Targeted sulfur(VI) fluoride exchange-mediated covalent modification of a tyrosine residue in the catalytic pocket of tyrosyl-DNA phosphodiesterase 1

Abstract Developing effective inhibitors of the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (TDP1) has been challenging because of the enzyme shallow catalytic pocket and non-specific substrate binding interactions. Recently, we discovered a quinolone-binding hot spot in TDP1’s active site pro...

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Autors principals:	Xue Zhi Zhao, Idris A. Barakat, George T. Lountos, Wenjie Wang, Keli Agama, Md Rasel Al Mahmud, Kiall F. Suazo, Thorkell Andresson, Yves Pommier, Terrence R. Burke
Format:	Artigo
Idioma:	Inglês
Publicat:	Nature Portfolio 2024-09-01
Col·lecció:	Communications Chemistry
Accés en línia:	https://doi.org/10.1038/s42004-024-01298-w
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