REV1 and fibrosarcoma: In a series of works, researchers at the University of Connecticut identified multiple small molecule TLS inhibitors targeting Rev1-CT/RIR PPIs.328–332 Two initial scaffolds, thiophene and piperazine, identified in an FP-based HTS assay disrupted the Rev1-CT PPI with a fluorescently tagged FAM-Polκ-RIR peptide (Fig. 9C).328 The thiophene scaffold compound was shown to bind the RIR-interface of Rev1-CT by NMR, sensitized fibrosarcoma cells to cisplatin, and reduced cisplatin-induced mutagenesis.