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Related Concept Videos

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...
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...
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...
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...
GPCR Desensitization01:12

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...

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Related Experiment Video

Updated: Jun 23, 2026

Identifying the Binding Proteins of Small Ligands with the Differential Radial Capillary Action of Ligand Assay (DRaCALA)
09:26

Identifying the Binding Proteins of Small Ligands with the Differential Radial Capillary Action of Ligand Assay (DRaCALA)

Published on: March 19, 2021

Structural insight into PPARgamma ligands binding.

A Farce1, N Renault, P Chavatte

  • 1Laboratoire de Chimie Thérapeutique, EA1043, Faculté des Sciences Pharmaceutiques et Biologiques, 3 rue du Professeur Laguesse, BP 83, 59006 Lille Cedex, France.

Current Medicinal Chemistry
|May 16, 2009
PubMed
Summary

Peroxisome proliferator-activated receptors (PPARs) are key targets for metabolic syndrome. Research clarifies PPARgamma agonist binding modes, informing the development of novel therapeutic compounds.

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Modeling Ligands into Maps Derived from Electron Cryomicroscopy
09:30

Modeling Ligands into Maps Derived from Electron Cryomicroscopy

Published on: July 19, 2024

Related Experiment Videos

Last Updated: Jun 23, 2026

Identifying the Binding Proteins of Small Ligands with the Differential Radial Capillary Action of Ligand Assay (DRaCALA)
09:26

Identifying the Binding Proteins of Small Ligands with the Differential Radial Capillary Action of Ligand Assay (DRaCALA)

Published on: March 19, 2021

Modeling Ligands into Maps Derived from Electron Cryomicroscopy
09:30

Modeling Ligands into Maps Derived from Electron Cryomicroscopy

Published on: July 19, 2024

Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors crucial for metabolic homeostasis.
  • Their role in lipid and glucose regulation makes them therapeutic targets for metabolic syndrome.

Purpose of the Study:

  • To elucidate the binding modes of PPARgamma agonists.
  • To understand the structural basis for PPARgamma-mediated drug action.

Main Methods:

  • Analysis of crystallographic data for PPAR-ligand complexes.
  • Structure-activity relationship studies of PPAR modulator compounds.

Main Results:

  • PPAR agonists typically exhibit a three-module structure: binder, linker, and effector.
  • Agonist binding involves specific hydrogen bonds and interactions within the Ligand Binding Domain (LBD).
  • Structural variations led to drug classes like glitazones and glitazars, with ongoing research into phthalates.

Conclusions:

  • Understanding PPARgamma binding modes is essential for designing effective metabolic syndrome therapies.
  • Structural insights guide the pharmacomodulation of PPAR agonists.
  • Diverse chemical structures, including phthalates, warrant further investigation for PPAR activation.