Substrate-based chemical probes for Alzheimer’s γ-secretase
Sign Up to like & getrecommendations! Published in 2020 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-020-02565-w
Abstract: The membrane-embedded γ-secretase complex carries out hydrolysis within the lipid bilayer in proteolyzing nearly 100 different membrane protein substrates. Among these substrates, the amyloid precursor protein (APP) has been the most studied, as generation of… read more here.
Keywords: secretase; based chemical; substrate based; chemical probes ... See more keywords
Chemical Probes in Sirtuin Research.
Sign Up to like & getrecommendations! Published in 2018 at "Progress in molecular biology and translational science"
DOI: 10.1016/bs.pmbts.2017.11.014
Abstract: Sirtuins refer to a family of intracellular enzymes that are the yeast silent information regulator 2 (sir2) protein homologs found in organisms from all the three kingdoms of life. This family of enzymes primarily catalyze… read more here.
Keywords: catalyzed deacylation; chemical probes; chemical; reaction ... See more keywords
Chemical Probes for Visualizing Intact Animal and Human Brain Tissue.
Sign Up to like & getrecommendations! Published in 2017 at "Cell chemical biology"
DOI: 10.1016/j.chembiol.2017.05.015
Abstract: Newly developed tissue clearing techniques can be used to render intact tissues transparent. When combined with fluorescent labeling technologies and optical sectioning microscopy, this allows visualization of fine structure in three dimensions. Gene-transfection techniques have… read more here.
Keywords: brain tissue; human brain; tissue; chemical probes ... See more keywords
Objective, Quantitative, Data-Driven Assessment of Chemical Probes
Sign Up to like & getrecommendations! Published in 2018 at "Cell Chemical Biology"
DOI: 10.1016/j.chembiol.2017.11.004
Abstract: Summary Chemical probes are essential tools for understanding biological systems and for target validation, yet selecting probes for biomedical research is rarely based on objective assessment of all potential compounds. Here, we describe the Probe… read more here.
Keywords: probes objective; objective quantitative; quantitative data; data driven ... See more keywords
Validation and Invalidation of Chemical Probes for the Human N-myristoyltransferases
Sign Up to like & getrecommendations! Published in 2019 at "Cell Chemical Biology"
DOI: 10.1016/j.chembiol.2019.03.006
Abstract: Summary On-target, cell-active chemical probes are of fundamental importance in chemical and cell biology, whereas poorly characterized probes often lead to invalid conclusions. Human N-myristoyltransferase (NMT) has attracted increasing interest as target in cancer and… read more here.
Keywords: target; validation invalidation; chemical; biology ... See more keywords
Chemical Probes to Control and Visualize Lipid Metabolism in the Brain
Sign Up to like & getrecommendations! Published in 2022 at "Accounts of Chemical Research"
DOI: 10.1021/acs.accounts.2c00521
Abstract: Conspectus Signaling lipids, such as the endocannabinoids, play an important role in the brain. They regulate synaptic transmission and control various neurophysiological processes, including pain sensation, appetite, memory formation, stress, and anxiety. Unlike classical neurotransmitters,… read more here.
Keywords: control; brain; chemical probes; activity ... See more keywords
Paramagnetic Chemical Probes for Studying Biological Macromolecules.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical reviews"
DOI: 10.1021/acs.chemrev.1c00708
Abstract: Paramagnetic chemical probes have been used in electron paramagnetic resonance (EPR) and nuclear magnetic resonance (NMR) spectroscopy for more than four decades. Recent years witnessed a great increase in the variety of probes for the… read more here.
Keywords: probes studying; spectroscopy; paramagnetic chemical; biological macromolecules ... See more keywords
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01106
Abstract: LIMKs are important regulators of actin and microtubule dynamics, and they play essential roles in many cellular processes. Deregulation of LIMKs has been linked to the development of diverse diseases, including cancers and cognitive disabilities,… read more here.
Keywords: type iii; type type; development; chemical probes ... See more keywords
Potent Uncompetitive Inhibitors of Nicotinamide N-Methyltransferase (NNMT) as In Vivo Chemical Probes.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01166
Abstract: NNMT uses SAM as a cofactor to catalyze the methylation of nicotinamide, producing 1-methylnicotinamide. Recent studies have shown that NNMT upregulation in cancer-associated fibroblasts (CAFs) is required to maintain the CAF phenotype in high-grade serous… read more here.
Keywords: potent uncompetitive; chemical probes; uncompetitive inhibitors; nicotinamide methyltransferase ... See more keywords
Identification of Chemical Probes Targeting MBD2.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical biology"
DOI: 10.1021/acschembio.1c00959
Abstract: Epigenetics has received much attention in the past decade. Many insights on epigenetic (dys)regulation in diseases have been obtained, and clinical therapies targeting them are in place. However, the readers of the epigenetic marks are… read more here.
Keywords: identification chemical; probes targeting; targeting mbd2; chemical probes ... See more keywords
R-BIND: An Interactive Database for Exploring and Developing RNA-Targeted Chemical Probes.
Sign Up to like & getrecommendations! Published in 2019 at "ACS chemical biology"
DOI: 10.1021/acschembio.9b00631
Abstract: While the opportunities available for targeting RNA with small molecules have been widely appreciated, the challenges associated with achieving specific RNA recognition in biological systems have hindered progress and prevented many researchers from entering the… read more here.
Keywords: targeted chemical; exploring developing; rna; database ... See more keywords