DREADDs: novel tools for drug discovery and development
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Updated: May 6, 2026

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System
Published on: December 11, 2016
Hyeong-Min Lee1, Patrick M Giguere1, Bryan L Roth1
1Department of Pharmacology, Program in Neuroscience, Division of Chemical Biology and Medicinal Chemistry, and NIMH Psychoactive Drug Screening Program, University of North Carolina, Chapel Hill Medical School, 4072 Genetic Medicine Building, Chapel Hill, NC 27514, USA.
Abstract:
Since the invention of the first designer receptors exclusively activated by designer drugs (DREADDs), these engineered G protein-coupled receptors (GPCRs) have been widely applied in investigations of biological processes and behaviors. DREADD technology has emerged as a powerful tool with great potential for drug discovery and development. DREADDs can facilitate the identification of druggable targets and enable researchers to explore the activities of novel drugs against both known and orphan GPCRs. Here, we discuss how DREADDs can be used as novel tools for drug discovery and development.
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