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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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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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Related Experiment Video

Updated: Jun 21, 2026

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library
10:17

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library

Published on: January 14, 2020

Ligand discovery using encoded combinatorial libraries.

D S Tan1, J J Burbaum

  • 1Department of Chemistry and Chemical Biology, Institute of Chemistry and Cell Biology, Harvard University, Cambridge, MA 02138, USA. dstan@slsiris.harvard.edu

Current Opinion in Drug Discovery & Development
|August 4, 2009
PubMed
Summary
This summary is machine-generated.

Solid-phase synthesis generates large molecule libraries for drug discovery. Encoding methods track molecular identities, enabling efficient ligand identification and optimization for biological applications.

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Area of Science:

  • Medicinal Chemistry
  • Chemical Biology
  • Drug Discovery

Background:

  • Solid-phase combinatorial synthesis enables the creation of extensive molecular libraries.
  • Encoding techniques are crucial for tracking the identity of synthesized compounds.
  • Ligand discovery is a critical process in pharmaceutical research.

Purpose of the Study:

  • To provide an overview of solid-phase combinatorial synthesis for library generation.
  • To discuss the application of these libraries in ligand discovery.
  • To compare this approach with alternative methods.

Main Methods:

  • Utilizing split-pool or direct divide methods for solid-phase synthesis.
  • Employing encoding techniques to identify synthesized molecules.
  • Performing biological assays on- or off-solid support.

Main Results:

  • Successful generation of large, complex molecular libraries.
  • Readily determined identities of synthesized products through encoding.
  • Numerous examples of successful ligand discovery reported.

Conclusions:

  • Solid-phase synthesis with encoding is a powerful strategy for ligand discovery.
  • Libraries can be tailored for different screening purposes (discovery, targeted, optimization).
  • This methodology facilitates the identification of molecules with desired biological activity or receptor binding.