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Related Concept Videos

Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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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,...
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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.
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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Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

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Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
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Cholinergic Receptors: Muscarinic01:25

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The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. 
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+....
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The Two-State Receptor Model01:29

The Two-State Receptor Model

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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
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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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Related Experiment Video

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Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET
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Mouse and human FcR effector functions.

Pierre Bruhns1,2, Friederike Jönsson1,2

  • 1Unité des Anticorps en Thérapie et Pathologie, Département d'Immunologie, Institut Pasteur, Paris, France.

Immunological Reviews
|October 27, 2015
PubMed
Summary

Researchers explored Fc receptors (FcRs) using advanced mouse models. These models are crucial for understanding FcR functions and developing targeted therapies and engineered antibodies.

Keywords:
Fc receptorFcγRantibody-mediated diseaseantibody-mediated therapyhigh-affinity receptormouse models

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Area of Science:

  • Immunology
  • Pharmacology

Background:

  • Fc receptors (FcRs) are critical for immune responses and therapeutic antibody development.
  • Research has focused on FcR characterization, polymorphisms, and their role in disease.
  • FcRs are key targets for drug development and antibody engineering.

Purpose of the Study:

  • To review the current FcR family, their effector functions, and available in vivo models.
  • To highlight how in vivo models have redefined FcR properties and functions.
  • To address misconceptions about high-affinity IgG receptors and antibody engineering.

Main Methods:

  • Utilizing knockout mouse lines for individual and multiple FcRs.
  • Employing cell-specific FcR knockouts and human FcR transgenic models.
  • Analyzing data from in vivo studies to re-evaluate FcR roles.

Main Results:

  • In vivo models have been instrumental in uncovering previously overlooked FcR functions.
  • New insights into the properties and effector functions of FcRs have emerged.
  • Misconceptions regarding the role of high-affinity IgG receptors in vivo are being addressed.

Conclusions:

  • Advanced in vivo models are essential for a comprehensive understanding of FcR biology.
  • FcR research continues to drive innovation in therapeutic antibody design and immune-based therapies.
  • Accurate in vivo data is crucial for correcting past assumptions and advancing FcR-targeted strategies.