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The development of a novel high-throughput membrane potential assay and a solid-supported membrane (SSM)-based electrophysiological assay to study the pharmacological inhibition of GLUT9/SLC2A9 isoforms in a drug discovery program.
SLAS Discov
December 2024
Sanofi, Integrated Drug Discovery, Industriepark Hoechst, Frankfurt am Main, Germany. Electronic address:
GLUT9/SLC2A9 is a urate transporter and takes a fundamental role in the maintenance of normal serum urate levels. GLUT9 is the sole transporter of reabsorbed urate from renal epithelial cells to blood, thus making it an ideal pharmacological target for the development of urate-lowering drugs. None of the three currently available assays for studying GLUT9 pharmacological inhibition can support a high throughput drug discovery screening campaign.
View Article and Find Full Text PDFExploring the Interaction of Lipid Bilayers with Curcumin-Laponite Nanoparticles: Implications for Drug Delivery and Therapeutic Applications.
Small
December 2024
Centro de Física de Materiales (CFM) (CSIC-UPV/EHU) - Materials Physics Center (MPC), Paseo Manuel de Lardizabal 5, San Sebastián, 20018, Spain.
Article Synopsis
- Curcumin, found in turmeric, has strong anti-inflammatory, antioxidant, and antimicrobial properties that could help treat conditions like arthritis and cancer, but its effectiveness is hindered by poor bioavailability.
- Recent research is exploring ways to enhance curcumin delivery using advanced materials like nanoparticles and liposomes, with a focus on laponite, a synthetic nanoclay that improves curcumin's stability and delivery due to its unique properties.
- This study investigates how curcumin-laponite nanoparticles can effectively deliver curcumin to cell membranes, using various high-tech methods to monitor their interaction, ultimately aiming to develop targeted therapies for diseases such as cardiovascular issues, neurological disorders, and cancer.
Transport mechanism of DgoT, a bacterial homolog of SLC17 organic anion transporters.
EMBO J
December 2024
Institute of Biological Information Processing (IBI-1), Molekular- und Zellphysiologie, Forschungszentrum Jülich, 52425, Jülich, Germany.
The solute carrier 17 (SLC17) family contains anion transporters that accumulate neurotransmitters in secretory vesicles, remove carboxylated monosaccharides from lysosomes, or extrude organic anions from the kidneys and liver. We combined classical molecular dynamics simulations, Markov state modeling and hybrid first principles quantum mechanical/classical mechanical (QM/MM) simulations with experimental approaches to describe the transport mechanisms of a model bacterial protein, the D-galactonate transporter DgoT, at atomic resolution. We found that protonation of D46 and E133 precedes galactonate binding and that substrate binding induces closure of the extracellular gate, with the conserved R47 coupling substrate binding to transmembrane helix movement.
View Article and Find Full Text PDFSubstrate dependence of transport coupling and phenotype of a small multidrug resistance transporter in .
J Bacteriol
October 2024
Department of Biochemistry, University of Wisconsin-Madison, Madison, Wisconsin, USA.
Unlabelled: Small multidrug resistance (SMR) transporters are key players in the defense of multidrug-resistant pathogens to toxins and other homeostasis-perturbing compounds. However, recent evidence demonstrates that EmrE, an SMR from and a model for understanding transport, can also induce susceptibility to some compounds by drug-gated proton leak. This runs down the ∆pH component of the proton-motive force (PMF), reducing the viability of the affected bacteria.
View Article and Find Full Text PDF[Determination of ten bisphenols and five parabens in urine by solid supported liquid-liquid extraction and liquid chromatography-tandem mass spectrometry].
Se Pu
September 2024
State Key Laboratory of Organic Geochemistry, Guangdong Provincial Key Laboratory of Environmental Protection and Resources Utilization, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, Guangzhou 510640, China.
Article Synopsis
- * The study developed a new procedure using solid supported liquid-liquid extraction (SLE) to effectively separate and analyze ten BPs and five PBs in urine through high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS).
- * The method involved optimizing extraction conditions and using a specific pH adjustment, enzyme digestion, and a particular elution solvent mix to accurately quantify the target chemicals in urine samples.
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