99733-18-3Relevant articles and documents
Molecular recognition in bisurea thermoplastic elastomers studied with pyrene-based fluorescent probes and atomic force microscopy
Botterhuis, Nicole E.,Karthikeyan,Veldman, Dirk,Meskers, Stefan C. J.,Sijbesma, Rint P.
, p. 3915 - 3917 (2008)
Fluorescence spectroscopy and atomic force microscopy (AFM) measurements using bisurea-pyrene probes show that they are randomly dispersed in the hard blocks of thermoplastic elastomers with matching bisurea groups, whereas they phase separate from polymers with non-matching or no bisurea groups. The Royal Society of Chemistry.
Design, synthesis and biological evaluation of tyrosinase-targeting PROTACs
Cui, Xin,Deng, Yun,Fu, Dingqiang,Li, Guangxun,Qin, Fengming,Tang, Zhuo,Xu, Yan,Yao, Shaohua,Yuan, Yi
supporting information, (2021/10/12)
The human tyrosinase is the most prominent therapeutic target for pigmentary skin disorders. However, the overwhelming majority efforts have been devoted to search mushroom tyrosinase inhibitors, which show poor inhibitory activity on human tyrosinase and certain side effects that cause skin damage in practical application. Herein, a series of degraders that directly targeted human tyrosinase was firstly designed and synthesized based on newly developed PROTAC technology. The best PROTAC TD9 induced human tyrosinase degradation obviously in dose and time-dependent manner, and its mechanism of inducing tyrosinase degradation has also been clearly demonstrated. Besides, encouraging results that low-toxicity PROTAC TD9 was applied to reduce zebrafish melanin synthesis have been obtained, highlighting the potential to treatment of tyrosinase-related disorders. Moreover, this work has innovatively expanded the application scope of PROTAC technology and laid a solid foundation for further development of novel drugs treating pigmentary skin disorders.
Fluorescent H2Receptor Squaramide-Type Antagonists: Synthesis, Characterization, and Applications
Alencastre, Inês,Bernhardt, Günther,Biselli, Sabrina,Buschauer, Armin,Chen, Mengya,Erdmann, Daniela,Gomez-Lazaro, Maria,Keller, Max,Lamghari, Meriem,Littmann, Timo,Maia, André F.,Ozawa, Takeaki,Tanaka, Miho,Tropmann, Katharina
supporting information, p. 1521 - 1528 (2020/09/15)
Fluorescence labeled ligands have been gaining importance as molecular tools, enabling receptor-ligand-binding studies by various fluorescence-based techniques. Aiming at red-emitting fluorescent ligands for the hH2R, a series of squaramides labeled with pyridinium or cyanine fluorophores (19-27) was synthesized and characterized. The highest hH2R affinities in radioligand competition binding assays were obtained in the case of pyridinium labeled antagonists 19-21 (pKi: 7.71-7.76) and cyanine labeled antagonists 23 and 25 (pKi: 7.67, 7.11). These fluorescent ligands proved to be useful tools for binding studies (saturation and competition binding as well as kinetic experiments), using confocal microscopy, flow cytometry, and high content imaging. Saturation binding experiments revealed pKd values comparable to the pKi values. The fluorescent probes 21, 23, and 25 could be used to localize H2 receptors in HEK cells and to determine the binding affinities of unlabeled compounds.
