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Review
. 2025 Mar 12;125(5):2665-2702.
doi: 10.1021/acs.chemrev.4c00582. Epub 2025 Feb 25.

Principles and Design of Molecular Tools for Sensing and Perturbing Cell Surface Receptor Activity

Jennifer Sescil  1   2 , Steven M Havens  1   2 , Wenjing Wang  1   2   3   4
Affiliations
Review

Principles and Design of Molecular Tools for Sensing and Perturbing Cell Surface Receptor Activity

Jennifer Sescil et al. Chem Rev. .

Abstract

Cell-surface receptors are vital for controlling numerous cellular processes with their dysregulation being linked to disease states. Therefore, it is necessary to develop tools to study receptors and the signaling pathways they control. This Review broadly describes molecular approaches that enable 1) the visualization of receptors to determine their localization and distribution; 2) sensing receptor activation with permanent readouts as well as readouts in real time; and 3) perturbing receptor activity and mimicking receptor-controlled processes to learn more about these processes. Together, these tools have provided valuable insight into fundamental receptor biology and helped to characterize therapeutics that target receptors.

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Conflict of interest statement

Conflict of Interests

The authors have no conflicts of interests.

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References

    1. Cooper G. The Cell: A Molecular Approach. ; Sinauer Associates, 2000.
    1. Sjulson L; Cassataro D; DasGupta S; Miesenbock G Cell-Specific Targeting of Genetically Encoded Tools for Neuroscience. Annu Rev Genet 2016, 50, 571–594. DOI: 10.1146/annurev-genet-120215-035011. - DOI - PMC - PubMed
    1. Wacker D; Stevens RC; Roth BL How Ligands Illuminate GPCR Molecular Pharmacology. Cell 2017, 170 (3), 414–427. DOI: 10.1016/j.cell.2017.07.009. - DOI - PMC - PubMed
    1. Weis WI; Kobilka BK The Molecular Basis of G Protein-Coupled Receptor Activation. Annu Rev Biochem 2018, 87, 897–919. DOI: 10.1146/annurev-biochem-060614-033910. - DOI - PMC - PubMed
    1. Syrovatkina V; Alegre KO; Dey R; Huang XY Regulation, Signaling, and Physiological Functions of G-Proteins. J Mol Biol 2016, 428 (19), 3850–3868. DOI: 10.1016/j.jmb.2016.08.002. - DOI - PMC - PubMed

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