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Related Concept Videos

Allosteric Regulation01:08

Allosteric Regulation

60.8K
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...
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Cooperative Allosteric Transitions01:58

Cooperative Allosteric Transitions

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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...
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Allosteric Proteins-ATCase01:19

Allosteric Proteins-ATCase

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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...
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Ligand Binding and Linkage00:49

Ligand Binding and Linkage

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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...
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Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

3.1K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
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Covalently Linked Protein Regulators02:04

Covalently Linked Protein Regulators

7.8K
Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
These groups modify specific amino acids in a protein....
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Related Experiment Video

Updated: Oct 11, 2025

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation

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Wandering beyond small molecules: peptides as allosteric protein modulators.

Morgane Mannes1, Charlotte Martin1, Christel Menet2

  • 1Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, Brussels, Belgium.

Trends in Pharmacological Sciences
|December 3, 2021
PubMed
Summary

Peptide-based allosteric modulators offer a promising avenue for drug discovery, demonstrating high potency and selectivity. This study explores their application in modulating various protein targets for therapeutic development.

Keywords:
allosteric modulatorsdrug discoverypeptide therapeuticsprotein targets

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Related Experiment Videos

Last Updated: Oct 11, 2025

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library
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Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library

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Peptide-based Identification of Functional Motifs and their Binding Partners
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Peptide-based Identification of Functional Motifs and their Binding Partners

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Area of Science:

  • Pharmacology and Drug Discovery
  • Medicinal Chemistry
  • Biochemistry

Background:

  • Allosteric modulation has emerged as a key strategy in modern drug design, leading to several clinical candidates.
  • While small molecules have been extensively studied for allosteric modulation, particularly for membrane receptors, peptide-based modulators remain underexplored.
  • Peptides offer potential advantages in drug discovery due to their inherent high target potency and selectivity compared to small molecules.

Purpose of the Study:

  • To investigate the potential of peptide-based molecules as allosteric modulators for diverse protein targets.
  • To highlight the application of peptide allosteric modulators in drug discovery and development.
  • To explore the modulation of various protein classes, including G protein-coupled receptors and protein-protein interactions, using peptides.

Main Methods:

  • Exploration of peptide screening campaigns for identifying allosteric modulators.
  • Characterization of peptide interactions with target proteins.
  • Assessment of peptide-induced allosteric effects on protein function.

Main Results:

  • Demonstration of peptides as effective allosteric modulators across a range of protein targets.
  • Evidence of peptides' high potency and selectivity in modulating protein activity.
  • Successful application of peptide allosteric modulators in targeting G protein-coupled receptors and protein-protein interactions.

Conclusions:

  • Peptide-based allosteric modulators represent a significant and promising class of therapeutics.
  • These modulators can effectively target key biological pathways, offering new therapeutic strategies.
  • Further research into peptide allosteric modulators is warranted for advancing drug discovery.