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Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

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.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
Regulation of Nuclear Protein Sorting01:45

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Nuclear protein sorting regulates nucleus composition and gene expression, crucial for determining the fate of a eukaryotic cell. Hence, the entry and exit of molecules across the nuclear envelope is a tightly controlled process. Nuclear protein sorting can be inhibited by one of the following ways: 1) masking cargo signal sequences, 2) modifying the nuclear receptor's affinity for cargo, 3) controlling the nuclear pore size, 4) retaining the cargo during its transit to the cytosol or the...
Signal Transduction: Overview01:26

Signal Transduction: Overview

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.
Typically, signal transduction involves three...
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Intracellular Hormone Receptors01:08

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Types of Receptors: Internal Receptors01:07

Types of Receptors: Internal Receptors

Many cellular signals are hydrophilic and cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind intracellular receptors that reside within the cell cytoplasm or nucleus. Many mammalian steroid hormones and nitric oxide (NO) gas use this cell signaling mechanism.
Similar to membrane-bound receptors, the binding of a ligand to the intracellular receptor of causes a conformational change in the...

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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Insect nuclear receptors.

Susan E Fahrbach1, Guy Smagghe, Rodrigo A Velarde

  • 1Department of Biology, Wake Forest University, Winston-Salem, North Carolina 27109, USA. fahrbach@wfu.edu

Annual Review of Entomology
|October 25, 2011
PubMed
Summary
This summary is machine-generated.

Nuclear receptors (NRs) are key transcription factors in insects. The ecdysone receptor (EcR) is a target for developing safe pesticides and new medical technologies.

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Area of Science:

  • Molecular Biology
  • Genomics
  • Entomology

Background:

  • Nuclear receptors (NRs) are ancient transcription factors with DNA-binding domains (DBDs) and ligand-binding domains (LBDs).
  • Insect genomes, like Drosophila melanogaster, contain numerous NRs, with conserved structures but diverse functional roles.
  • Understanding insect NR isoforms is crucial for comprehending their roles in development, reproduction, and homeostasis.

Purpose of the Study:

  • To highlight the importance of functional analysis of insect nuclear receptor isoforms.
  • To emphasize the significance of the ecdysone receptor (EcR) in insect biology and pest control.
  • To introduce novel applications of EcR in gene-switch systems.

Main Methods:

  • Genomic analysis of nuclear receptors in insects.
  • Functional studies of insect nuclear receptor isoforms.
  • Development of nonsteroidal ecdysteroid agonists for EcR.

Main Results:

  • Identification of 18 canonical NRs and 3 DBD-only receptors in Drosophila.
  • Demonstration of EcR's role as the receptor for ecdysteroid molting hormones.
  • Development of nonsteroidal agonists targeting EcR for potential pesticide applications.

Conclusions:

  • Functional characterization of insect NRs is essential for understanding their diverse biological roles.
  • EcR-targeting compounds offer a promising avenue for developing safe and effective pesticides.
  • Chimeric, ligand-inducible gene-switch systems utilizing EcR have potential applications in pest management and medicine.