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Related Concept Videos

Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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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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Enzyme-linked Receptors01:00

Enzyme-linked Receptors

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Enzyme-linked receptors are proteins that act as both receptor and enzyme, activating multiple intracellular signals. This is a large group of receptors that include the receptor tyrosine kinase (RTK) family. Many growth factors and hormones bind to and activate the RTKs.
Neurotrophin (NT) receptors are a family of RTKs, including trkA, trkB, and trkC (tropomyosin-related kinase) receptors. TrkA is specific for nerve growth factor (NGF), neurotrophin-6, and neurotrophin-7. TrkB binds...
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Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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Thermosensation01:43

Thermosensation

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Peripheral thermosensation is the perception of external temperature. A change in temperature (on the surface of the skin and other tissues) is detected by a family of temperature-sensitive ion channels called Transient Receptor Potential, or TRP, receptors. These receptors are located on free nerve endings. Those detecting cold temperatures are closer to the surface of the skin than the nerve endings detecting warmth. These thermoTRP channels, while temperature selective, have relatively...
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G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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.
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Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

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Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
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In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease.

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Treatment with HC-070, a potent inhibitor of TRPC4 and TRPC5, leads to anxiolytic and antidepressant effects in mice.

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Related Experiment Video

Updated: Feb 22, 2026

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
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Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b

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TRP Channels as Potential Drug Targets.

Magdalene M Moran1

  • 1Hydra Biosciences, Cambridge, Massachusetts 02138, USA;

Annual Review of Pharmacology and Toxicology
|September 26, 2017
PubMed
Summary

Transient Receptor Potential (TRP) channels are crucial for cellular function and implicated in genetic diseases. Pharmaceutical research is actively targeting these TRP channels for therapeutic interventions.

Area of Science:

  • Ion channel research
  • Molecular biology
  • Pharmacology

Background:

  • Transient Receptor Potential (TRP) channels are a diverse superfamily of cation channels.
  • These channels form tetramers and regulate ion flux, impacting cellular excitability and calcium homeostasis.
  • TRP channel dysfunction is linked to various genetic disorders affecting skeletal, skin, sensory, ocular, cardiac, and nervous systems.

Purpose of the Study:

  • To review the rationale for targeting TRP channels in drug discovery.
  • To provide an overview of the current status of pharmaceutical efforts focused on TRP channels.

Main Methods:

  • Review of existing scientific literature on TRP channel function and disease association.
  • Analysis of clinical trial data for compounds targeting specific TRP channels.
Keywords:
TRP channelTRPA1TRPV4drug discoverygenetic disorders

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Controllable Ion Channel Expression through Inducible Transient Transfection
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Related Experiment Videos

Last Updated: Feb 22, 2026

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
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Main Results:

  • TRP channels are critical regulators of cellular processes.
  • Mutations in TRP channels lead to a wide spectrum of diseases.
  • Several TRP channel modulators, including those targeting TRPV1, TRPV3, TRPV4, TRPA1, and TRPM8, have advanced to clinical trials.

Conclusions:

  • TRP channels represent significant targets for pharmaceutical intervention due to their role in disease.
  • Ongoing drug discovery efforts show promise for developing novel therapeutics for TRP channel-related conditions.