Structure-based evolution of a promiscuous inhibitor to a selective stabilizer of protein–protein interactions
oleh: Eline Sijbesma, Emira Visser, Kathrin Plitzko, Philipp Thiel, Lech-Gustav Milroy, Markus Kaiser, Luc Brunsveld, Christian Ottmann
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2020-08-01 |
Deskripsi
Small molecule stabilizers of protein–protein interactions hold great therapeutic potential. Based on virtual screening and molecular docking, the authors here develop a strategy to evolve weak, promiscuous inhibitors of 14-3-3 interactions into selective stabilizers of the 14-3-3/ChREBP complex.