Potent synthetic and endogenous ligands for the adopted orphan nuclear receptor Nurr1
- Title
- Potent synthetic and endogenous ligands for the adopted orphan nuclear receptor Nurr1
- Author
- 장용우
- Issue Date
- 2021-01
- Publisher
- SPRINGERNATURE
- Citation
- EXPERIMENTAL AND MOLECULAR MEDICINE, v. 53, no. 1, page. 19-29
- Abstract
- Until recently, Nurr1 (NR4A2) was known as an orphan nuclear receptor without a canonical ligand-binding domain, featuring instead a narrow and tight cavity for small molecular ligands to bind. In-depth characterization of its ligand-binding pocket revealed that it is highly dynamic, with its structural conformation changing more than twice on the microsecond-to-millisecond timescale. This observation suggests the possibility that certain ligands are able to squeeze into this narrow space, inducing a conformational change to create an accessible cavity. The cocrystallographic structure of Nurr1 bound to endogenous ligands such as prostaglandin E1/A1 and 5,6-dihydroxyindole contributed to clarifying the crucial roles of Nurr1 and opening new avenues for therapeutic interventions for neurodegenerative and/or inflammatory diseases related to Nurr1. This review introduces novel endogenous and synthetic Nurr1 agonists and discusses their potential effects in Nurr1-related diseases.
- URI
- https://www.nature.com/articles/s12276-021-00555-5https://repository.hanyang.ac.kr/handle/20.500.11754/176280
- ISSN
- 1226-3613; 2092-6413
- DOI
- 10.1038/s12276-021-00555-5
- Appears in Collections:
- COLLEGE OF MEDICINE[S](의과대학) > MEDICINE(의학과) > Articles
- Files in This Item:
- Potent synthetic and endogenous ligands for the adopted orphan nuclear receptor Nurr1.pdfDownload
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