First Fluorescent Acetylspermidine Deacetylation Assay for HDAC10 Identifies Selective Inhibitors with Cellular Target Engagement
Sign Up to like & getrecommendations! Published in 2022 at "Chembiochem"
DOI: 10.1002/cbic.202200180
Abstract: Histone deacetylases (HDACs) are important epigenetic regulators involved in many diseases, especially cancer. Five HDAC inhibitors have been approved for anticancer therapy and many are in clinical trials. Among the 11 zinc‐dependent HDACs, HDAC10 has… read more here.
Keywords: assay hdac10; deacetylation; cellular target; target engagement ... See more keywords
Gold Nanoparticle-Based Photo-Cross-Linking Strategy for Cellular Target Identification of Supercomplex Molecular Systems.
Sign Up to like & getrecommendations! Published in 2022 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.1c04652
Abstract: Cellular target identification plays an essential role in innovative drug development and pharmacological mechanism elucidation. However, very few practical experimental methodologies have been developed for identifying target proteins for supercomplex molecular systems such as biologically… read more here.
Keywords: cellular target; supercomplex molecular; molecular systems; cross ... See more keywords
Cellular Target Proteome in Breast Cancer Cells of an Oplopane Sesquiterpenoid Isolated from Tussilago farfara.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of natural products"
DOI: 10.1021/acs.jnatprod.0c00043
Abstract: Tussilago farfara is a traditional herbal medicine used to treat coughs, bronchitis, and asthma. Its bioactive compounds include sesquiterpenoids with anti-inflammatory, antiproliferative, neuroprotective, and other effects. Biochemical studies have highlighted the mechanisms of action, but… read more here.
Keywords: cellular target; target; breast cancer; cancer cells ... See more keywords
Cellular Target Deconvolution of Small Molecules Using a Selection-Based Genetic Screening Platform
Sign Up to like & getrecommendations! Published in 2022 at "ACS Central Science"
DOI: 10.1021/acscentsci.2c00609
Abstract: Small-molecule drug target identification is an essential and often rate-limiting step in phenotypic drug discovery and remains a major challenge. Here, we report a novel platform for target identification of activators of signaling pathways by… read more here.
Keywords: platform; target; cellular target; small molecules ... See more keywords
Photoaffinity labelling-based chemoproteomic strategy identifies PEBP1 as the target of ethyl gallate against macrophage activation.
Sign Up to like & getrecommendations! Published in 2023 at "Chemical communications"
DOI: 10.1039/d2cc05440j
Abstract: Ulcerative colitis (UC) is an inflammatory disease of the colon with an unmet need for therapeutic targets. Ethyl gallate (EG) is a natural small molecule for UC treatment, but its cellular target is unknown. By… read more here.
Keywords: ethyl gallate; cellular target; labelling based; photoaffinity labelling ... See more keywords
Microglia as a cellular target of diclofenac therapy in Alzheimer’s disease
Sign Up to like & getrecommendations! Published in 2023 at "Therapeutic Advances in Neurological Disorders"
DOI: 10.1177/17562864231156674
Abstract: Alzheimer’s disease (AD) is an untreatable cause of dementia, and new therapeutic approaches are urgently needed. AD pathology is defined by extracellular amyloid plaques and intracellular neurofibrillary tangles. Research of the past decades has suggested… read more here.
Keywords: cellular target; alzheimer disease; pathology; microglia cellular ... See more keywords