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Related Concept Videos

Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
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...
Ligand Binding and Linkage00:49

Ligand Binding and Linkage

Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked.  In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence the...
Ligand Binding and Linkage00:49

Ligand Binding and Linkage

Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked.  In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence the...

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Updated: Jun 24, 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 ligand discovery.

Marcus Fischer1, Roderick E Hubbard

  • 1York Structural Biology Laboratory, University of York, York YO105YW, UK.

Molecular Interventions
|March 21, 2009
PubMed
Summary
This summary is machine-generated.

Fragment-based ligand discovery is revolutionizing drug development. This modular approach uses chemical building blocks to evolve potential medicines, with several compounds already in clinical use.

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Last Updated: Jun 24, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
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Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Structural Biology

Background:

  • Modular design principles are increasingly applied across scientific disciplines.
  • High-throughput screening platforms are adapting diverse methodologies for drug discovery.
  • Fragment-based ligand discovery (FBLD) is an emerging strategy in pharmaceutical research.

Purpose of the Study:

  • To highlight the adaptation of modular design in drug discovery.
  • To explain the process and significance of fragment-based ligand discovery.
  • To underscore the growing acceptance of FBLD in identifying drug candidates.

Main Methods:

  • Utilizing Nuclear Magnetic Resonance (NMR) and X-ray crystallography.
  • Adapting techniques to high-throughput screening platforms.
  • Employing a wide array of methods to optimize fragment binding to target biomolecules.

Main Results:

  • Several drug compounds evolved from fragments have advanced to clinical trials.
  • FBLD demonstrates a viable pathway for identifying novel hit compounds.
  • The approach is increasingly recognized as a valuable tool in inhibitor design.

Conclusions:

  • Fragment-based ligand discovery represents a significant advancement in modern drug development.
  • The modular, evolutionary nature of FBLD allows for efficient optimization of drug candidates.
  • FBLD is becoming an indispensable strategy for pharmaceutical discovery and the design of targeted inhibitors.