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

You might also read

Related Articles

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

Sort by
Same author

Uncovering the isoform-resolution kinetic landscape of nonsense-mediated mRNA decay with EZbakR.

Genome biology·2026
Same author

Chemoselective Halogenation of Premarineosin A for Next-Generation Antimalarial Development.

bioRxiv : the preprint server for biology·2026
Same author

A Hybrid Experimental and in silico Platform for ITPK1 Chemical Probe Discovery.

SLAS discovery : advancing life sciences R & D·2026
Same author

Integrating AI in Medicinal Chemistry for Accelerated Drug Discovery: A Comprehensive SAR (CSAR) Optimization Strategy and Discovery of Potent ALDH3A1 Inhibitors.

Journal of medicinal chemistry·2026
Same author

A fission yeast-based platform for nematode PDE inhibitor discovery.

Cellular signalling·2026
Same author

SELECTIVE ACTIVATION OF GIRK POTASSIUM CHANNELS REDUCES BEHAVIORAL AND BRAIN RESPONSES TO ETHANOL IN MICE.

bioRxiv : the preprint server for biology·2026

Related Experiment Video

Updated: Jan 10, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

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

11.8K

Cyclic peptides as ligands for competition binding assays.

Renier H P van Neer1, Patricia K Dranchak1, Abigail M Davis1

  • 1Division of Preclinical Innovation, National Center for Advancing Translational Sciences, NIH, Rockville, MD, United States.

Methods in Enzymology
|November 20, 2025
PubMed
Summary

Cyclic peptides are effective probes for high-throughput screening (HTS) assays, overcoming limitations in drug development. Researchers explore their use in challenging enzyme targets, demonstrating diverse assay formats for drug discovery.

Keywords:
Binding assayFluoresceinFluorescence polarizationIpglycermideLanthanideLaser scanning cytometryLigandLigand displacementTime-resolved fluorescencemRNA display

More Related Videos

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
07:11

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center

Published on: September 28, 2022

3.1K
An ELISA Based Binding and Competition Method to Rapidly Determine Ligand-receptor Interactions
08:40

An ELISA Based Binding and Competition Method to Rapidly Determine Ligand-receptor Interactions

Published on: March 14, 2016

20.1K

Related Experiment Videos

Last Updated: Jan 10, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

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

11.8K
Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
07:11

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center

Published on: September 28, 2022

3.1K
An ELISA Based Binding and Competition Method to Rapidly Determine Ligand-receptor Interactions
08:40

An ELISA Based Binding and Competition Method to Rapidly Determine Ligand-receptor Interactions

Published on: March 14, 2016

20.1K

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Cyclic peptides are discovered using nucleic acid-encoded libraries and affinity-based screening.
  • Poor pharmacokinetic properties limit cyclic peptide drug development but not their use as assay probes.
  • Cyclic peptides offer broad protein surface complementarity and straightforward discovery.

Purpose of the Study:

  • Discuss the discovery, characterization, and utilization of macrocyclic peptide ligands as assay probes.
  • Highlight the application of cyclic peptides in ligand-displacement assays for challenging protein targets.
  • Detail specific enzyme targets and assay formats for high-throughput screening (HTS).

Main Methods:

  • Discovery and characterization of macrocyclic peptide ligands.
  • Development and utilization of cyclic peptides as assay probes in ligand-displacement assays.
  • Application of eight different assay formats, including fluorescence binding, fluorescence polarization, laser scanning cytometry, HTRF, and NanoBRET.

Main Results:

  • Demonstrated the utility of cyclic peptides as assay probes for difficult targets like iPGM and *MtbCM.
  • Successfully employed various ligand-displacement assay formats for HTS.
  • Showcased the adaptability of cyclic peptides in diverse biochemical assay designs.

Conclusions:

  • Cyclic peptides are valuable tools for enabling HTS against challenging protein targets.
  • The described assay methodologies facilitate the screening of enzymes previously intractable for HTS.
  • Macrocyclic peptides serve as effective probes, advancing drug discovery screening capabilities.