Results 21 to 30 of about 3,370 (187)
Wogonoside alleviates hyperosmotic stress-induced inflammation and apoptosis in human corneal epithelial cells via PI3K/AKT signaling [PDF]
Frontiers in MedicineBackgroundDry eye is a multifactorial ocular surface disorder in which tear hyperosmolarity acts as a major stressor that promotes inflammatory injury and apoptosis in corneal epithelial cells.
Yuan Zhong +6 more
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Sinomenine Regulates PSMB9 to Mediate Therapeutic Effects in Rheumatoid Arthritis [PDF]
CellsRheumatoid arthritis (RA) is a systemic immune-related disease characterized by chronic synovial inflammation and progressive joint destruction. However, the molecular mechanisms and diagnostic biomarkers underlying RA remain unclear.
Cui Zhang +4 more
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Scientific ReportsAs an important self-protection response mechanism of the body, inflammation can not only remove the necrotic or even malignant cells in the body, but also take a series of targeted measures to eliminate the pathogen of foreign invasion and block the ...
Yu Zhou Shen +5 more
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MS CETSA deep functional proteomics uncovers DNA repair programs leading to gemcitabine resistance
Nature CommunicationsMechanisms for resistance to cytotoxic cancer drugs are dependent on dynamic changes in the biochemistry of cellular pathways, information which is hard to obtain at the systems level.
Ying Yu Liang +12 more
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Perspective on CETSA Literature: Toward More Quantitative Data Interpretation [PDF]
SLAS Discovery, 2020 The cellular thermal shift assay (CETSA) was introduced in 2013 to investigate drug-target engagement inside live cells and tissues. As with all thermal shift assays, the response measured by CETSA is not simply governed by ligand affinity to the investigated target protein, but the thermodynamics and kinetics of ligand binding and protein unfolding ...
Brinton Seashore-Ludlow +2 more
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CETSA-based target engagement of taxanes as biomarkers for efficacy and resistance [PDF]
Scientific Reports, 2019 AbstractThe use of taxanes has for decades been crucial for treatment of several cancers. A major limitation of these therapies is inherent or acquired drug resistance. A key to improved outcome of taxane-based therapies is to develop tools to predict and monitor drug efficacy and resistance in the clinical setting allowing for treatment and dose ...
Anette Langebäck +13 more
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Structural Alternation in Heat Shock Proteins of Activated Macrophages
Cells, 2021 The inflammatory response of macrophages is an orderly and complex process under strict regulation accompanied by drastic changes in morphology and functions.
Wenhao Zhang +9 more
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A real-time cellular thermal shift assay (RT-CETSA) to monitor target engagement [PDF]
, 2022 Abstract Determining a molecule’s mechanism of action is paramount during chemical probe development and drug discovery. The cellular thermal shift assay (CETSA) is a valuable tool to confirm target engagement in cells for a small molecule that demonstrates a pharmacological effect.
Tino W. Sanchez +14 more
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CETSA quantitatively verifies in vivo target engagement of novel RIPK1 inhibitors in various biospecimens [PDF]
Scientific Reports, 2017 AbstractThe proof of target engagement (TE) is a key element for evaluating potential investment in drug development. The cellular thermal shift assay (CETSA) is expected to facilitate direct measurement of intracellular TE at all stages of drug development.
Ishii, Tsuyoshi +10 more
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Pharmaceuticals, 2023 Fenofibrate is known as a lipid-lowering drug. Although previous studies have reported that fenofibrate exhibits potential antitumor activities, IC50 values of fenofibrate could be as high as 200 μM. Therefore, we investigated the antitumor activities of
Jin Jin +9 more
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