Virtual Screening and Biological Evaluation of Inhibitors Targeting the XPA-ERCC1 Interaction

Authors: Barakat KH, Jordheim LP, Perez-Pineiro R, Wishart D, Dumont E, Tuszynski JA
Publication: PLoS One
Keywords: cell line tumor, DNA metabolism, DNA repair, DNA-binding proteins, humans, kinetics, protein binding, solubility
Software: ADMET Predictor®

Background

Nucleotide excision repair (NER) removes many types of DNA lesions including those induced by UV radiation and platinum-based therapy. Resistance to platinum-based therapy correlates with high expression of ERCC1, a major element of the NER machinery. The interaction between ERCC1 and XPA is essential for a successful NER function. Therefore, one way to regulate NER is by inhibiting the activity of ERCC1 and XPA.