Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation

Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6 (HDAC6) has been associated with the pathogenesis of cancer and neurodegeneration, thus making these two enzymes promising targets for pharmaceutical intervention. Herein, we report the design, synthesis, and...

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Veröffentlicht in:	Journal of medicinal chemistry 2023-11, Vol.66 (21), p.14787-14814
Hauptverfasser:	Sinatra, Laura, Vogelmann, Anja, Friedrich, Florian, Tararina, Margarita A., Neuwirt, Emilia, Colcerasa, Arianna, König, Philipp, Toy, Lara, Yesiloglu, Talha Z., Hilscher, Sebastian, Gaitzsch, Lena, Papenkordt, Niklas, Zhai, Shiyang, Zhang, Lin, Romier, Christophe, Einsle, Oliver, Sippl, Wolfgang, Schutkowski, Mike, Gross, Olaf, Bendas, Gerd, Christianson, David W., Hansen, Finn K., Jung, Manfred, Schiedel, Matthias
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylation Benzamides - chemistry Benzamides - pharmacology Biochemistry, Molecular Biology Chemical Sciences Histone Deacetylase 6 Histone Deacetylase Inhibitors - pharmacology Life Sciences Medicinal Chemistry Pharmaceutical sciences Pharmacology Pyrimidines - chemistry Pyrimidines - pharmacology Sirtuin 2 - metabolism Structural Biology Thiazoles - chemistry Thiazoles - pharmacology Tubulin - metabolism
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