Identification of a covalent binder to the oncoprotein gankyrin using a NIR-Based OBOC screening method.

ABSTRACT: Despite huge advancements in the process of synthesizing small molecules as part of one-bead-one-compound (OBOC) libraries, progress lags in the ability to screen these libraries against proteins of interest. Recently, we developed a method to screen OBOC libraries in which a target protein is labeled with a near-infrared (NIR) range fluorophore. The labeled protein incubates with beads of a library in a 96-well plate, then the plate is imaged for fluorescence. Fluorescence intensities produced by the labeled protein binding the bead can be quantitated and provide a basis to rank hits. Here, we present an application of this technique by screening the oncoprotein gankyrin against a 343-member peptoid library. The library was composed of four positions occupied by one of seven amines. In th

SUBMITTER: Maresh ME 

PROVIDER: S-EPMC8697547 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature