From G-Protein-Coupled Receptors to Designer Receptors Exclusively Activated by Designer Drugs

2021 ◽  
pp. 1-26
Author(s):  
Emmanouil Perakis
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
Designer Drugs ◽  
G Protein Coupled

Engineered GPCRs as Tools to Modulate Signal Transduction

Physiology ◽  
2008 ◽  
Vol 23 (6) ◽  
pp. 313-321 ◽  
Author(s):  
Ying Pei ◽  
Sarah C. Rogan ◽  
Feng Yan ◽  
Bryan L. Roth
Keyword(s):  
Signal Transduction ◽  
Signaling Pathways ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
Designer Drugs ◽  
Modulate Signal ◽  
Synthetic Drug ◽  
G Protein Coupled

Different families of G-protein-coupled receptors (GPCRs) have been engineered to provide exclusive control over the activation of these receptors and thus to understand better the consequences of their signaling in vitro and in vivo. These engineered receptors, named RASSLs (receptors activated solely by synthetic ligands) and DREADDs (designer receptors exclusively activated by designer drugs), are insensitive to their endogenous ligands but can be activated by synthetic drug-like compounds. Currently, the existing RASSLs and DREADDs cover the Gi, Gq, and Gs signaling pathways. These modified GPCRs can be utilized as ideal tools to study GPCR functions selectively in specific cellular populations.

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