GPCRRD: G protein-coupled receptor spatial restraint database for 3D structure modeling and function annotation.
1Center for Computational Medicine and Bioinformatics, University of Michigan, 100 Washtenaw Ave, Ann Arbor, MI 48109, USA.
Bioinformatics (Oxford, England)
|October 8, 2010
Summary
The GPCRRD database collects experimental data on G protein-coupled receptors (GPCRs), crucial drug targets. This resource aids in modeling GPCR structures and understanding their functions.
Area of Science:
- Biochemistry
- Structural Biology
- Pharmacology
Background:
- G protein-coupled receptors (GPCRs) are the largest family of integral membrane proteins.
- GPCRs represent a critical class of drug targets in medicine.
- Limited crystal structures exist for GPCRs, necessitating alternative methods for structural insights.
Purpose of the Study:
- To create the GPCRRD database for systematic collection of experimental restraints for GPCRs.
- To aid in the 3D structure modeling and functional annotation of GPCRs.
- To consolidate data from literature and primary resources using automated text mining and manual validation.
Main Methods:
- Automated text mining algorithms to extract experimental restraints from literature.
- Manual validation of extracted data for accuracy and reliability.
- Systematic collection of residue orientation, contact, and distance maps.
Main Results:
- The GPCRRD database now contains thousands of spatial restraints.
- Data is sourced from diverse experimental techniques including mutagenesis, disulfide mapping, cryo-EM, and FTIR spectroscopy.
- The database provides a comprehensive resource for GPCR structural studies.
Conclusions:
- The GPCRRD database is a valuable tool for GPCR 3D structure modeling.
- It facilitates functional annotation of GPCRs by providing experimental evidence.
- The database supports research on GPCRs as drug targets.
More Related Videos
Related Concept Videos
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...
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 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...
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 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...
GPCRs are also called heptahelical, 7TM, or...
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 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 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...


