The search is on for effective specific inhibitors for PI3Kα mutants. PI3Kα, a critical lipid
kinase, has two subunits, catalytic and inhibitory. PIK3CA, the gene that encodes the p110α …

Allostery is a universal, biological phenomenon in which orthosteric sites are fine‐tuned by
topologically distal allosteric sites triggered by perturbations, such as ligand binding, residue …

Missense mutations may affect proteostasis by destabilizing or over-stabilizing protein
complexes and changing the pathway flux. Predicting the effects of stabilizing mutations on …

Understanding molecular mechanisms underlying the complexity of allosteric regulation in
proteins has attracted considerable attention in drug discovery due to the benefits and …

Highlights•Allosteric drugs have become an indispensable tool in precision medicine.•Major
targets for allosteric drugs: diversity structures and functions.•Allosteric effects of mutations …

Here, we discuss the principles of allosteric activating mutations, propagation downstream of
the signals that they prompt, and allosteric drugs, with examples from the Ras signaling …

Highlights•Allosteric drug discovery is gaining increasing attention.•Allosteric drug-
resistance mutations hamper the application of allosteric drugs.•We review the emergence …

The AlloSigMA 2 server provides an interactive platform for exploring the allosteric signaling
caused by ligand binding and/or mutations, for analyzing the allosteric effects of mutations …

Driver mutations can contribute to the initial processes of cancer, and their identification is
crucial for understanding tumorigenesis as well as for molecular drug discovery and …

The interactions between residues in a protein tertiary structure can be studied effectively
using the approach of protein structure network (PSN). A PSN is a node-edge representation …