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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: 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...
G-protein Coupled Receptors01:21

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 Receptors01:21

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.
GPCR Desensitization01:12

GPCR Desensitization

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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Related Experiment Video

Updated: Jun 10, 2026

Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons
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An improved classification of G-protein-coupled receptors using sequence-derived features.

Zhen-Ling Peng1, Jian-Yi Yang, Xin Chen

  • 11Department of Electrical and Computer Engineering, University of Alberta, Edmonton, Alberta, T6G 2V4, Canada.

BMC Bioinformatics
|August 11, 2010
PubMed
Summary

This study introduces PCA-GPCR, a computational method to predict G-protein-coupled receptors (GPCRs) from protein sequences. PCA-GPCR achieves high accuracy in identifying and classifying GPCRs across five levels, aiding in drug discovery.

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Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons
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Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
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Area of Science:

  • Bioinformatics
  • Computational Biology
  • Genomics

Background:

  • G-protein-coupled receptors (GPCRs) are crucial drug targets, but their 3D structures are scarce.
  • A large number of GPCR primary sequences are available, necessitating computational prediction methods.

Purpose of the Study:

  • To develop an accurate computational method for predicting GPCRs from protein primary sequences.
  • To facilitate the identification and characterization of novel GPCRs.

Main Methods:

  • Proposed PCA-GPCR method utilizing 1497 sequence-derived features.
  • Principal Component Analysis (PCA) for feature space dimension reduction to 32.
  • Intimate sorting classification algorithm applied at five hierarchical levels.

Main Results:

  • PCA-GPCR achieved high prediction accuracies: 99.5% (level 1), 88.8% (level 2), 80.47% (level 3), 80.3% (level 4), and 92.34% (level 5).
  • Demonstrated superior performance compared to existing methods on independent datasets.
  • The method effectively predicts GPCRs and their classification into families, subfamilies, and subtypes.

Conclusions:

  • The 1497 features capture essential protein information (amino acid composition, sequence order, physicochemical properties).
  • PCA-GPCR provides a robust and accurate tool for GPCR prediction and classification.
  • The method holds significant potential for accelerating the discovery of novel GPCRs and drug candidates.