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

Cooperative Allosteric Transitions01:58

Cooperative Allosteric Transitions

8.0K
Cooperative allosteric transitions can occur in multimeric proteins, where each subunit of the protein has its own ligand-binding site. When a ligand binds to any of these subunits, it triggers a conformational change that affects the binding sites in the other subunits; this can change the affinity of the other sites for their respective ligands. The ability of the protein to change the shape of its binding site is attributed to the presence of a mix of flexible and stable segments in the...
8.0K
Allosteric Regulation01:08

Allosteric Regulation

58.5K
Allosteric regulation of enzymes occurs when the binding of an effector molecule to a site that is different from the active site causes a change in the enzymatic activity. This alternate site is called an allosteric site, and an enzyme can contain more than one of these sites. Allosteric regulation can either be positive or negative, resulting in an increase or decrease in enzyme activity. Most enzymes that display allosteric regulation are metabolic enzymes involved in the degradation or...
58.5K
Allosteric Proteins-ATCase01:19

Allosteric Proteins-ATCase

5.8K
Binding sites linkages can regulate a protein's function.  For example, enzyme activity is often regulated through a feedback mechanism where the end product of the biochemical process serves as an inhibitor.
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to  N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis...
5.8K
Ligand Binding and Linkage00:49

Ligand Binding and Linkage

4.9K
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...
4.9K
Cooperative Binding of Transcription Regulators02:13

Cooperative Binding of Transcription Regulators

6.5K
Transcriptional regulators bind to specific cis-regulatory sequences in the DNA to regulate gene transcription. These cis-regulatory sequences are very short, usually less than ten nucleotide pairs in length. The short length means that there is a high probability of the exact same sequence randomly occurring throughout the genome.  Since regulators can also bind to groups of similar sequences, this further increases the chances of random binding. Transcriptional regulators form...
6.5K
The Equilibrium Binding Constant and Binding Strength02:18

The Equilibrium Binding Constant and Binding Strength

13.1K
The equilibrium binding constant (Kb) quantifies the strength of a protein-ligand interaction. Kb can be calculated as follows when the reaction is at equilibrium:
13.1K

You might also read

Related Articles

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

Sort by
Same author

COVID-19-Triggered Miller Fisher Syndrome Masking Leptomeningeal Progression of Merkel Cell Carcinoma: A Fatal Diagnostic Dilemma.

Cureus·2026
Same author

Rescue Inhaler Overuse in Severe Asthma: A Real-World Study of Short-Acting β<sub>2</sub>-Agonist and Short-Acting Muscarinic Antagonist Use.

Biomedicines·2026
Same author

Real-World Effectiveness of Tezepelumab Across T2 and Non-T2 Severe Asthma Phenotypes: A Multicenter Spanish Cohort Study.

Archivos de bronconeumologia·2026
Same author

In silico prediction of novel effective combinational treatment of chronic pain in individual patients: A joint white paper of the H2020 QSPainRelief consortium.

British journal of pharmacology·2026
Same author

A data-driven performance index for center forwards in the English Premier League.

Scientific reports·2026
Same author

How Different Physical Qualities Influence Repeated Sprint Ability Tests in Elite Youth Soccer Players?

Journal of human kinetics·2026
Same journal

From biologics to small-molecule modulators: The evolving landscape of interleukin-targeted therapeutics.

Drug discovery today·2026
Same journal

Targeting the GLP-1 receptor pathways for dual management of obesity and depression.

Drug discovery today·2026
Same journal

Chemical intervention strategies targeting MYC for cancer therapy.

Drug discovery today·2026
Same journal

How many protein pairs can we chemically target?

Drug discovery today·2026
Same journal

From trial-and-error to inverse design: how AI is redefining drug delivery systems.

Drug discovery today·2026
Same journal

Critical evaluation of the key mediators causing life-threatening symptoms during human anaphylaxis.

Drug discovery today·2026
See all related articles

Related Experiment Video

Updated: Aug 22, 2025

Bio-layer Interferometry for Measuring Kinetics of Protein-protein Interactions and Allosteric Ligand Effects
13:57

Bio-layer Interferometry for Measuring Kinetics of Protein-protein Interactions and Allosteric Ligand Effects

Published on: February 18, 2014

29.5K

Allosteric binding cooperativity in a kinetic context.

Óscar Díaz1, Victor Martín2, Pedro Renault1

  • 1Laboratory of Molecular Neuropharmacology and Bioinformatics, Unitat de Bioestadística and Institut de Neurociències, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain; Instituto de Salud Carlos III, Centro de Investigación Biomédica en Red de Salud Mental, CIBERSAM, Spain; Unitat de Neurociència Traslacional, Parc Taulí Hospital Universitari, Institut d'Investigació i Innovació Parc Taulí (I3PT), Institut de Neurociències, Universitat Autònoma de Barcelona, Spain.

Drug Discovery Today
|November 13, 2022
PubMed
Summary
This summary is machine-generated.

Allosteric modulators are key in drug discovery. Analyzing binding cooperativity

Keywords:
GPCRsallosteric modulationbinding cooperativitybinding kineticscooperativity rate constantheterodimer receptorrate constantresidence time

More Related Videos

The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis
19:16

The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis

Published on: March 17, 2010

20.7K
Determination of Protein-ligand Interactions Using Differential Scanning Fluorimetry
13:26

Determination of Protein-ligand Interactions Using Differential Scanning Fluorimetry

Published on: September 13, 2014

61.9K

Related Experiment Videos

Last Updated: Aug 22, 2025

Bio-layer Interferometry for Measuring Kinetics of Protein-protein Interactions and Allosteric Ligand Effects
13:57

Bio-layer Interferometry for Measuring Kinetics of Protein-protein Interactions and Allosteric Ligand Effects

Published on: February 18, 2014

29.5K
The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis
19:16

The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis

Published on: March 17, 2010

20.7K
Determination of Protein-ligand Interactions Using Differential Scanning Fluorimetry
13:26

Determination of Protein-ligand Interactions Using Differential Scanning Fluorimetry

Published on: September 13, 2014

61.9K

Area of Science:

  • Pharmacology and Drug Discovery
  • Biophysics
  • Biochemistry

Background:

  • Allosteric modulators regulate endogenous ligand binding and function, offering advantages over orthosteric ligands.
  • Binding cooperativity is a critical parameter in allosteric modulation, often yielding complex kinetic behaviors.
  • Understanding these kinetic behaviors is crucial for effective drug design.

Purpose of the Study:

  • To derive a relationship between kinetic parameters of binding cooperativity in allosteric modulation.
  • To explore how equilibrium binding cooperativity values can correspond to multiple kinetic parameter combinations.
  • To provide a framework for interpreting complex experimental results in allosteric drug discovery.

Main Methods:

  • Utilized two established receptor models: the allosteric ternary complex model and the heterodimer receptor model.
  • Derived a mathematical relationship connecting rate constant parameters of binding cooperativity.
  • Analyzed the implications of this relationship for interpreting equilibrium binding data.

Main Results:

  • A novel relationship for cooperativity rate constant parameters was established.
  • Demonstrated that a single equilibrium binding cooperativity value can arise from diverse combinations of kinetic parameters.
  • Highlighted the potential for unexpected kinetic behaviors underlying seemingly simple equilibrium measurements.

Conclusions:

  • The derived relationship offers a deeper understanding of allosteric modulation kinetics.
  • Facilitates the interpretation of complex experimental outcomes in allosteric systems.
  • Guides future research directions in allosteric drug discovery and modulator design.