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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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Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
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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.
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Related Experiment Video

Updated: May 6, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Methods to accelerate PROTAC drug discovery.

Jeyan Osman^1,2, Philip E Thompson¹, Manuela Jörg^1,3

¹Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia.

The Biochemical Journal

|June 26, 2025

Summary

This summary is machine-generated.

Proteolysis-targeting chimeras (PROTACs) offer a new way to study diseases and find drugs. This review highlights key strategies to speed up PROTAC development for better drug discovery.

Keywords:

DNA-encoded library click chemistry direct-to-biology proteolysis-targeting chimeras solid-phase synthesis

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Last Updated: May 6, 2026

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A Fluorescence-based Protocol for Preliminary Screening of Protein Synthesis Inhibitors from Natural Sources

A Fluorescence-based Protocol for Preliminary Screening of Protein Synthesis Inhibitors from Natural Sources

Published on: January 27, 2026

Area of Science:

Biochemistry
Medicinal Chemistry
Drug Discovery

Background:

Proteolysis-targeting chimeras (PROTACs) are a novel therapeutic modality.
PROTACs leverage the cell's ubiquitin-proteasome system for targeted protein degradation.
The complexity of PROTACs presents challenges in their design and synthesis.

Purpose of the Study:

To review critical areas for accelerating PROTAC development.
To identify strategies for overcoming PROTAC design and synthesis challenges.
To enhance the efficiency of PROTAC-based drug discovery programs.

Main Methods:

Focus on appropriate target selection for protein degradation.
Emphasize modular chemical synthesis approaches for PROTACs.
Utilize high-throughput biological assays for PROTAC evaluation.

Main Results:

Streamlined development pathways for PROTACs.
Increased success rates in PROTAC-based discovery.
Facilitated understanding of PROTAC mechanisms and applications.

Conclusions:

Strategic target selection, synthesis, and evaluation are crucial for PROTAC advancement.
Optimized methodologies can accelerate the development of novel PROTAC therapeutics.
PROTAC technology holds significant promise for future drug discovery.