Lee Hyeong-Min, Giguere Patrick M, Roth Bryan L
Department 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.
Department 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.
Drug Discov Today. 2014 Apr;19(4):469-73. doi: 10.1016/j.drudis.2013.10.018. Epub 2013 Nov 1.
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.
自从首个仅由设计药物特异性激活的设计受体(DREADDs)发明以来,这些工程化的G蛋白偶联受体(GPCRs)已广泛应用于生物过程和行为的研究中。DREADD技术已成为一种具有巨大药物发现和开发潜力的强大工具。DREADDs有助于确定可成药靶点,并使研究人员能够探索针对已知和孤儿GPCRs的新型药物的活性。在此,我们讨论DREADDs如何用作药物发现和开发的新型工具。