A novel FRET-based screen in high-throughput format to identify inhibitors of malarial and human glucose transporters [PDF]
, 2016 The glucose transporter PfHT is essential to the survival of the malaria parasite Plasmodium falciparum and has been shown to be a druggable target with high potential for pharmacological intervention.
Autry, Joseph M +9 more
core +2 more sources
An update on placental drug transport and its relevance to fetal drug exposure
Medical Review, 2022 Pregnant women are often complicated with diseases that require treatment with medication. Most drugs administered to pregnant women are off-label without the necessary dose, efficacy, and safety information. Knowledge concerning drug transfer across the
Mao Qingcheng, Chen Xin
doaj +1 more source
Unique metabolite preferences of the drug transporters OAT1 and OAT3 analyzed by machine learning
Journal of Biological Chemistry, 2020 The multispecific organic anion transporters, OAT1 (SLC22A6) and OAT3 (SLC22A8), the main kidney elimination pathways for many common drugs, are often considered to have largely-redundant roles.
Anisha K. Nigam +7 more
semanticscholar +1 more source
Lesinurad, a novel, oral compound for gout, acts to decrease serum uric acid through inhibition of urate transporters in the kidney. [PDF]
, 2016 BackgroundExcess body burden of uric acid promotes gout. Diminished renal clearance of uric acid causes hyperuricemia in most patients with gout, and the renal urate transporter (URAT)1 is important for regulation of serum uric acid (sUA) levels.
Girardet, Jean-Luc +12 more
core +2 more sources
Multiple blood-brain barrier transport mechanisms limit bumetanide accumulation, and therapeutic potential, in the mammalian brain [PDF]
, 2017 There is accumulating evidence that bumetanide, which has been used over decades as a potent loop diuretic, also exerts effects on brain disorders, including autism, neonatal seizures, and epilepsy, which are not related to its effects on the kidney but ...
Erker, Thomas +7 more
core +2 more sources
Energetics and Mechanism of Drug Transport Mediated by the Lactococcal Multidrug Transporter LmrP [PDF]
, 1996 The gene encoding the secondary multidrug transporter LmrP of Lactococcus lactis was heterologously expressed in Escherichia coli. The energetics and mechanism of drug extrusion mediated by LmrP were studied in membrane vesicles of E. coli. LmrP-mediated
Bolhuis, Henk, +6 more
core +1 more source
ADMET and DMPK, 2017 It is clear that many drug transporters (both ABCs and SLCs) are present in the human skin. Different in vitro skin models can be used to investigate the role of drug transporters in the skin despite quantitative differences in expression profile across ...
Hanan Osman-Ponchet +3 more
doaj +1 more source
Using cellular fitness to map the structure and function of a major facilitator superfamily effluxer. [PDF]
, 2017 The major facilitator superfamily (MFS) effluxers are prominent mediators of antimicrobial resistance. The biochemical characterization of MFS proteins is hindered by their complex membrane environment that makes in vitro biochemical analysis challenging.
Bennett, Matthew R +5 more
core +2 more sources
Utilizing in vitro transporter data in IVIVE-PBPK: an overview
ADMET and DMPK, 2017 In vitro-in vivo extrapolation (IVIVE) integrated in physiologically-based pharmacokinetic (PBPK) models have been increasingly used during drug discovery and development processes to predict human pharmacokinetic (PK) parameters.
Pankajini Mallick
doaj +1 more source
Advances in Pharmacokinetic Mechanisms of Transporter-Mediated Herb-Drug Interactions
Pharmaceuticals, 2022 As the use of herbs has become more popular worldwide, there are increasing reports of herb-drug interactions (HDIs) following the combination of herbs and drugs. The active components of herbs are complex and have a variety of pharmacological activities,
Jie Li +4 more
doaj +1 more source