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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

16.5K
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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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 Receptors01:21

G-protein Coupled Receptors

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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.
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GPCR Desensitization01:12

GPCR Desensitization

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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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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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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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Related Experiment Video

Updated: Jan 15, 2026

Peptide-based Identification of Functional Motifs and their Binding Partners
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Peptide-based Identification of Functional Motifs and their Binding Partners

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State-Specific Peptide Design Targeting G Protein-Coupled Receptors.

Yang Xue1, Hong Wang2, Jun Li1

  • 1Baidu Inc. NLP, Shenzhen 518000, China.

Journal of Chemical Information and Modeling
|October 11, 2025
PubMed
Summary
This summary is machine-generated.

We developed a state-specific peptide design pipeline for G protein-coupled receptors (GPCRs). This method efficiently creates targeted peptide agonists or antagonists for GPCRs, improving drug discovery.

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Last Updated: Jan 15, 2026

Peptide-based Identification of Functional Motifs and their Binding Partners
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Area of Science:

  • Pharmacology
  • Structural Biology
  • Drug Discovery

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets involved in numerous physiological processes.
  • Peptides offer advantages over small molecules for GPCR targeting due to higher affinity, selectivity, and potency.
  • GPCR conformational states (active/inactive) dictate ligand interactions, necessitating state-specific design strategies.

Purpose of the Study:

  • To develop an efficient, state-specific peptide design pipeline for GPCRs.
  • To enable the tailored design of peptide agonists or antagonists based on GPCR structural states.
  • To validate the pipeline by identifying novel peptides for specific GPCR targets.

Main Methods:

  • Developed a state-specific peptide design framework for GPCRs.
  • Utilized GPCR active and inactive conformational states for tailored peptide design.
  • Employed a state-specific folding model optimized for GPCR-peptide complexes to select high-potential peptides.

Main Results:

  • Successfully designed and identified peptide agonists and antagonists for the Apelin Receptor (APJR) and Growth Hormone Secretagogue Receptor (GHSR).
  • Identified a competitive inhibitor peptide for the Glucagon-Like Peptide-1 Receptor (GLP-1R).
  • Demonstrated the efficacy of the state-specific design pipeline in generating functional peptides.

Conclusions:

  • The developed pipeline provides an efficient strategy for state-specific peptide design targeting GPCRs.
  • This approach facilitates the discovery of novel peptide therapeutics with improved specificity and potency.
  • The findings open new avenues for peptide-based drug development for various GPCRs.