Related Experiment Video
Updated: Jul 19, 2025

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023
Thomas P Burris1, Ian Mitchelle S de Vera2, Isabelle Cote2
1University 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.
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.
More Related Videos
08:15Network Pharmacology and Validation of the Antidepressant Mechanisms of Qiangzhifang in a Chronic Restraint Stress-induced Depression Rat Model
Published on: June 6, 2025
13:18Network Pharmacology Prediction and Experimental Validation of Trichosanthes-Fritillaria thunbergii Action Mechanism Against Lung Adenocarcinoma
Published on: March 3, 2023
Related Concept Videos
Transducer Mechanism: Nuclear Receptors
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Signal Transduction: Overview
Typically, signal transduction involves three...
Co-activators and Co-repressors
Covalently Linked Protein Regulators
These groups modify specific amino acids in a protein....
NF-κB-dependent Signaling Pathway
NF-κB-dependent Signaling Mechanism
The...