Results 31 to 40 of about 3,370 (187)
Current and emerging target identification methods for novel antimalarials
International Journal for Parasitology: Drugs and Drug Resistance, 2022 New antimalarial compounds with novel mechanisms of action are urgently needed to combat the recent rise in antimalarial drug resistance. Phenotypic high-throughput screens have proven to be a successful method for identifying new compounds, however, do ...
Matthew P. Challis +2 more
doaj +1 more source
Comparison of Cellular Target Engagement Methods for the Tubulin Deacetylases Sirt2 and HDAC6: NanoBRET, CETSA, Tubulin Acetylation, and PROTACs [PDF]
ACS Pharmacology & Translational Science, 2022 The tubulin deacetylases Sirt2 and HDAC6 have been associated with the development of various diseases. Herein, we discuss recent approaches that enable cellular target engagement studies for these deacetylases and thus play a critical role in the evaluation of small molecule inhibitors of Sirt2 or HDAC6 as potential therapeutic agents.
Anja Vogelmann +3 more
openaire +3 more sources
Biological Evaluation of a Mitochondrial Phosphoenolpyruvate Carboxykinase Inhibitor
Proceedings, 2019 Phosphoenolpyruvate carboxykinase (PEPCK) is a key enzyme in gluconeogenesis, catalyzingthe decarboxylation of oxaloacetate to phosphoenolpyruvate. [...]
Sergio Rodríguez-Arévalo +9 more
doaj +1 more source
Streamlining cellular thermal shift assay for ultra-high throughput screening
SLAS DiscoveryThe Cellular Thermal Shift Assay (CETSA) has emerged as a powerful tool for evaluating drug-target interactions in live cells, yet its application in ultra-high throughput screening (uHTS) has been limited by technical constraints.
Pascal Lambertz +9 more
doaj +1 more source
Olea europaea Suppresses Inflammation by Targeting TAK1-Mediated MAP Kinase Activation
Molecules, 2021 Possessing a variety of medicinal functions, Olea europaea L. is widely cultivated across the world. However, the anti-inflammatory mechanism of Olea europaea is not yet fully elucidated.
Chaoran Song, Mi-Yeon Kim, Jae Youl Cho
doaj +1 more source
SLAS DiscoveryThe cellular thermal shift assay (CETSA®) is a target engagement method widely used for preclinical characterization of small molecule compounds. CETSA® has been used for semi-quantitative readouts in whole blood with PBMC isolation, and quantitative ...
Shitalben Patel +9 more
doaj +1 more source
Redox Biology, 2023 Benzo[α]pyrene (Bap) is recognized as a ubiquitous environmental pollutant among the polycyclic aromatic hydrocarbons (PAHs) class. Previous studies have shown that the hepatotoxicity of Bap is mainly caused by its metabolites, although it remains ...
Yanwei Wang +8 more
doaj +1 more source
Proteome-wide CETSA reveals new step in apoptosis control
Trends in Cell BiologyApoptosis, a well-established program of cell death, is fundamental to all multicellular organisms. Recent studies of apoptosis initiation events using proteome-wide cellular thermal shift assay (CETSA) have revealed a novel regulatory mechanism involving the cleavage of nuclear substrates.
Inna N, Lavrik, Nikita V, Ivanisenko
openaire +2 more sources
Advanced Materials, EarlyView.Lignin‐mimicking protein methylation can enhance the efficacy and mitigate the toxicity of the classic FOLFOX chemotherapy regimen. ABSTRACT FOLFOX has served as the standard chemotherapy regimen for advanced stages, specifically in the treatment of pancreatic, colorectal, and bladder cancers.
Shiyao Song +14 more
wiley +1 more source
Advanced Science, EarlyView.ABSTRACT Brown and beige adipocytes dissipate energy as heat, yet effective strategies to enhance their mitochondrial efficiency remain limited. Here, we identify Agnuside (AGN) as a selective stabilizer of the complex I assembly factor NDUFAF6. AGN directly binds cytosolic NDUFAF6, suppresses its ubiquitination, prolongs its half‐life, and facilitates
Qingwen Zhao +7 more
wiley +1 more source