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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...

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Updated: Oct 14, 2025

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

Drug discovery for epigenetics targets.

Geoffrey A Holdgate¹, Catherine Bardelle¹, Alice Lanne¹

¹High-throughput Screening, Discovery Sciences, BioPharmaceuticals R&D, AstraZeneca, Alderley Park, UK.

Drug Discovery Today

|November 3, 2021

Summary

This summary is machine-generated.

Epigenetic drug targets offer a promising therapeutic strategy for diseases like cancer and neurological disorders. This review details drug development, from target identification to clinical candidates, highlighting future potential.

Keywords:

Drug discovery Epigenetics Hit identification Optimisation

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Isolation of Specific Genomic Regions and Identification of Associated Molecules by enChIP

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Published on: January 20, 2016

Area of Science:

Biochemistry
Pharmacology
Genetics

Background:

Epigenetic dysregulation is implicated in major diseases, including cancer, autoimmune, cardiovascular, and neurological disorders.
Epigenetic proteins (readers, writers, erasers) are druggable targets for small-molecule inhibitors.
The reversible nature of epigenetic modifications makes pharmacological intervention an attractive therapeutic strategy.

Purpose of the Study:

To provide an overview of epigenetics drug targets.
To focus on approaches for initial hit identification in drug discovery.
To describe the role of structure-guided chemistry in optimizing drug candidates and highlight challenges and future potential for epigenetics-based therapies.

Main Methods:

Literature review of epigenetics drug targets and development strategies.
Analysis of approaches for initial hit identification.
Discussion of structure-guided chemistry optimization for clinical candidates.

Main Results:

Epigenetic drug targets are viable for therapeutic intervention across various diseases.
Small-molecule inhibitors targeting epigenetic proteins are a key focus in drug development.
Structure-guided chemistry plays a crucial role in advancing initial hits to clinical candidates.

Conclusions:

Epigenetics-based therapies represent a significant and evolving area in pharmaceutical research.
Continued research into epigenetic drug targets and development pathways holds substantial promise for treating complex diseases.
Overcoming current challenges is essential for realizing the full potential of epigenetics-based treatments.