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Related Concept Videos

Epigenetic Regulation01:37

Epigenetic Regulation

Epigenetic changes alter the physical structure of the DNA without changing the genetic sequence and often regulate whether genes are turned on or off. This regulation ensures that each cell produces only proteins necessary for its function. For example, proteins that promote bone growth are not produced in muscle cells. Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
X-chromosome...
Epigenetic Regulation01:46

Epigenetic Regulation

Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
Epigenetic Regulation01:46

Epigenetic Regulation

Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
Regulation of Expression at Multiple Steps01:23

Regulation of Expression at Multiple Steps

The gene expression in cells is regulated at different stages: (i) transcription, (ii) RNA processing, (iii) RNA localization, and (iv) translation. Transcriptional regulation is mediated by regulatory proteins such as transcription factors, activators, or repressors—these control gene expression by initiating or inhibiting the transcription of genes. Once a precursor or pre-mRNA is produced, it undergoes post-transcriptional modification, including 5' capping, splicing, and the addition of a...
Combinatorial Gene Control02:33

Combinatorial Gene Control

Combinatorial gene control is the synergistic action of several transcriptional factors to regulate the expression of a single gene. The absence of one or more of these factors may lead to a significant difference in the level of gene expression or repression.
The expression of more than 30,000 genes is controlled by approximately 2000-3000 transcription factors. This is possible because a single transcription factor can recognize more than one regulatory sequence. The specificity in gene...
Regulation of Expression Occurs at Multiple Steps02:24

Regulation of Expression Occurs at Multiple Steps

Gene expression can be regulated at almost every step from gene to protein. Transcription is the step that is most commonly regulated. This involves the binding of proteins to short regulatory sequences on the DNA. This association can either promote or inhibit the transcription of a gene associated with the respective sequence.
Transcription results in the generation of precursor (pre-mRNA) that consists of both exons and introns, which needs further processing before being translated to a...

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Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
10:28

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers

Published on: September 20, 2018

Epigenetic multiple modulators.

Rosana Álvarez1, Lucia Altucci, Hinrich Gronemeyer

  • 1Departamento de Química Orgánica, Universidade de Vigo, 36310 VIGO, ES, Spain.

Current Topics in Medicinal Chemistry
|November 2, 2011
PubMed
Summary
This summary is machine-generated.

Designed epigenetic multiple ligands offer advantages over traditional therapies by targeting multiple epigenetic enzymes simultaneously. This approach promises reduced drug interactions and resistance for complex diseases.

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Area of Science:

  • Epigenetics
  • Pharmacology
  • Medicinal Chemistry

Background:

  • The development of single chemical entities targeting multiple epigenetic enzymes simultaneously is an emerging field.
  • Current strategies involve combining existing drug pharmacophores or designing novel compounds with multi-target activities.
  • These designed epigenetic multiple ligands offer potential advantages in treating multifactorial diseases.

Purpose of the Study:

  • To review the current landscape of designed epigenetic multiple ligands.
  • To discuss the advantages of using single entities to modulate multiple epigenetic targets.
  • To outline structure-based principles for designing effective and selective multiple epigenetic ligands.

Main Methods:

  • Review of existing literature on epigenetic drugs and multi-target ligands.
  • Analysis of structure-activity relationships for compounds targeting multiple epigenetic enzymes.
  • Discussion of design strategies and optimization principles for multiple epigenetic ligands.

Main Results:

  • Designed epigenetic multiple ligands present conceptual advantages including reduced drug-drug interactions, minimized resistance, exploited pathway synergies, and lower effective concentrations.
  • Significant challenges remain in achieving high selectivity and efficiency while avoiding off-target effects.
  • The rational design of these ligands is complex but crucial for therapeutic success.

Conclusions:

  • Single chemical entities modulating multiple epigenetic targets offer a promising therapeutic strategy for complex diseases.
  • Overcoming design challenges related to selectivity and off-target effects is key to realizing the full potential of these ligands.
  • Further research into structure-based design principles is essential for advancing this field.