[1,2,4]Triazolo[3,4-b]benzothiazole Scaffold as Versatile Nicotinamide Mimic Allowing Nanomolar Inhibition of Different PARP Enzymes

[Image: see text] We report [1,2,4]triazolo[3,4-b]benzothiazole (TBT) as a new inhibitor scaffold, which competes with nicotinamide in the binding pocket of human poly- and mono-ADP-ribosylating enzymes. The binding mode was studied through analogues and cocrystal structures with TNKS2, PARP2, PARP1...

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Detalles Bibliográficos
Autores principales: Murthy, Sudarshan, Nizi, Maria Giulia, Maksimainen, Mirko M., Massari, Serena, Alaviuhkola, Juho, Lippok, Barbara E., Vagaggini, Chiara, Sowa, Sven T., Galera-Prat, Albert, Ashok, Yashwanth, Venkannagari, Harikanth, Prunskaite-Hyyryläinen, Renata, Dreassi, Elena, Lüscher, Bernhard, Korn, Patricia, Tabarrini, Oriana, Lehtiö, Lari
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2023
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9884089/
https://www.ncbi.nlm.nih.gov/pubmed/36598465
http://dx.doi.org/10.1021/acs.jmedchem.2c01460

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