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Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

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Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
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Internal Receptors01:31

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Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
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Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

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Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
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Cell Signaling in Plants01:25

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Plant cells communicate to coordinate their cycle of growth, flowering and fruiting, and activities in roots, shoots, and leaves in response to the changing environmental conditions. Plant signaling is distinct from animal signaling. Plants primarily utilize enzyme-linked receptors, whereas the largest class of cell-surface receptors in animals are G-protein coupled receptors (GPCRs). Unlike animals, receptor tyrosine kinases are rare in plants. Instead, plants have a diverse class of...
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The Two-State Receptor Model01:29

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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
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Signal Transduction: Overview01:26

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Cells respond to many types of information, often through receptor proteins positioned on the membrane. They respond to chemical signals, such as hormones, neurotransmitters, and other signaling molecules, initiating a series of molecular reactions to produce an appropriate response. This is called signal transduction. Cells also coordinate different responses elicited by the same signaling molecule via mediators, allowing molecular cross-talk.
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Updated: Mar 29, 2026

Prediction and Validation of Gene Regulatory Elements Activated During Retinoic Acid Induced Embryonic Stem Cell Differentiation
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Advances in understanding aryl hydrocarbon receptor structure, function, and modulation.

Qinghong Shang1, Sepideh Khorasanizadeh2, Xiaotong Diao1

  • 1State Key Laboratory of Microbial Technology, Shandong University, Qingdao 266237, China.

Trends in Biochemical Sciences
|March 27, 2026
PubMed
Summary
This summary is machine-generated.

The aryl hydrocarbon receptor (AHR) is a key transcription factor in barrier tissues. Structural biology advances reveal AHR

Keywords:
PAS domainaryl hydrocarbon receptorbHLH–PAS familydrug discoveryligand-activated transcription factorprotein–ligand interaction

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Area of Science:

  • Molecular Biology
  • Structural Biology
  • Immunology

Background:

  • The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor crucial in barrier tissues.
  • AHR signaling diversity arises from ligand specificity and protein interactions.
  • AHR's role in sensing diverse chemical cues suggests therapeutic potential in autoimmune and oncological disorders.

Purpose of the Study:

  • To review recent structural biology breakthroughs in AHR function and modulation.
  • To highlight how structural insights redefine mechanistic understanding of AHR.
  • To guide strategies for pharmacological modulation of AHR in physiological and pathological contexts.

Main Methods:

  • Review of recent structural biology studies on AHR.
  • Analysis of AHR's ligand recognition, heterodimerization, and DNA binding.
  • Comparison of AHR with other bHLH-PAS family members.

Main Results:

  • Structural insights elucidate AHR's promiscuous ligand recognition.
  • Key aspects of AHR heterodimerization and DNA response element engagement are clarified.
  • Ligand-dependent AHR activation mechanisms are distinguished from other bHLH-PAS proteins.

Conclusions:

  • High-resolution structural data significantly advances our understanding of AHR.
  • These insights are crucial for developing targeted AHR-based therapies.
  • Structural biology is redefining AHR's role in health and disease.