Results 31 to 40 of about 10,907 (165)

Screening Drugs for Broad-Spectrum, Host-Directed Antiviral Activity: Lessons from the Development of Probenecid for COVID-19

Viruses, 2023
In the early stages of drug discovery, researchers develop assays that are compatible with high throughput screening (HTS) and structure activity relationship (SAR) measurements.
Ralph A. Tripp, David E. Martin
doaj   +1 more source

Novel (sulfated) thyroid hormone transporters in the solute carrier 22 family

European Thyroid Journal, 2023
Objective: Thyroid hormone (TH) transport represents a critical first step in governing intracellular TH regulation. It is still unknown whether the full repertoire of TH transporters has been identified.
Zhongli Chen, Robin P Peeters, Wesley Flach, Linda J de Rooij, Sena Yildiz, Alexander Teumer, Matthias Nauck, Rosalie B T M Sterenborg, Joost H W Rutten, Marco Medici, W Edward Visser, Marcel E Meima   +11 more
doaj   +1 more source

Probenecid‐Boosted Tenofovir: A Physiologically‐Based Pharmacokinetic Model‐Informed Strategy for On‐Demand HIV Preexposure Prophylaxis

CPT: Pharmacometrics & Systems Pharmacology, 2020
Multiple doses of tenofovir disoproxil fumarate (TDF) together with emtricitabine is effective for HIV preexposure prophylaxis (PrEP). TDF is converted to tenofovir (TFV) in circulation, which is subsequently cleared via tubular secretion by organic ion ...
Stephanie N. Liu, Zeruesenay Desta, Brandon T. Gufford   +2 more
doaj   +1 more source

Caregiver Perspectives on the Burden of Disease and Treatment in Uncontrolled Gout

Arthritis Care &Research, EarlyView.
Objective Uncontrolled gout (UG) refers to persistently elevated serum urate (SU) levels >6 mg/dL and ongoing gout symptoms despite use of urate‐lowering therapy (ULT). The objective of this study was to evaluate the burden associated with informal caregiving for individuals with UG.
Angelo Gaffo, Bhavisha Desai, Abiola Oladapo, Nana Kragh, Rebekah Zincavage, Brad Padilla, Naomi Schlesinger   +6 more
wiley   +1 more source

Synthesis, X-ray diffraction analysis, quantum chemical studies and α-amylase inhibition of probenecid derived S-alkylphthalimide-oxadiazole-benzenesulfonamide hybrids

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Sulphonamide and 1,3,4-oxadiazole moieties are present as integral structural parts of many drugs and pharmaceuticals. Taking into account the significance of these moieties, we herein present the synthesis, single-crystal X-ray analysis, DFT studies ...
Bilal Ahmad Khan, Syeda Shamila Hamdani, Muhammad Naeem Ahmed, Shahid Hameed, Muhammad Ashfaq, Ahmed M. Shawky, Mahmoud A. A. Ibrahim, Peter A. Sidhom   +7 more
doaj   +1 more source

Versatile Detection of Cellular Protein via Fluorescence Anisotropy

Advanced Science, EarlyView.
Cell Lysate Fluorescence Anisotropy (CFAST) utilizes long lifetime dye‐labeled nanobodies for rapid protein quantification in minimally purified, complex cell lysate. When coupled with cellular thermal shift, CFAST allows high‐throughput detection of endogenous protein‐small molecule engagement, facilitating the discovery of novel binders for ...
Qing Tang, Yuan‐Ping Wei, Ricky Ruiqi Ma, Na Wei, Tammy Zihan Zhou, Hilary Kung‐Yu Ho, Zafar Iqbal Bhat, Iqra Ishrat, Xiaoyu Li, Judy Wai Ping Yam, Yung Hou Wong, Qiankun Wang, Justin L. Tan   +12 more
wiley   +1 more source

Inhibition of ABCC6 Transporter Modifies Cytoskeleton and Reduces Motility of HepG2 Cells via Purinergic Pathway

Cells, 2020
ABCC6, belonging to sub-family C of ATP-binding cassette transporter, is an ATP-dependent transporter mainly present in the basolateral plasma membrane of hepatic and kidney cells.
Angela Ostuni, Monica Carmosino, Rocchina Miglionico, Vittorio Abruzzese, Fabio Martinelli, Daniela Russo, Ilaria Laurenzana, Agata Petillo, Faustino Bisaccia   +8 more
doaj   +1 more source

MAM‐Localized MANF Counteracts Microinflammatory Stress to Attenuate Mitochondrial Dysfunction and Cataractogenesis in High Myopia

Advanced Science, EarlyView.
Chronic microinflammation in high myopia suppresses MANF in lens epithelial cells. MANF normally resides within MAMs and promotes ubiquitin‐mediated degradation of the ER Ca2+ pump SERCA2. MANF loss causes pathological SERCA2 accumulation, MAM hyperassembly, and disrupted ER‐to‐mitochondria Ca2+ transfer, leading to mitochondrial failure, oxidative ...
Xin Liu, Hao Li, Ching Kang, Dongling Guo, Shuyu Liu, Jiaqi Meng, Zhiqian Huang, Yu Du, Xiangjia Zhu   +8 more
wiley   +1 more source

Combination of probenecid-sulphadoxine-pyrimethamine for intermittent preventive treatment in pregnancy

Malaria Journal, 2012
The antifolate sulphadoxine-pyrimethamine (SP) has been used in the intermittent prevention of malaria in pregnancy (IPTp). SP is an ideal choice for IPTp, however, as resistance of Plasmodium falciparum to SP increases, data are accumulating that SP may
Gutman Julie, Kachur S, Slutsker Laurence, Nzila Alexis, Mutabingwa Theonest   +4 more
doaj   +1 more source

Towards pharmacokinetic boosting of phenoxymethylpenicillin (penicillin-V) using probenecid for the treatment of bacterial infections

Scientific Reports
In the face of increasing antimicrobial tolerance and resistance there is a global obligation to optimise oral antimicrobial dosing strategies including narrow spectrum penicillins, such as penicillin-V.
Richard C. Wilson, Alaa Riezk, Paul Arkell, Damien Ming, Ryan Armiger, Victoria Latham, Mark J. Gilchrist, Anne-Grete Märtson, William W. Hope, Alison H. Holmes, Timothy M. Rawson   +10 more
doaj   +1 more source