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Related Concept Videos

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...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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:
Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Drug-Receptor Interactions01:29

Drug-Receptor Interactions

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.
The Two-State Receptor Model01:29

The Two-State Receptor Model

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 one...

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BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
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Dependence receptors: from basic research to drug development.

Patrick Mehlen1, Dale E Bredesen

  • 1Apoptose, Cancer et Développement, CNRS UMR5538, Centre Léon Bérard, University of Lyon, Lyon 69008, France. dbredesen@buckinstitute

Science Signaling
|January 27, 2011
PubMed
Summary
This summary is machine-generated.

New dependence receptors were identified, clarifying the switch between cell survival and death signaling. Research also explored dependence receptor roles in development, disease, and potential new therapies.

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Published on: February 20, 2018

Area of Science:

  • Molecular biology
  • Cell signaling
  • Neuroscience

Background:

  • Dependence receptors mediate cellular responses to trophic support, influencing cell survival and death.
  • The transition from trophic to apoptotic signaling is crucial in various physiological and pathological processes.
  • Understanding dependence receptor function is key to developing novel therapeutic strategies.

Purpose of the Study:

  • To present newly identified dependence receptors and their functions.
  • To elucidate the mechanisms underlying the switch between trophic and apoptotic signaling.
  • To discuss the in vivo roles of dependence receptors in development, disease, and potential therapeutic applications.

Main Methods:

  • Identification and characterization of novel dependence receptors.
  • Mechanistic studies on signal transduction pathways.
  • In vivo studies in models of development, angiogenesis, oncogenesis, and neurodegeneration.
  • Evaluation of therapeutic strategies targeting dependence receptors.

Main Results:

  • Discovery of previously unknown dependence receptors.
  • Detailed mechanistic insights into the switch between anti-apoptotic and pro-apoptotic signaling upon loss of trophic support.
  • Evidence for the involvement of antitrophins in the loss of trophic support.
  • In vivo data highlighting the roles of dependence receptors in development, angiogenesis, oncogenesis, and neurodegeneration.
  • Presentation of novel therapeutic approaches.

Conclusions:

  • Dependence receptors represent a critical signaling network with diverse roles.
  • The balance of dependence receptor signaling is vital for normal development and disease prevention.
  • Targeting dependence receptors offers promising therapeutic avenues for various conditions.