Allosteric regulation of kinase activity in living cells

This concise review provides a clear and instructive picture of the state-of-the-art understanding of protein kinases' activity and sets of approaches and tools to analyse and regulate it.

Three major parts of the work include: methods to map allosteric communications, tools to control allostery, and allosteric regulation of protein kinases. The work provides an important and timely view of the current status of our understanding of the function of protein kinases and state-of-the-art methods to study its allosteric regulation and to develop allosteric approaches to control it.

The following is the authors’ response to the previous reviews

Comments from reviewer 1:

Comment 1. Regarding SBSMMA, the authors may complement their discussion by mentioning recent work (PMID: 35738428) where SBSMMA was used to exemplify a potential fragment-based design approach for developing allosteric effectors for kinases.

Thank you for the suggestion, we have added a short summary of the work where SBSMMA is used as a basis for developing small molecules to target kinases using fragment-based design approach