title: Ubiquitylation of nuclear receptors: new linkages and therapeutic implications.
abstract: The nuclear receptor (NR) superfamily is a group of transcriptional regulators that control multiple aspects of both physiology and pathology and are broadly recognized as viable therapeutic targets. While receptor-modulating drugs have been successful in many cases, the discovery of new drug targets is still an active area of research, because resistance to NR-targeting therapies remains a significant clinical challenge. Many successful targeted therapies have harnessed the control of receptor activity by targeting events within the NR signaling pathway. In this review, we explore the role of NR ubiquitylation and discuss how the expanding roles of ubiquitin could be leveraged to identify additional entry points to control receptor function for future therapeutic development.
authors.affiliation: McArdle Laboratory for Cancer ResearchDepartment of Oncology, 6151 Wisconsin Institutes for Medical Research, University of Wisconsin Carbone Cancer Center, University of Wisconsin-Madison, 1111 Highland Avenue, Madison, Wisconsin 53705, USA.
authors.forename: Kyle T
authors.initials: KT
authors.lastname: Helzer
authors.affiliation: McArdle Laboratory for Cancer ResearchDepartment of Oncology, 6151 Wisconsin Institutes for Medical Research, University of Wisconsin Carbone Cancer Center, University of Wisconsin-Madison, 1111 Highland Avenue, Madison, Wisconsin 53705, USA.
authors.forename: Christopher
authors.initials: C
authors.lastname: Hooper
authors.affiliation: McArdle Laboratory for Cancer ResearchDepartment of Oncology, 6151 Wisconsin Institutes for Medical Research, University of Wisconsin Carbone Cancer Center, University of Wisconsin-Madison, 1111 Highland Avenue, Madison, Wisconsin 53705, USA.
authors.forename: Shigeki
authors.initials: S
authors.lastname: Miyamoto
authors.affiliation: McArdle Laboratory for Cancer ResearchDepartment of Oncology, 6151 Wisconsin Institutes for Medical Research, University of Wisconsin Carbone Cancer Center, University of Wisconsin-Madison, 1111 Highland Avenue, Madison, Wisconsin 53705, USA alarid@oncology.wisc.edu.
authors.forename: Elaine T
authors.initials: ET
authors.lastname: Alarid
mesh_terms: D000818:Animals; D005786:Gene Expression Regulation; D006801:Humans; D058990:Molecular Targeted Therapy; D010766:Phosphorylation; D055550:Protein Stability; D059748:Proteolysis; D018160:Receptors, Cytoplasmic and Nuclear / Q000378:metabolism*; D015398:Signal Transduction; D025801:Ubiquitin / Q000378:metabolism; D044767:Ubiquitin-Protein Ligases / Q000502:physiology; D054875:Ubiquitination
chemical_list: D018160:Receptors, Cytoplasmic and Nuclear; D025801:Ubiquitin; D044767:Ubiquitin-Protein Ligases
keywords: E3 ligase; NF-κB; proteasome; steroid