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

• المؤلفون الرئيسيون: Almqvist, Helena, Axelsson, Hanna, Jafari, Rozbeh, Dan, Chen, Mateus, André, Haraldsson, Martin, Larsson, Andreas, Molina, Daniel Martinez, Artursson, Per, Lundbäck, Thomas, Nordlund, Pär
• مؤلفون آخرون: School of Biological Sciences
• التنسيق: مقال
• اللغة: English
• منشور في: 2018
• الموضوعات: Screening; DRNTU::Science::Biological sciences; Molecular Biophysics
• الوصول للمادة أونلاين: https://hdl.handle.net/10356/89820; http://hdl.handle.net/10220/47161

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...