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Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
Therapeutic Drug Monitoring: Overview and Classification01:16

Therapeutic Drug Monitoring: Overview and Classification

Therapeutic Drug Monitoring (TDM) is a clinical practice that measures specific drug levels in a patient's blood at designated intervals to ensure the drug concentration stays within a therapeutic range. This monitoring is crucial for optimizing individual dosage regimens, enhancing therapeutic efficacy, and minimizing drug-related toxicity. TDM is vital for drugs with narrow therapeutic windows, significant variability in pharmacokinetics, and a clear correlation between plasma levels and...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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Patented TGR5 modulators: a review (2006 - present).

Antimo Gioiello1, Emiliano Rosatelli, Roberto Nuti

  • 1Dipartimento di Chimica e Tecnologia del Farmaco, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy. antimo@chimfarm.unipg.it

Expert Opinion on Therapeutic Patents
|October 9, 2012
PubMed
Summary
This summary is machine-generated.

TGR5 activation improves metabolic health and reduces inflammation in mice. Further research is needed to confirm these benefits and assess safety in humans for treating metabolic syndrome and liver diseases.

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Area of Science:

  • Pharmacology
  • Metabolic Diseases
  • Drug Discovery

Background:

  • TGR5 (G protein-coupled receptor) is central to bile acid signaling.
  • TGR5 activation enhances glycemic control, energy expenditure, and possesses anti-inflammatory effects.
  • TGR5 ligands are investigated for treating liver diseases and metabolic syndrome.

Purpose of the Study:

  • To review recent advances in TGR5 modulators.
  • To focus on patent applications and publications from the last six years.

Main Methods:

  • Literature review of peer-reviewed publications.
  • Analysis of patent applications related to TGR5 modulators.
  • Focus on research from the past 6 years.

Main Results:

  • TGR5 agonists demonstrated protective effects in mice against diabesity and insulin resistance.
  • TGR5 activation improved liver functions and attenuated atherosclerosis development in preclinical models.
  • Encouraging efficacy of TGR5 agonists observed in mouse models.

Conclusions:

  • TGR5 activation shows therapeutic potential for metabolic and inflammatory conditions in mice.
  • Human studies are required to validate TGR5 agonist efficacy and safety.
  • Development of selective TGR5 ligands is crucial for understanding its complex signaling network.