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Related Concept Videos

Internal Receptors01:31

Internal Receptors

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.
Co-activators and Co-repressors02:04

Co-activators and Co-repressors

Gene transcription is regulated by the synergistic action of several proteins that form a complex at a gene regulatory site. This is observed in eukaryotes, where the regulation of gene expression is a complex process. Regulatory proteins in eukaryotes can broadly be classified into two types – regulators that bind directly to specific DNA sequences and co-regulators that associate with regulatory proteins but cannot directly bind to the DNA. These co-regulators are further divided into...
Co-activators and Co-repressors02:04

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Gene transcription is regulated by the synergistic action of several proteins that form a complex at a gene regulatory site. This is observed in eukaryotes, where the regulation of gene expression is a complex process. Regulatory proteins in eukaryotes can broadly be classified into two types – regulators that bind directly to specific DNA sequences and co-regulators that associate with regulatory proteins but cannot directly bind to the DNA. These co-regulators are further divided into...
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.
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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:
The Two-State Receptor Model01:29

The Two-State Receptor Model

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.
The binding affinity of a drug determines its interaction with one...

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From ligand to response: generating diversity in nuclear receptor coregulator function.

N J McKenna1, B W O'Malley

  • 1Department of Molecular and Cellular Biology, Baylor College of Medicine, One Baylor Plaza, 77030, Houston, TX, USA.

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Summary

Nuclear receptor ligands control biological processes by activating nuclear receptors. Coactivators are key factors in this process, mediating the effects of these ligands and influencing gene expression.

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Area of Science:

  • Molecular Biology
  • Endocrinology
  • Genetics

Background:

  • Nuclear receptors are crucial intracellular proteins regulating gene expression.
  • Ligands binding to nuclear receptors modulate diverse physiological functions.
  • The precise mechanisms of nuclear receptor-mediated gene regulation are under investigation.

Purpose of the Study:

  • To review recent advancements in understanding nuclear receptor function.
  • To explore the role of coactivators in nuclear receptor signaling.
  • To discuss the pharmacological implications of coactivators in nuclear receptor ligand action.

Main Methods:

  • Literature review of recent studies on nuclear receptors and coactivators.
  • Analysis of mechanistic aspects of receptor-coactivator interactions.
  • Discussion of pharmacological relevance based on current research.

Main Results:

  • Nuclear receptors, upon activation by ligands, recruit diverse coactivator proteins.
  • Coactivators are essential for efficient transcriptional regulation by activated nuclear receptors.
  • These interactions form the basis for the complex pharmacology of nuclear receptor ligands.

Conclusions:

  • Coactivators play a central role in mediating the biological effects of nuclear receptor ligands.
  • Understanding coactivator function is critical for developing targeted therapies.
  • Further research into receptor-coactivator mechanisms will illuminate nuclear receptor pharmacology.