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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.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
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Nuclear Export of mRNA02:31

Nuclear Export of mRNA

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Before mRNAs are exported to the cytoplasm, it is crucial to check each mRNA for structural and functional integrity. Eukaryotic cells use several different mechanisms, collectively known as mRNA surveillance, to look for irregularities in mRNAs. Irregular or aberrant mRNA are rapidly degraded by various enzymes. If a defective mRNA escapes the surveillance, it would be translated into a protein which would either be non-functional or not function properly. One of the primary irregularities in...
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Nuclear Stability03:18

Nuclear Stability

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Protons and neutrons, collectively called nucleons, are packed together tightly in a nucleus. With a radius of about 10−15 meters, a nucleus is quite small compared to the radius of the entire atom, which is about 10−10 meters. Nuclei are extremely dense compared to bulk matter, averaging 1.8 × 1014 grams per cubic centimeter. If the earth’s density were equal to the average nuclear density, the earth’s radius would be only about 200 meters.
To hold positively charged protons together...
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Nuclear Fusion02:45

Nuclear Fusion

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The process of converting very light nuclei into heavier nuclei is also accompanied by the conversion of mass into large amounts of energy, a process called fusion. The principal source of energy in the sun is a net fusion reaction in which four hydrogen nuclei fuse and ultimately produce one helium nucleus and two positrons.
A helium nucleus has a mass that is 0.7% less than that of four hydrogen nuclei; this lost mass is converted into energy during the fusion. This reaction produces about...
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Internal Receptors01:31

Internal Receptors

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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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Non-nuclear Inheritance01:29

Non-nuclear Inheritance

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Most DNA resides in the nucleus of a cell. However, some organelles in the cell cytoplasm⁠—such as chloroplasts and mitochondria⁠—also have their own DNA. These organelles replicate their DNA independently of the nuclear DNA of the cell in which they reside. Non-nuclear inheritance describes the inheritance of genes from structures other than the nucleus.
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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
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Development of Nuclear Receptor Modulators.

Simone Schierle1, Daniel Merk2

  • 1Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Frankfurt, Germany.

Methods in Molecular Biology (Clifton, N.J.)
|July 25, 2018
PubMed
Summary
This summary is machine-generated.

Nuclear receptors are promising drug targets, but developing small molecule ligands requires careful consideration of binding affinity, nuclear localization, and transactivation. This chapter introduces nuclear receptor ligand development strategies and characterization methods.

Keywords:
Drug discoveryFarnesoid X receptorMedicinal chemistryNuclear receptorsReporter gene assayTransactivation assay

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Area of Science:

  • Pharmacology
  • Molecular Biology
  • Drug Discovery

Background:

  • The nuclear receptor superfamily comprises 49 members, presenting numerous opportunities for pharmacological intervention.
  • While some nuclear receptors are established drug targets, many lack identified ligands, highlighting a gap in therapeutic development.
  • Developing small molecule modulators for nuclear receptors is complex, necessitating high-affinity binding, correct nuclear localization, and effective transactivation modulation.

Purpose of the Study:

  • To provide a comprehensive overview of nuclear receptors as drug targets.
  • To outline strategies for identifying and optimizing small molecule ligands for nuclear receptors.
  • To detail in vitro methods for characterizing nuclear receptor modulators.

Main Methods:

  • Summarizing the characteristics of nuclear receptors as a target family.
  • Describing hit and lead identification strategies.
  • Presenting a variety of in vitro characterization methods for nuclear receptor modulators.
  • Detailing an example optimization of a nuclear receptor modulator.
  • Highlighting hybrid reporter gene assays for flexible in vitro characterization.

Main Results:

  • The chapter provides a foundational understanding of nuclear receptor ligand development.
  • It equips researchers with strategies for hit and lead identification.
  • It details essential in vitro characterization techniques for assessing modulator efficacy and properties.

Conclusions:

  • Nuclear receptors represent a significant and largely untapped resource for drug discovery.
  • Effective development of nuclear receptor-targeting drugs requires a multifaceted approach encompassing target properties and ligand characteristics.
  • The presented strategies and methods facilitate the advancement of nuclear receptor ligand development for therapeutic applications.