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Related Concept Videos

Drug Discovery: Overview01:26

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 Design01:28

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...
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
Modified-Release Drug Delivery Systems: Site-Targeted01:24

Modified-Release Drug Delivery Systems: Site-Targeted

Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
Principles of Drug Action01:24

Principles of Drug Action

Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...

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Related Experiment Video

Updated: Jun 15, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
06:26

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Published on: May 16, 2021

[Fragment-based drug discovery: concept and aim].

Daisuke Tanaka1

  • 1Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd, Japan. daisuke-tanaka@ds-pharma.co.jp

Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan
|March 2, 2010
PubMed
Summary

Fragment-Based Drug Discovery (FBDD) utilizes small molecule fragments for drug lead identification. This method excels at targeting challenging proteins where traditional screening fails, offering a complementary approach to drug discovery.

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NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode
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NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode

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Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
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Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

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Related Experiment Videos

Last Updated: Jun 15, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
06:26

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Published on: May 16, 2021

NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode
09:19

NMR-Based Fragment Screening in a Minimum Sample but Maximum Automation Mode

Published on: June 4, 2021

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
08:31

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Published on: December 1, 2020

Area of Science:

  • Drug discovery and medicinal chemistry.
  • Biophysical and chemical screening methodologies.
  • Lead identification and optimization.

Context:

  • Fragment-Based Drug Discovery (FBDD) is an emerging methodology distinct from conventional high-throughput screening (HTS).
  • FBDD employs small, weakly binding fragments (<300 Da) as starting points for drug development.
  • Advances in biophysical screening have made fragment screening practical and effective.

Purpose:

  • To introduce the fundamental concepts of Fragment-Based Drug Discovery (FBDD).
  • To discuss the advantages of FBDD compared to conventional drug discovery approaches.
  • To highlight FBDD's utility in identifying leads for challenging or 'undruggable' targets.

Summary:

  • FBDD involves biophysical screening of small fragments and chemistry-driven optimization from fragment hits to lead compounds.
  • Key advantages include focusing on weak but specific binding fragments and leveraging ligand efficiency for lead-likeness.
  • This approach has successfully identified leads for targets intractable by HTS.

Impact:

  • FBDD is emerging as a valuable complement to established drug discovery methodologies.
  • It offers a viable strategy for tackling previously undruggable targets.
  • Successful FBDD applications demonstrate its potential to expand the scope of drug development.