25692-41-5Relevant academic research and scientific papers
Demonstrating Ligandability of the LC3A and LC3B Adapter Interface
Hartmann, Markus,Huber, Jessica,Kramer, Jan S.,Heering, Jan,Pietsch, Larissa,Stark, Holger,Odadzic, Dalibor,Bischoff, Iris,Fürst, Robert,Schr?der, Martin,Akutsu, Masato,Chaikuad, Apirat,D?tsch, Volker,Knapp, Stefan,Biondi, Ricardo M.,Rogov, Vladimir V.,Proschak, Ewgenij
, p. 3720 - 3746 (2021/05/04)
Autophagy is the common name for a number of lysosome-based degradation pathways of cytosolic cargos. The key components of autophagy are members of Atg8 family proteins involved in almost all steps of the process, from autophagosome formation to their selective fusion with lysosomes. In this study, we show that the homologous members of the human Atg8 family proteins, LC3A and LC3B, are druggable by a small molecule inhibitor novobiocin. Structure-activity relationship (SAR) studies of the 4-hydroxy coumarin core scaffold were performed, supported by a crystal structure of the LC3A dihydronovobiocin complex. The study reports the first nonpeptide inhibitors for these protein interaction targets and will lay the foundation for the development of more potent chemical probes for the Atg8 protein family which may also find applications for the development of autophagy-mediated degraders (AUTACs).
COMPOUNDS FOR MODULATING DDAH AND ADMA LEVELS, AS WELL AS METHODS OF USING THEREOF TO TREAT DISEASE
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Page/Page column 69; 70, (2019/11/19)
Disclosed are compounds that can modulate DDAH and the amount of asymmetric dimethylarginine (ADMA) in a subject. Also provided are pharmaceutical compositions comprising these compounds, as well as methods of using these compositions to treat and/or prevent diseases associated with elevated or low levels of DDAH and ADMA.
Ratiometric O2 sensing based on selective self-sensitized photooxidation of donor-acceptor fluorophores
Wang, Jian-Xin,Niu, Li-Ya,Chen, Peng-Zhong,Chen, Yu-Zhe,Yang, Qing-Zheng,Boulatov, Roman
supporting information, p. 7017 - 7020 (2019/06/20)
We report a series of organic fluorophores that undergo selective self-sensitized photooxidation upon light irradiation in air accompanied by a change of fluorescence from yellow to blue on the seconds timescale. The distinct emission changes allow the ratiometric quantitation of O2 concentration.
Synthesis and Use of Intermetallic Iron Palladium Nanoparticle Compositions
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Page/Page column 4, (2011/10/02)
An intermetallic magnetic compound of iron oxide and palladium with a nanometer particle size is disclosed, together with a method of making magnetic nanoparticles that include an intermetallic bond between palladium and iron-oxide. Additionally, a method is disclosed of catalyzing an organic reaction by contacting the organic reagents with an intermetallic magnetic compound of iron oxide and palladium that has nanometer particle size in an amount sufficient to catalyze the organic reaction.
Alpha-helical mimetics
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Page/Page column 90, (2011/05/18)
Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.
ALPHA-HELICAL MIMETICS
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Page/Page column 183-184, (2010/02/15)
Benzoyl urea derivatives that are alpha helical peptide mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralising pro-survival Bcl-2 proteins. Use of the benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also disclosed.
