Rho Family Proteins: Covalent Inhibitors Allosterically Block the Activation of Rho Family Proteins and Suppress Cancer Cell Invasion (Adv. Sci. 14/2020)

In article number 2000098, Bo Liu, Chuanpeng Liu, Yongjun Dang, Cheng Luo, and co‐workers describe the fi rst covalent and allosteric inhibitors targeting RhoA, which had been deemed as an “undruggable” protein target. This study reveals a novel allosteric regulatory site within the Rho family, which could be exploited for anti‐metastasis drug development, and also provides a novel strategy for inhibitor discovery toward “undruggable” proteins.