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How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition—The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine

The β-carboline alkaloid harmine is a potent DYRK1A inhibitor, but suffers from undesired potent inhibition of MAO-A, which strongly limits its application. We synthesized more than 60 analogues of harmine, either by direct modification of the alkaloid or by de novo synthesis of β-carboline and rela...

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Detalles Bibliográficos
Autores principales: Wurzlbauer, Anne, Rüben, Katharina, Gürdal, Ece, Chaikuad, Apirat, Knapp, Stefan, Sippl, Wolfgang, Becker, Walter, Bracher, Franz
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7765920/
https://www.ncbi.nlm.nih.gov/pubmed/33339338
http://dx.doi.org/10.3390/molecules25245962