Issue 3, 2022

Chemogenetics of cell surface receptors: beyond genetic and pharmacological approaches

Abstract

Cell surface receptors transmit extracellular information into cells. Spatiotemporal regulation of receptor signaling is crucial for cellular functions, and dysregulation of signaling causes various diseases. Thus, it is highly desired to control receptor functions with high spatial and/or temporal resolution. Conventionally, genetic engineering or chemical ligands have been used to control receptor functions in cells. As the alternative, chemogenetics has been proposed, in which target proteins are genetically engineered to interact with a designed chemical partner with high selectivity. The engineered receptor dissects the function of one receptor member among a highly homologous receptor family in a cell-specific manner. Notably, some chemogenetic strategies have been used to reveal the receptor signaling of target cells in living animals. In this review, we summarize the developing chemogenetic methods of transmembrane receptors for cell-specific regulation of receptor signaling. We also discuss the prospects of chemogenetics for clinical applications.

Graphical abstract: Chemogenetics of cell surface receptors: beyond genetic and pharmacological approaches

Article information

Article type
Review Article
Submitted
07 Oct 2021
Accepted
20 Jan 2022
First published
27 Jan 2022
This article is Open Access
Creative Commons BY-NC license

RSC Chem. Biol., 2022,3, 269-287

Chemogenetics of cell surface receptors: beyond genetic and pharmacological approaches

Y. Miura, A. Senoo, T. Doura and S. Kiyonaka, RSC Chem. Biol., 2022, 3, 269 DOI: 10.1039/D1CB00195G

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