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G-protein Coupled Receptors

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.

Thermosensation

Thermosensation

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...

G-protein Coupled Receptors

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 Receptors

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 Receptors

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...

Spare Receptors

Spare Receptors

Some receptors remain unoccupied even when an agonist produces a maximal response. Such empty ones are called spare receptors. In presence of spare receptors the maximum effect of an agonist drug is achieved with fewer than 100% of the receptors being occupied. To determine the presence of spare receptors, scientists often compare the concentration of the drug needed to produce 50% of the maximum effect (EC50) with the concentration of the drug needed to occupy 50% of the receptors (Kd). If the...

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Related Experiment Video

Updated: Jun 28, 2026

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4

Published on: December 31, 2013

TRPV6.

U Wissenbach¹, B A Niemeyer

¹Experimentelle und Klinische Pharmakologie und Toxikologie, Medizinische Fakultät, Universität des Saarlandes, 66421 Homburg, Germany. ulrich.wissenbach@uniklinikum-saarland.de

Handbook of Experimental Pharmacology

|January 16, 2007

Summary

This summary is machine-generated.

The epithelial calcium channel TRPV6 is regulated by vitamin D and intracellular calcium. Its dysregulation is linked to prostate cancer progression.

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Expression and Purification of the Human Lipid-sensitive Cation Channel TRPC3 for Structural Determination by Single-particle Cryo-electron Microscopy

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Published on: January 7, 2019

Area of Science:

Biochemistry
Molecular Biology
Physiology

Background:

TRPV6 (Transient Receptor Potential Vanilloid 6) is an epithelial calcium channel crucial for calcium transport in organs like the intestine, kidney, and placenta.
TRPV6 expression is transcriptionally regulated by 1,25-dihydroxyvitamin D (the active form of vitamin D3) and other calcium-dependent and vitamin D3-independent pathways.
The TRPV6 channel exhibits high calcium selectivity and undergoes complex inactivation mediated by intracellular calcium and magnesium ions.

Purpose of the Study:

To summarize the known functions and regulation of the TRPV6 ion channel.
To highlight the role of TRPV6 in calcium homeostasis and its potential involvement in disease.
To review the transcriptional regulation and channel conductance properties of TRPV6.

Main Methods:

Literature review of existing studies on TRPV6 function, regulation, and expression.
Analysis of data pertaining to TRPV6's role in calcium transport and its transcriptional control.
Examination of evidence linking TRPV6 to pathological conditions, including cancer.

Main Results:

TRPV6 is a key epithelial calcium channel involved in high-demand calcium transport organs.
Transcriptional regulation of TRPV6 is influenced by vitamin D and intracellular calcium levels.
Altered TRPV6 regulation in tissues like the prostate is associated with malignant transformation and cancer progression.

Conclusions:

TRPV6 plays a vital role in physiological calcium absorption and homeostasis.
The complex regulation of TRPV6 by vitamin D and calcium highlights its importance in cellular function.
TRPV6 represents a potential therapeutic target in cancers, particularly prostate cancer, due to its link to disease progression.