CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

• Main Authors: Almqvist, Helena, Axelsson, Hanna, Jafari, Rozbeh, Dan, Chen, Mateus, André, Haraldsson, Martin, Larsson, Andreas, Molina, Daniel Martinez, Artursson, Per, Lundbäck, Thomas, Nordlund, Pär
• Other Authors: School of Biological Sciences
• Format: Article
• Language: English
• Published: 2018
• Subjects: Screening; DRNTU::Science::Biological sciences; Molecular Biophysics
• Online Access: https://hdl.handle.net/10356/89820; http://hdl.handle.net/10220/47161
• Institution: Nanyang Technological University

Target engagement is a critical factor for therapeutic efficacy. Assessment of compound binding to native target proteins in live cells is therefore highly desirable in all stages of drug discovery. We report here the first compound library screen based on biophysical measurements of intracellular t...