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Epigenetic Regulation

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 Regulation

Epigenetic Regulation

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

Drug Discovery: Overview

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...

Structure-Activity Relationships and Drug Design

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...

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Related Experiment Video

Updated: Jun 4, 2026

In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing

In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing

Published on: May 5, 2023

Computer- and structure-based lead design for epigenetic targets.

Ralf Heinke¹, Luca Carlino, Srinivasaraghavan Kannan

¹Department of Pharmaceutical Chemistry, Martin-Luther University of Halle-Wittenberg, 06120 Halle/Saale, Germany.

Bioorganic & Medicinal Chemistry

|February 15, 2011

Summary

This summary is machine-generated.

Epigenetic modifications, like DNA methylation, influence traits without altering genes. This review covers small molecule inhibitors targeting histone-modifying enzymes for drug discovery.

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Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers

Published on: September 20, 2018

Area of Science:

Biochemistry
Molecular Biology
Pharmacology

Background:

Epigenetics involves inheritable changes influencing phenotype without altering the genome.
Key epigenetic mechanisms include DNA methylation and posttranslational histone modifications.
Aberrant epigenetic marks are implicated in various diseases, driving demand for enzyme inhibitors.

Purpose of the Study:

To review progress in identifying small molecule epigenetic inhibitors.
To focus on inhibitors targeting histone-modifying enzymes.
To highlight structure- and computer-based drug discovery approaches.

Main Methods:

Structure-based drug design.
Computer-aided drug design (CADD).
Literature review of identified small molecule inhibitors.

Main Results:

Emerging research on reversible histone methylation inhibitors.
Progress in structure- and computer-based identification of epigenetic inhibitors.
Identification of small molecules targeting histone-modifying enzymes.

Conclusions:

Small molecule inhibitors targeting epigenetic modifications show therapeutic potential.
Structure- and computer-based approaches are effective for discovering epigenetic drugs.
Further research into histone methylation inhibitors is crucial for drug discovery.