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Sustained Inhibition of Proton-Coupled Folate Transporter by Myricetin

Drug Metabolism and Pharmacokinetics, 2015
Myricetin is a flavonoid that has recently been suggested to interfere with the intestinal folate transport system. To examine that possibility, focusing on its sustained inhibitory effect on proton-coupled folate transporter (PCFT), the uptake of folate was examined in Caco-2 cells, in which PCFT is known to be in operation, in the absence of ...
Hiroaki Yuasa   +2 more
exaly   +3 more sources

Functional role of serine 318 of the proton-coupled folate transporter in methotrexate transport

Drug Metabolism and Pharmacokinetics, 2021
This study revealed the importance of serine 318 (S318) residue for proton-coupled folate transporter (PCFT, SLC46A1) functioning. Substitution of S318 with arginine or lysine impaired transport of methotrexate (MTX), but substitution with alanine (has a simple side chain structure), or cysteine (structurally similar to serine), had no significant ...
Tomoya, Narawa   +3 more
openaire   +2 more sources

Specific Inhibitory Effects of Myricetin on Human Proton-Coupled Folate Transporter: Comparison With Its Effects on Rat Proton-Coupled Folate Transporter and Human Riboflavin Transporter 3

Drug Metabolism and Pharmacokinetics, 2017
Myricetin is a flavonoid that inhibits human proton-coupled folate transporter (hPCFT) in a transient manner, in which inhibition is manifested in its presence, and also in a sustained manner, in which inhibition induced in its presence persists after its removal.
Hiroaki Yuasa   +2 more
exaly   +3 more sources

Cell-Free Expression of Proton-Coupled Folate Transporter in the Presence of Nanodiscs

2022
Proton coupled folate transporter (PCFT) is an integral membrane protein with 12 transmembrane segments localized to the plasma membrane. PCFT is the main route by which folate, vitamin B9, from dietary sources enters mammalian cells in the small intestine.
Hoa Quynh, Do, Michaela, Jansen
openaire   +2 more sources

Kinetic and Time-Dependent Features of Sustained Inhibitory Effect of Myricetin on Folate Transport by Proton-Coupled Folate Transporter

Drug Metabolism and Pharmacokinetics, 2015
Myricetin is a flavonoid that has recently been suggested to induce sustained inhibition of proton-coupled folate transporter (PCFT/SLC46A1), which operates for intestinal folate uptake. The present study was conducted to characterize the inhibitory effect in more detail, using human PCFT stably expressed in Madin-Darby canine kidney II cells, to gain ...
Hiroaki Yuasa   +2 more
exaly   +3 more sources

Functional elements in the minimal promoter of the human proton-coupled folate transporter

Biochemical and Biophysical Research Communications, 2009
The proton-coupled folate transporter (PCFT) is the dominant intestinal folate transporter, however, its promoter has yet to be revealed. Hence, we here cloned a 3.1kb fragment upstream to the first ATG of the human PCFT gene and generated sequential deletion constructs evaluated in luciferase reporter assay.
Michal, Stark   +2 more
openaire   +2 more sources

Vitamin D is not linked to folate status and mRNA expression of intestinal proton-coupled folate transporter

European Journal of Nutrition, 2013
In vitro studies discovered intestinal proton-coupled folate transporter (PCFT) as a vitamin D hormone-responsive gene. In vivo effects of vitamin D on PCFT and folate status are currently not available.Three experiments were conducted. At first, vitamin D receptor knockout (VDR(-/-)) mice and corresponding wild-type (WT) mice were compared for their ...
C, Brandsch   +7 more
openaire   +2 more sources

502 Increased Folate Transport During Folate Deficiency Is Associated with Upregulation of Reduced Folate Carrier and Proton Coupled Folate Transporter in Rat Intestine

Gastroenterology, 2009
G A A b st ra ct s HIF-1α signaling in response to Cdif toxin. Results: Caco-2 cells exposed to Cdif toxin displayed a significant increase in HIF-1α transcription, protein levels and DNA binding. Cdif toxin-induced HIF-1α protein accumulation was attenuated by nitric oxide synthase inhibitors.
Nissar Ahmad Wani, Jyotdeep Kaur
openaire   +1 more source

The human proton-coupled folate transporter (hPCFT): modulation of intestinal expression and function by drugs

American Journal of Physiology-Gastrointestinal and Liver Physiology, 2010
Folic acid is a vitamin essential for thymidylate and purine synthesis. The human proton-coupled folate transporter (hPCFT) has recently been identified as a pH-dependent folic acid transporter, and mutations in this transporter have been linked to hereditary folic acid malabsorption.
Bradley L, Urquhart   +5 more
openaire   +2 more sources

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