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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Autori principali:	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
Natura:	Artigo
Lingua:	Inglês
Pubblicazione:	Nature Portfolio 2024-09-01
Serie:	Communications Chemistry
Accesso online:	https://doi.org/10.1038/s42004-024-01298-w
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