Identification of a ligand binding hot spot and structural motifs replicating aspects of tyrosyl-DNA phosphodiesterase I (TDP1) phosphoryl recognition by crystallographic fragment cocktail screening

Identification of a ligand binding hot spot and structural motifs replicating aspects of tyrosyl-DNA phosphodiesterase I (TDP1)

Crystal structure of Tyrosyl DNA-phosphodiesterase I (TDP1) bound to one of the small molecule inhibitors discovered by crystallographic fragment screening establishes a foundation for structure-assisted development of medicinal inhibitors of TDP1, a cancer drug target. View the artical

Citation: 

See: Identification of a ligand binding hot spot and structural motifs replicating aspects of tyrosyl-DNA phosphodiesterase I (TDP1) phosphoryl recognition by crystallographic fragment cocktail screening by George T. Lountos, Xue Zhi Zhao, Evgeny Kiselev, Joseph E. Tropea, Danielle Needle, Yves Pommier, Terrence R. Burke, Jr. and David S. Waugh in Nucleic Acids Research, 2019, 47, 10134–10150.

Published Date: 
October, 2019