International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023

Thomas P Burris¹, Ian Mitchelle S de Vera², Isabelle Cote², Colin A Flaveny², Udayanga S Wanninayake², Arindam Chatterjee², John K Walker², Nickolas Steinauer², Jinsong Zhang², Laurel A Coons², Kenneth S Korach², Derek W Cain², Anthony N Hollenberg², Paul Webb², Douglas Forrest², Anton M Jetten², Dean P Edwards², Sandra L Grimm², Sean Hartig², Carol A Lange², Jennifer K Richer², Carol A Sartorius², Marc Tetel², Cyrielle Billon², Bahaa Elgendy², Lamees Hegazy², Kristine Griffett², Nahuel Peinetti², Kerry L Burnstein², Travis S Hughes², Sadichha Sitaula², Keitch R Stayrook², Alexander Culver², Meghan H Murray², Brian N Finck², John A Cidlowski²

Affiliations

¹ University of Florida Genetics Institute, Gainesville, Florida (T.P.B., I.C.); Department of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri (I.M.S.d.V., U.S.W., A.C., J.K.W., N.S., J.Z.); Pfizer, San Diego, California (C.A.F.); Receptor Biology Section, Reproductive and Developmental Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina (L.A.C., K.S.K.); Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, North Carolina (L.A.C.); Duke Human Vaccine Institute, Durham, North Carolina (D.W.C.); Department of Medicine, Boston University Chobanian and Avedisian School of Medicine, Boston, Massachusetts (A.N.H.); The California Institute of Regenerative Medicine, South San Francisco, California (P.W.); Laboratory of Endocrinology and Receptor Biology, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (D.G.); National Institute of Environmental Health Sciences, National Institutes of Health, Durham, North Carolina (A.M.J.); Department of Molecular and Cellular Pharmacology, Baylor College of Medicine, Houston, Texas (D.P.E., S.L.G., S.H.); Department of Medicine, Division of Hematology, Oncology and Transplantation, University of Minnesota, Minneapolis, Minnesota (C.A.L.); Department of Pathology, University of Colorado, Aurora, Colorado (J.K.R., C.A.S.); Neuroscience Program, Wellesley College, Wellesley, Massachusetts (M.T.); Center for Clinical Pharmacology, University of Health Sciences and Pharmacy, Saint Louis, Missouri (C.B., B.E., L.H.); Department of Anatomy, Physiology, and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, Alabama (K.G.); Department of Molecular and Cellular Pharmacology, University of Miami School of Medicine, Miami, Florida (N.P., K.L.B.); Department of Biomedical and Pharmaceutical Sciences, Center for Biomolecular Structure and Dynamics, University of Montana, Missoula, Montana (T.S.H.); Asteroid Therapeutics, Inc. Indianapolis, Indiana (S.S., K.R.S., A.C.); Saint Louis University School of Medicine, St. Louis, Missouri (M.H.M.); Department of Medicine, Washington University School of Medicine, St. Louis, Missouri (B.N.F.); and Signal Transduction Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, North Carolina (J.A.C.) burris.thomas@ufl.edu.
² University of Florida Genetics Institute, Gainesville, Florida (T.P.B., I.C.); Department of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri (I.M.S.d.V., U.S.W., A.C., J.K.W., N.S., J.Z.); Pfizer, San Diego, California (C.A.F.); Receptor Biology Section, Reproductive and Developmental Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina (L.A.C., K.S.K.); Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, North Carolina (L.A.C.); Duke Human Vaccine Institute, Durham, North Carolina (D.W.C.); Department of Medicine, Boston University Chobanian and Avedisian School of Medicine, Boston, Massachusetts (A.N.H.); The California Institute of Regenerative Medicine, South San Francisco, California (P.W.); Laboratory of Endocrinology and Receptor Biology, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (D.G.); National Institute of Environmental Health Sciences, National Institutes of Health, Durham, North Carolina (A.M.J.); Department of Molecular and Cellular Pharmacology, Baylor College of Medicine, Houston, Texas (D.P.E., S.L.G., S.H.); Department of Medicine, Division of Hematology, Oncology and Transplantation, University of Minnesota, Minneapolis, Minnesota (C.A.L.); Department of Pathology, University of Colorado, Aurora, Colorado (J.K.R., C.A.S.); Neuroscience Program, Wellesley College, Wellesley, Massachusetts (M.T.); Center for Clinical Pharmacology, University of Health Sciences and Pharmacy, Saint Louis, Missouri (C.B., B.E., L.H.); Department of Anatomy, Physiology, and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, Alabama (K.G.); Department of Molecular and Cellular Pharmacology, University of Miami School of Medicine, Miami, Florida (N.P., K.L.B.); Department of Biomedical and Pharmaceutical Sciences, Center for Biomolecular Structure and Dynamics, University of Montana, Missoula, Montana (T.S.H.); Asteroid Therapeutics, Inc. Indianapolis, Indiana (S.S., K.R.S., A.C.); Saint Louis University School of Medicine, St. Louis, Missouri (M.H.M.); Department of Medicine, Washington University School of Medicine, St. Louis, Missouri (B.N.F.); and Signal Transduction Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, North Carolina (J.A.C.).

PMID: 37586884
PMCID: PMC10595025
DOI: 10.1124/pharmrev.121.000436

Review

International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023

Thomas P Burris et al. Pharmacol Rev. 2023 Nov.

. 2023 Nov;75(6):1233-1318.

doi: 10.1124/pharmrev.121.000436. Epub 2023 Aug 16.

