Fabian Offensperger, Gary Tin, Miquel Duran-Frigola, Elisa Hahn, Sarah Dobner, Christopher W Am Ende, Joseph W Strohbach, Andrea Rukavina, Vincenth Brennsteiner, Kevin Ogilvie, Nara Marella, Katharina Kladnik, Rodolfo Ciuffa, Jaimeen D Majmudar, S Denise Field, Ariel Bensimon, Luca Ferrari, Evandro Ferrada, Amanda Ng, Zhechun Zhang, Gianluca Degliesposti, Andras Boeszoermenyi, Sascha Martens, Robert Stanton, André C Müller, J Thomas Hannich, David Hepworth, Giulio Superti-Furga, Stefan Kubicek, Monica Schenone, Georg E Winter
Chemical modulation of proteins enables a mechanistic understanding of biology and represents the foundation of most therapeutics. However, despite decades of research, 80% of the human proteome lacks functional ligands. Chemical proteomics has advanced fragment-based ligand discovery toward cellular systems, but throughput limitations have stymied the scalable identification of fragment-protein interactions. We report proteome-wide maps of protein-binding propensity for 407 structurally diverse small-molecule fragments...
April 26, 2024: Science