Related Experiment Video
Updated: May 27, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Constitutive androstane receptor (CAR) is a xenosensor and target for therapy
E M Kachaylo1, V O Pustylnyak, V V Lyakhovich
1Institute of Molecular Biology and Biophysics, Siberian Division of the Russian Academy of Medical Sciences, Novosibirsk, Russia.
Abstract:
Constitutive androstane receptor (CAR, NR1I3), which is under consideration in this review, is a member of the superfamily of nuclear receptors. However, certain features distinguish CAR from the variety of nuclear receptors. First, this receptor has structural features that allow it to display constitutive activity in the absence of a ligand and to interact in a species-specific manner with a huge number of ligands diverse in chemical structure and origin. Second, recently many researchers are focused on CAR because the significance is increasingly shown of its influence on a variety of physiological functions, such as gluconeogenesis, metabolism of xenobiotics, fatty acids, bilirubin, and bile acids, hormonal regulation, etc. In addition to the fundamental scientific interest, the study of CAR is of practical importance because changes in CAR activity can lead to disorders in physiological processes, which finally can result in changes in pathological states. However, despite intensive studies, many mechanisms are still unclear, which makes it difficult to understand the role of CAR in the overall picture of molecular regulation of physiological processes. This review analyzes the features and diversity of the functions of CAR.
Insights
The constitutive androstane receptor (CAR) is a nuclear receptor with unique ligand interactions and broad physiological roles. Understanding CAR
Area of Science:
- Pharmacology and Toxicology
- Molecular Biology
- Endocrinology
Background:
- The constitutive androstane receptor (CAR, NR1I3) is a nuclear receptor with unique structural and functional properties.
- CAR exhibits constitutive activity and interacts with diverse ligands in a species-specific manner.
- CAR plays a significant role in various physiological functions, including metabolism and hormonal regulation.
Purpose of the Study:
- To review the distinct features of CAR compared to other nuclear receptors.
- To analyze the diverse functions of CAR in physiological processes.
- To highlight the significance of CAR in both fundamental science and practical medicine.
Main Methods:
- Literature review of existing studies on CAR.
- Analysis of CAR's structural features and ligand interactions.
- Synthesis of information on CAR's physiological roles and pathological implications.
Main Results:
- CAR possesses unique structural characteristics enabling ligand-independent activity and broad ligand binding.
- CAR significantly influences gluconeogenesis, xenobiotic metabolism, and bile acid homeostasis.
- Dysregulation of CAR activity is linked to various pathological conditions.
Conclusions:
- CAR is a crucial regulator of diverse physiological processes with significant implications for health and disease.
- Further research is needed to elucidate the complex mechanisms underlying CAR's functions.
- Understanding CAR's role is vital for developing therapeutic strategies targeting metabolic and other disorders.
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:
Internal Receptors
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
GPCRs Regulate Adenylyl Cylase Activity
Two...
Signal Transduction: Overview
Typically, signal transduction involves three...
The Two-State Receptor Model
The binding affinity of a drug determines its interaction with one...