Authors

Affiliations

¹ University of Florida Genetics Institute, Gainesville, Florida (T.P.B., I.C.); Department of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri (I.M.S.d.V., U.S.W., A.C., J.K.W., N.S., J.Z.); Pfizer, San Diego, California (C.A.F.); Receptor Biology Section, Reproductive and Developmental Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina (L.A.C., K.S.K.); Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, North Carolina (L.A.C.); Duke Human Vaccine Institute, Durham, North Carolina (D.W.C.); Department of Medicine, Boston University Chobanian and Avedisian School of Medicine, Boston, Massachusetts (A.N.H.); The California Institute of Regenerative Medicine, South San Francisco, California (P.W.); Laboratory of Endocrinology and Receptor Biology, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (D.G.); National Institute of Environmental Health Sciences, National Institutes of Health, Durham, North Carolina (A.M.J.); Department of Molecular and Cellular Pharmacology, Baylor College of Medicine, Houston, Texas (D.P.E., S.L.G., S.H.); Department of Medicine, Division of Hematology, Oncology and Transplantation, University of Minnesota, Minneapolis, Minnesota (C.A.L.); Department of Pathology, University of Colorado, Aurora, Colorado (J.K.R., C.A.S.); Neuroscience Program, Wellesley College, Wellesley, Massachusetts (M.T.); Center for Clinical Pharmacology, University of Health Sciences and Pharmacy, Saint Louis, Missouri (C.B., B.E., L.H.); Department of Anatomy, Physiology, and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, Alabama (K.G.); Department of Molecular and Cellular Pharmacology, University of Miami School of Medicine, Miami, Florida (N.P., K.L.B.); Department of Biomedical and Pharmaceutical Sciences, Center for Biomolecular Structure and Dynamics, University of Montana, Missoula, Montana (T.S.H.); Asteroid Therapeutics, Inc. Indianapolis, Indiana (S.S., K.R.S., A.C.); Saint Louis University School of Medicine, St. Louis, Missouri (M.H.M.); Department of Medicine, Washington University School of Medicine, St. Louis, Missouri (B.N.F.); and Signal Transduction Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, North Carolina (J.A.C.) burris.thomas@ufl.edu.
² University of Florida Genetics Institute, Gainesville, Florida (T.P.B., I.C.); Department of Pharmacology and Physiology, Saint Louis University School of Medicine, Saint Louis, Missouri (I.M.S.d.V., U.S.W., A.C., J.K.W., N.S., J.Z.); Pfizer, San Diego, California (C.A.F.); Receptor Biology Section, Reproductive and Developmental Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina (L.A.C., K.S.K.); Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, North Carolina (L.A.C.); Duke Human Vaccine Institute, Durham, North Carolina (D.W.C.); Department of Medicine, Boston University Chobanian and Avedisian School of Medicine, Boston, Massachusetts (A.N.H.); The California Institute of Regenerative Medicine, South San Francisco, California (P.W.); Laboratory of Endocrinology and Receptor Biology, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland (D.G.); National Institute of Environmental Health Sciences, National Institutes of Health, Durham, North Carolina (A.M.J.); Department of Molecular and Cellular Pharmacology, Baylor College of Medicine, Houston, Texas (D.P.E., S.L.G., S.H.); Department of Medicine, Division of Hematology, Oncology and Transplantation, University of Minnesota, Minneapolis, Minnesota (C.A.L.); Department of Pathology, University of Colorado, Aurora, Colorado (J.K.R., C.A.S.); Neuroscience Program, Wellesley College, Wellesley, Massachusetts (M.T.); Center for Clinical Pharmacology, University of Health Sciences and Pharmacy, Saint Louis, Missouri (C.B., B.E., L.H.); Department of Anatomy, Physiology, and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, Alabama (K.G.); Department of Molecular and Cellular Pharmacology, University of Miami School of Medicine, Miami, Florida (N.P., K.L.B.); Department of Biomedical and Pharmaceutical Sciences, Center for Biomolecular Structure and Dynamics, University of Montana, Missoula, Montana (T.S.H.); Asteroid Therapeutics, Inc. Indianapolis, Indiana (S.S., K.R.S., A.C.); Saint Louis University School of Medicine, St. Louis, Missouri (M.H.M.); Department of Medicine, Washington University School of Medicine, St. Louis, Missouri (B.N.F.); and Signal Transduction Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, North Carolina (J.A.C.).

PMID: 37586884
PMCID: PMC10595025
DOI: 10.1124/pharmrev.121.000436

Abstract

The NR superfamily comprises 48 transcription factors in humans that control a plethora of gene network programs involved in a wide range of physiologic processes. This review will summarize and discuss recent progress in NR biology and drug development derived from integrating various approaches, including biophysical techniques, structural studies, and translational investigation. We also highlight how defective NR signaling results in various diseases and disorders and how NRs can be targeted for therapeutic intervention via modulation via binding to synthetic lipophilic ligands. Furthermore, we also review recent studies that improved our understanding of NR structure and signaling. SIGNIFICANCE STATEMENT: Nuclear receptors (NRs) are ligand-regulated transcription factors that are critical regulators of myriad physiological processes. NRs serve as receptors for an array of drugs, and in this review, we provide an update on recent research into the roles of these drug targets.

U.S. Government work not protected by U.S. copyright.

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Figures

**Fig. 1**
The human nuclear receptor superfamily and its classification into groups.

See this image and copyright information in PMC

References

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International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023

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International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023

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