Nsp3 macrodomain of SARS-CoV-2 ; A Target Enabling Package

The conserved macrodomain encoded as non-structural protein 3 (Nsp3 Mac1) is employed by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) to remove host-derived ribosylation, which is a post-translational modification involved in the production of antiviral cytokines. This TEP provides early tools to develop Nsp3 Mac1 inhibitors, including purification protocols of recombinant proteins, reproducible crystallisation condition suitable for X-ray crystallography fragment screening, biophysical (activity and binding) assays and over 200 fragment hits representing a wide range of chemotypes, that are a starting point for the development of more selective and potent compounds.