New routes for PTP1B allosteric inhibition by multitemperature crystallography, fragment screening and covalent tethering
D. A. Keedy, Z. B. Hill, J. T. Biel, E. Kang, T. J. Rettenmaier, J. Brandao-Neto, N. M. Pearce, F. von Delft, J. A. Wells, J. S. Fraser
The paper identifies a new allosteric site in PTP1B using multitemperature crystallography and fragment screening, showing covalent tethering can inhibit enzyme activity.
bioRxiv · Nov 13, 2017Biophysics