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The histone demethylase KDM5C enhances the sensitivity of acute myeloid leukemia cells to lenalidomide by stabilizing cereblon.
Cell Mol Biol Lett
January 2025
Jiangsu Key Laboratory of Neuropsychiatric Diseases and College of Pharmaceutical Sciences, Jiangsu Province Engineering Research Center of Precision Diagnostics and Therapeutics Development, Jiangsu Key Laboratory of Preventive and Translational Medicine for Geriatric Diseases, Suzhou Key Laboratory of Drug Research for Prevention and Treatment of Hyperlipidemic Diseases, Soochow University, 199 Ren'ai Road, Suzhou, 215123, Jiangsu, China.
Background: The protein cereblon (CRBN) mediates the antileukemia effect of lenalidomide (Len). Len binds to CRBN, recruits IKZF1/IKZF3, and promotes their ubiquitination and degradation, through which Len exhibits its antileukemia and antimyeloma activity. Therefore, the protein level of CRBN might affect the antiproliferative effect of Len.
View Article and Find Full Text PDFCopper-dependent halogenase catalyses unactivated C-H bond functionalization.
Nature
January 2025
Department of Chemical and Biomolecular Engineering, University of California, Los Angeles, Los Angeles, CA, USA.
Carbon-hydrogen (C-H) bonds are the foundation of essentially every organic molecule, making them an ideal place to do chemical synthesis. The key challenge is achieving selectivity for one particular C(sp)-H bond. In recent years, metalloenzymes have been found to perform C(sp)-H bond functionalization.
View Article and Find Full Text PDFThe usefulness of HbA1c measurement in diabetic mouse models using various devices.
Exp Anim
January 2025
Division of Diabetes and Endocrinology, Department of Internal Medicine, Kobe University Graduate School of Medicine.
In most cases, the diagnosis of diabetes in animal models is based solely on blood glucose levels. While hemoglobin A1c (HbA1c) is widely used in the diagnosis of diabetes in humans, it is rarely measured in mice in diabetes research. This is thought to be because there are no established reference values for mouse HbA1c, as well as the fact that there are very few reports on the variability and reproducibility of measurements taken using different devices.
View Article and Find Full Text PDFκ-Carrageenan tetrasaccharide ameliorates particulate matter-induced defects in skin hydration of human keratinocytes cells and skin barrier disorders.
Int J Biol Macromol
January 2025
College of Ocean Food and Biological Engineering, Jimei University, Xiamen 361021, China; Fujian Provincial Key Laboratory of Food Microbiology and Enzyme Engineering, Xiamen 361021, China. Electronic address:
Urban air pollutants, mainly represented by PM containing organic and inorganic substances, can penetrate the human skin and trigger oxidative stress, potentially causing skin barrier damage and aging. κ-Carrageenan oligosaccharides as degradation products of natural sulfated polysaccharide have a great potential for skin moisturization as well as improving oxidative stress and inflammation. In this study, κ-carrageenan tetrasaccharide was obtained by enzymatic digestion of κ-carrageenan, and its role in alleviating particulate matter-induced inflammatory response in HaCaT keratinocyte cell line and skin barrier dysfunction was evaluated.
View Article and Find Full Text PDFSynthesis and biological evaluation of new dual APN/NEP inhibitors as potent analgesics.
Bioorg Chem
January 2025
School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Jinan 250012, China. Electronic address:
An alternative approach for the management of acute and chronic pains involves prolonging the half-life of endogenous opiates, such as enkephalins that are released in response to nociceptive stimuli. This can be achieved through the inhibition of enzymatic pathways responsible for the hydrolysis of these peptides, particularly targeting Aminopeptidase N (APN) and Neutral Endopeptidase (NEP). In this study, we designed and synthesized a series of dual enkephalinase inhibitors (DENKIs) targeting both APN and NEP as novel analgesic treatments.
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