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Related Concept Videos

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...
Multi-pass Transmembrane Proteins and β-barrels01:09

Multi-pass Transmembrane Proteins and β-barrels

In multi-pass transmembrane proteins, the polypeptide chain crosses the membrane more than once. The transmembrane polypeptide chain either forms an α-helix or β-strand structure. α-Helix containing multi-pass transmembrane proteins are ubiquitous, whereas β-strand containing ones are mainly found in gram-negative bacteria, mitochondria, and chloroplasts.
α-Helix containing multi-pass transmembrane proteins
Multi-pass transmembrane proteins such as G-protein-linked receptors (GPCRs) 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...
Insertion of Multi-pass Transmembrane Proteins in the RER01:29

Insertion of Multi-pass Transmembrane Proteins in the RER

The rough ER membrane synthesizes, assembles, and embeds transmembrane proteins in diverse topologies. These proteins function as transporters or channels and can remain in the ER membrane or are sent to the Golgi complex, lysosome, and cell membrane.
The multipass transmembrane proteins are the type IV integral membrane proteins with multiple topogenic sequences determining their spatial arrangement in the ER membrane. Nearly all multipass proteins lack a cleavable signal sequence and use...
Types of Receptors: Cell Surface Receptors01:28

Types of Receptors: Cell Surface Receptors

Cell-surface receptors, also known as transmembrane receptors, are cell surface, membrane-anchored (integral) proteins that bind to external ligand molecules. This type of receptor spans the plasma membrane and performs signal transduction, converting an extracellular signal into an intracellular signal. Ligands that interact with cell-surface receptors do not have to enter the cell that they affect. Cell-surface receptors are also called cell-specific proteins or markers because they are...

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Related Experiment Video

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

Seven transmembrane receptors: something old, something new.

R J Lefkowitz1

  • 1Department of Medicine, Howard Hughes Medical Institute, Duke University Medical Center, Durham, NC 27710, USA. lefko001@receptor-biol.duke.edu

Acta Physiologica (Oxford, England)
|April 13, 2007
PubMed
Summary

This research details the discovery and understanding of G protein-coupled receptors (GPCRs), vital cell signaling proteins and drug targets. It covers their identification, mechanisms, and conserved nature across a large receptor superfamily.

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Transmembrane Domain Oligomerization Propensity determined by ToxR Assay
06:45

Transmembrane Domain Oligomerization Propensity determined by ToxR Assay

Published on: May 26, 2011

Assaying Surface Expression of Chemosensory Receptors in Heterologous Cells
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Assaying Surface Expression of Chemosensory Receptors in Heterologous Cells

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Cellular receptors regulate physiological processes but their existence was debated 40 years ago.
  • G protein-coupled receptors (GPCRs) are the largest receptor class and key drug targets.
  • Adrenergic receptors were among the first GPCRs to be studied.

Purpose of the Study:

  • To provide a personal retrospective on the research leading to the understanding of GPCRs.
  • To highlight the discovery and characterization of adrenergic receptors.
  • To elucidate the mechanisms of GPCR signaling and regulation.

Main Methods:

  • Identification, purification, and cloning of adrenergic receptors.
  • Comparative analysis of receptor structures, including homology with rhodopsin.
  • Investigation of receptor desensitization and signaling pathways involving G protein-coupled receptor kinases and beta-arrestins.

Main Results:

  • Adrenergic receptors were identified, purified, and cloned.
  • Homology between adrenergic receptors and rhodopsin revealed a large family of GPCRs.
  • Molecular mechanisms of GPCR desensitization and signaling were elucidated.
  • Conserved structure, signaling, and regulatory mechanisms across the GPCR superfamily were appreciated.

Conclusions:

  • GPCRs are fundamental to cellular activity and physiological regulation.
  • The study of adrenergic receptors paved the way for understanding the broader GPCR superfamily.
  • GPCR signaling and regulation mechanisms are highly conserved, offering insights into drug development and disease treatment.