Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Protein-protein Interfaces02:04

Protein-protein Interfaces

Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a polypeptide...
Protein-Protein Interfaces02:04

Protein-Protein Interfaces

Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a polypeptide...
Protein Networks02:26

Protein Networks

An organism can have thousands of different proteins, and these proteins must cooperate to ensure the health of an organism. Proteins bind to other proteins and form complexes to carry out their functions. Many proteins interact with multiple other proteins creating a complex network of protein interactions.
These interactions can be represented through maps depicting protein-protein interaction networks, represented as nodes and edges. Nodes are circles that are representative of a protein,...
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...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

High-Throughput Screening of Potent Drug-like Molecules Targeting 17β-HSD10 for the Treatment of Alzheimer's Disease and Cancer.

ACS chemical biology·2025
Same author

Synthesis and Structure-Activity Relationships of N-(4-Benzamidino)-Oxazolidinones: Potent and Selective Inhibitors of Kallikrein-Related Peptidase 6.

ChemMedChem·2019
Same author

Structure-based design, synthesis and biological evaluation of a novel series of isoquinolone and pyrazolo[4,3-c]pyridine inhibitors of fascin 1 as potential anti-metastatic agents.

Bioorganic & medicinal chemistry letters·2019
Same author

In Vitro Assay Development and HTS of Small-Molecule Human ABAD/17β-HSD10 Inhibitors as Therapeutics in Alzheimer's Disease.

SLAS discovery : advancing life sciences R & D·2017
Same author

The importance of triaging in determining the quality of output from high-throughput screening.

Future medicinal chemistry·2015
Same author

A novel small-molecule MRCK inhibitor blocks cancer cell invasion.

Cell communication and signaling : CCS·2014

Related Experiment Video

Updated: May 21, 2026

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

Using fragment-based technologies to target protein-protein interactions.

Justin F Bower1, Andrew Pannifer

  • 1Drug Discovery Programme, Beatson Institute for Cancer Research, Garscube Estate, Bearsden, Glasgow. j.bower@beatson.gla.ac.uk

Current Pharmaceutical Design
|June 2, 2012
PubMed
Summary

Fragment-based screening is emerging as a powerful tool for discovering protein-protein interaction inhibitors. This review covers key technologies, case studies, and strategies for selecting diverse fragment libraries to advance drug discovery.

More Related Videos

Workflow and Tools for Crystallographic Fragment Screening at the Helmholtz-Zentrum Berlin
06:29

Workflow and Tools for Crystallographic Fragment Screening at the Helmholtz-Zentrum Berlin

Published on: March 3, 2021

Genome-wide Protein-protein Interaction Screening by Protein-fragment Complementation Assay (PCA) in Living Cells
08:38

Genome-wide Protein-protein Interaction Screening by Protein-fragment Complementation Assay (PCA) in Living Cells

Published on: March 3, 2015

Related Experiment Videos

Last Updated: May 21, 2026

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

Workflow and Tools for Crystallographic Fragment Screening at the Helmholtz-Zentrum Berlin
06:29

Workflow and Tools for Crystallographic Fragment Screening at the Helmholtz-Zentrum Berlin

Published on: March 3, 2021

Genome-wide Protein-protein Interaction Screening by Protein-fragment Complementation Assay (PCA) in Living Cells
08:38

Genome-wide Protein-protein Interaction Screening by Protein-fragment Complementation Assay (PCA) in Living Cells

Published on: March 3, 2015

Area of Science:

  • Drug Discovery
  • Medicinal Chemistry
  • Biochemistry

Background:

  • Fragment-based screening (FBS) is established for target-based drug discovery.
  • Its application in targeting protein-protein interactions (PPIs) is nascent.
  • PPI inhibitors are crucial for treating various diseases.

Purpose of the Study:

  • To review technologies for identifying fragment hits against PPI targets.
  • To highlight existing fragment-based PPI case studies.
  • To discuss the potential of FBS in PPI inhibitor discovery and fragment library design.

Main Methods:

  • Nuclear Magnetic Resonance (NMR) spectroscopy.
  • Surface Plasmon Resonance (SPR) imaging.
  • X-ray crystallography.
  • Biochemical screening assays.

Main Results:

  • FBS has demonstrated utility in identifying initial 'hits' for drug development.
  • Several case studies showcase FBS for PPI targets, though the field is young.
  • Optimization of fragment libraries is key for broader chemical space coverage.

Conclusions:

  • Fragment-based screening holds significant promise for developing novel PPI inhibitors.
  • Further development in fragment library design and screening technologies is needed.
  • This approach can uncover high-quality hit molecules for challenging drug targets.