Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site.

Autor: Exell JC; Centre for Chemical Biology, Department of Chemistry, Krebs Institute, University of Sheffield, Sheffield, UK., Thompson MJ; Centre for Chemical Biology, Department of Chemistry, Krebs Institute, University of Sheffield, Sheffield, UK., Finger LD; Centre for Chemical Biology, Department of Chemistry, Krebs Institute, University of Sheffield, Sheffield, UK., Shaw SJ; Centre for Chemical Biology, Department of Chemistry, Krebs Institute, University of Sheffield, Sheffield, UK., Debreczeni J; Discovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Cambridge, UK., Ward TA; Bioscience, Oncology Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Alderley Park, Cheshire, UK., McWhirter C; Discovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Cambridge, UK., Siöberg CL; Pelago Bioscience AB, Solna, Sweden., Martinez Molina D; Pelago Bioscience AB, Solna, Sweden., Abbott WM; Discovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Cambridge, UK., Jones CD; Chemistry, Oncology Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Alderley Park, UK., Nissink JW; Chemistry, Oncology Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Cambridge, UK., Durant ST; Bioscience, Oncology Innovative Medicines and Early Development Biotech Unit, Cambridge, UK., Grasby JA; Centre for Chemical Biology, Department of Chemistry, Krebs Institute, University of Sheffield, Sheffield, UK.; Bioscience, Oncology Innovative Medicines and Early Development Biotech Unit, Cambridge, UK.

Publikováno v: Nature chemical biology [Nat Chem Biol] 2016 Oct; Vol. 12 (10), pp. 815-21. Date of Electronic Publication: 2016 Aug 15.