Discovery of Potent Isoindolinone Inhibitors that Target an Active Conformation of PARP1 Using DNA-Encoded Libraries.

Kelly A McCarthy¹, Douglas J Marcotte¹, Sangram Parelkar¹, Crystal L McKinnon¹, Lindsay E Trammell¹, Eric L Stangeland¹, Rachael R Jetson¹

¹Discovery Sciences, Valo Health, 75 Hayden Avenue, Lexington, MA, 02421, United States.

PubMed DOI

Abstract

Inhibition of poly (ADP-ribose) polymerase-1 (PARP1), a DNA repair enzyme, has proven to be a successful strategy for the treatment of various cancers. With the appropriate selection conditions and protein design, DNA-encoded library (DEL) technology provides a powerful avenue to identify small molecules with the desired mechanism of action towards a target of interest. However, DNA-binding protei…

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