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Inhibition of phosphodiesterases 1 and 4 prevents myofibroblast transformation in Peyronie's disease.
BJU Int
December 2024
Fibrosis Research Group, Medical Technology Research Centre, Anglia Ruskin University, Chelmsford, UK.
Objectives: To investigate which phosphodiesterase (PDE) isoforms are expressed in fibroblasts isolated from the tunica albuginea (TA) of patients with Peyronie's disease (PD), and to measure the potency of PDE inhibitors in preventing transformation of these fibroblasts to profibrotic myofibroblasts.
Materials And Methods: Fibroblasts isolated from the TA of men undergoing surgery for correction of PD curvature were transformed to myofibroblasts using transforming growth factor beta-1. The expression of 21 PDE isoforms was investigated using quantitative reverse transcriptase-polymerase chain reaction and protein analysis, as were the effects of various PDE inhibitors on prevention of myofibroblast transformation.
Epertinib counteracts multidrug resistance in cancer cells by antagonizing the drug efflux function of ABCB1 and ABCG2.
Biomed Pharmacother
November 2024
Graduate Institute of Biomedical Sciences, College of Medicine, Chang Gung University, Taoyuan 33302, Taiwan; Department of Obstetrics and Gynecology, Taipei Chang Gung Memorial Hospital, Taipei 10507, Taiwan; Department of Physiology and Pharmacology, College of Medicine, Chang Gung University, Taoyuan 33302, Taiwan; Molecular Medicine Research Center, College of Medicine, Chang Gung University, Taoyuan 33302, Taiwan. Electronic address:
Article Synopsis
- Multidrug resistance (MDR) in cancer treatment is often caused by overactive ABC transporters like ABCB1 and ABCG2, which pump out drugs and lessen their effectiveness.
- Researchers are exploring drug repurposing to combat MDR, and epertinib, a drug in trials for solid tumors, shows promise in reversing MDR effects by enhancing the sensitivity of resistant cancer cells to chemotherapy.
- Epertinib works by blocking the efflux functions of ABCB1 and ABCG2 without changing their levels, suggesting it could be beneficial when combined with other treatments for patients with tumors high in these transporters.
The thienopyridine A-769662 and benzimidazole 991 inhibit human TASK-3 potassium channels in an AMPK-independent manner.
Biochem Pharmacol
December 2024
Centre for Discovery Brain Sciences, Hugh Robson Building, University of Edinburgh, Edinburgh EH8 9XD, UK. Electronic address:
Article Synopsis
- TASK-1/3 channels in carotid body type 1 cells are key for sensing low oxygen levels, affecting potassium currents and ultimately influencing breathing patterns.
- Recent studies questioned whether AMP-activated protein kinase (AMPK) directly inhibits TASK-3 channels in response to hypoxia, although a recognizable phosphorylation motif was found in human TASK-3.
- Experiments with various AMPK activators indicated that two compounds, A-769662 and 991, inhibit hTASK-3 currents, while establishing that AMPK does not regulate TASK-3 currents as initially proposed.
Valence Electronic Structure of Interfacial Phenol in Water Droplets.
J Phys Chem A
September 2024
Department of Chemistry and Applied Biosciences, ETH Zurich, 8093 Zurich, Switzerland.
Biochemistry and a large part of atmospheric chemistry occur in aqueous environments or at aqueous interfaces, where (photo)chemical reaction rates can be increased by up to several orders of magnitude. The key to understanding the chemistry and photoresponse of molecules in and "on" water lies in their valence electronic structure, with a sensitive probe being photoelectron spectroscopy. This work reports velocity-map photoelectron imaging of submicrometer-sized aqueous phenol droplets in the valence region after nonresonant (288 nm) and resonance-enhanced (274 nm) two-photon ionization with femtosecond ultraviolet light, complementing previous liquid microjet studies.
View Article and Find Full Text PDFPolysaccharide fraction from Triplostegia glandulifera Wall and its renoprotective effect in streptozotocin-induced diabetic mice by attenuating oxidative stress.
Nat Prod Bioprospect
August 2024
College of Pharmacy, Dali University, Xueren Road 2, Xiaguan, Dali, 671000, Yunnan Province, People's Republic of China.
Article Synopsis
- Triplostegia glandulifera (T. glandulifera) is a traditional medicine used in Yunnan, China, for treating kidney issues, but its active compounds and protective effects are not well-documented.
- This study extracted two polysaccharide fractions, TGB and TGC, revealing TGB's lower molecular weight and beneficial monosaccharide profile including D-galacturonic acid and D-glucose.
- The research demonstrated that TGB has strong antioxidant properties, improves kidney function, and reduces damage in both a lab cell model and diabetic mice, suggesting its effectiveness in combatting diabetic nephropathy.
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