in placental expression of bile acids transporters OATP1A2, OATP1B1, OATP1B3 in intrahepatic cholestasis of pregnancy

Archives of Gynecology and Obstetrics, 2011
To investigate whether bile acids transporters organic anion transporting polypeptides 1A2 (OATP1A2), organic anion transporting polypeptides 1B1 (OATP1B1), organic anion transporting polypeptides 1B3 (OATP1B3) were differently expressed in placenta of intrahepatic cholestasis of pregnancy (ICP).Thirty pregnant women with ICP were recruited and 30 ...
Huimin, Wang   +5 more
exaly   +3 more sources

Naringin is a Major and Selective Clinical Inhibitor of Organic Anion-Transporting Polypeptide 1A2 (OATP1A2) in Grapefruit Juice

Clinical Pharmacology and Therapeutics, 2007
We showed previously that grapefruit and orange juices inhibited human enteric organic anion-transporting polypeptide (OATP)1A2 in vitro and lowered oral fexofenadine bioavailability clinically. Inhibition of OATP1A2 transport by flavonoids in grapefruit (naringin) and orange (hesperidin) was conducted in vitro.
Richard B Kim
exaly   +3 more sources

Casein Kinase 2 Is a Novel Regulator of the Human Organic Anion Transporting Polypeptide 1A2 (OATP1A2) Trafficking

Molecular Pharmaceutics, 2015
Human organic anion transporting polypeptides (OATPs) mediate the influx of many important drugs into cells. Casein kinase 2 (CK2) is a critical protein kinase that phosphorylates >300 protein substrates and is dysregulated in a number of disease states.
Ting, Chan   +7 more
openaire   +2 more sources

Effects of β-Blockers and Tricyclic Antidepressants on the Activity of Human Organic Anion Transporting Polypeptide 1A2 (OATP1A2)

Journal of Pharmacology and Experimental Therapeutics, 2015
The organic anion transporting polypeptide 1A2 (OATP1A2), a membrane drug transporter expressed on important organs (such as the brain, kidney, and intestine) may be a key element in the disposition of drugs. Previous studies demonstrated that it could transport a broad spectrum of substrates, including endogenous molecules and clinically relevant ...
Veronique Michaud   +1 more
exaly   +3 more sources

Intestinal OATP1A2 inhibition as a potential mechanism for the effect of grapefruit juice on aliskiren pharmacokinetics in healthy subjects

European Journal of Clinical Pharmacology, 2011
To conduct a mechanistic investigation of the interaction between aliskiren and grapefruit juice in healthy subjects.Twenty-eight subjects received an oral dose of aliskiren 300 mg (highest recommended clinical dose) with 300 mL of either water or grapefruit juice in a two-way crossover design. Safety and pharmacokinetic analyses were performed.
Sam, Rebello   +7 more
openaire   +2 more sources

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