Allosteric regulation, i. e. the control exerted on an orthosteric site by an effector interacting at a distinct and distant site, represents a prime example of a precise tuning system of several key biological processes like gene transcription, cell adhesion and, most importantly, signal transduction. Since its discovery sixty years ago, the molecular mechanisms underlying this phenomenon have been extensively investigated. The aim of this minireview is to introduce the reader to the topic of protein allostery. In particular, we briefly overview the allosteric models postulated over the years and we describe the most relevant chemical and biophysical approaches reported so far for the identification of putative allosteric sites and/or for the investigation of allosteric signal propagation throughout the protein. An outlook of the main computational and experimental methods is followed by four case studies representative of different proteins classes: enzymes, hub proteins, cell receptors, and intrinsically disordered proteins.

Chemical and Biophysical Approaches to Allosteric Modulation / M. Civera, E. Moroni, L. Sorrentino, F. Vasile, S. Sattin. - In: EUROPEAN JOURNAL OF ORGANIC CHEMISTRY. - ISSN 1434-193X. - 2021:30(2021 Aug 13), pp. 4245-4259. [10.1002/ejoc.202100506]

Chemical and Biophysical Approaches to Allosteric Modulation

M. Civera
Primo
;
F. Vasile;S. Sattin
Ultimo
2021

Abstract

Allosteric regulation, i. e. the control exerted on an orthosteric site by an effector interacting at a distinct and distant site, represents a prime example of a precise tuning system of several key biological processes like gene transcription, cell adhesion and, most importantly, signal transduction. Since its discovery sixty years ago, the molecular mechanisms underlying this phenomenon have been extensively investigated. The aim of this minireview is to introduce the reader to the topic of protein allostery. In particular, we briefly overview the allosteric models postulated over the years and we describe the most relevant chemical and biophysical approaches reported so far for the identification of putative allosteric sites and/or for the investigation of allosteric signal propagation throughout the protein. An outlook of the main computational and experimental methods is followed by four case studies representative of different proteins classes: enzymes, hub proteins, cell receptors, and intrinsically disordered proteins.
Allostery; Molecular dynamics; Native mass spectrometry; NMR spectroscopy; X-ray crystallography
Settore CHIM/06 - Chimica Organica
1-giu-2021
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/887106
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