EMD-22283
cryo-EM of human GLP-1R bound to non-peptide agonist LY3502970
EMD-22283
Single-particle3.1 Å
Deposition: 07/07/2020
Map released: 18/11/2020
Last modified: 09/12/2020
Name: Cryo-EM structure of the Glucagon-like peptide-1 receptor in complex with G protein and a non-peptide agonist LY3502970
Summary:
- Complex
- Cryo-EM structure of the Glucagon-like peptide-1 receptor in complex with G protein and a non-peptide agonist LY3502970
- Glucagon-like peptide 1 receptor
- Trimeric stimulatory G protein
- Nanobody 35
- Single-chain variable fragment 16
- Protein
- Alpha subunit of Gs with N-terminus swapped with equivalent residues in Gi,Guanine nucleotide-binding protein G(s) subunit alpha isoforms XLas
- Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1
- single-chain variable fragment scFv16
- Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
- Nanobody 35
- Glucagon-like peptide 1 receptor
- Ligand
Cryo-EM structure of the Glucagon-like peptide-1 receptor in complex with G protein and a non-peptide agonist LY3502970
Name: Molecular weight
Experimental | Theoretical | Method |
---|---|---|
- | 150 kDa | - |
Glucagon-like peptide 1 receptor
Name: Natural source [1]
Organism: Homo sapiens
Recombinant Expression [1]
Organism | Strain | Cell | Plasmid |
---|---|---|---|
synthetic construct | - | - | - |
Trimeric stimulatory G protein
Name: Natural source [1]
Organism: Homo sapiens
Recombinant Expression [1]
Organism | Strain | Cell | Plasmid |
---|---|---|---|
Spodoptera frugiperda | - | - | - |
Nanobody 35
Name: Natural source [1]
Organism: Lama glama
Recombinant Expression [1]
Organism | Strain | Cell | Plasmid |
---|---|---|---|
Escherichia coli | - | - | - |
Single-chain variable fragment 16
Name: Natural source [1]
Organism: Mus musculus
Recombinant Expression [1]
Organism | Strain | Cell | Plasmid |
---|---|---|---|
Spodoptera frugiperda | - | - | - |
Alpha subunit of Gs with N-terminus swapped with equivalent residues in Gi,Guanine nucleotide-binding protein G(s) subunit alpha isoforms XLas
Number of copies: 1
UniProtKB PDBe-KB AlphaFold DB
Name: Number of copies: 1
UniProtKB PDBe-KB AlphaFold DB
Natural source
Organism: Homo sapiens
Molecular weight
Experimental | Theoretical | Method |
---|---|---|
- | 43 kDa | - |
Recombinant Expression
Organism | Strain | Cell | Plasmid |
---|---|---|---|
Trichoplusia ni | - | - | - |
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1
Number of copies: 1
UniProtKB PDBe-KB AlphaFold DB
Name: Number of copies: 1
UniProtKB PDBe-KB AlphaFold DB
Domains
Gene Ontology [25]
Biological process:
G protein-coupled acetylcholine receptor signaling pathway signal transduction G protein-coupled receptor signaling pathway sensory perception of taste adenylate cyclase-activating dopamine receptor signaling pathway phospholipase C-activating G protein-coupled receptor signaling pathway cellular response to prostaglandin E stimulus cellular response to catecholamine stimulus cell population proliferation retina development in camera-type eye Ras protein signal transduction
Molecular function:
protein-containing complex binding GTPase binding signaling receptor complex adaptor activity GTPase activity
Cellular location:
cytoplasm membrane synapse heterotrimeric G-protein complex extracellular exosome lysosomal membrane photoreceptor disc membrane extracellular vesicle cytosol plasma membrane
G protein-coupled acetylcholine receptor signaling pathway signal transduction G protein-coupled receptor signaling pathway sensory perception of taste adenylate cyclase-activating dopamine receptor signaling pathway phospholipase C-activating G protein-coupled receptor signaling pathway cellular response to prostaglandin E stimulus cellular response to catecholamine stimulus cell population proliferation retina development in camera-type eye Ras protein signal transduction
Molecular function:
protein-containing complex binding GTPase binding signaling receptor complex adaptor activity GTPase activity
Cellular location:
cytoplasm membrane synapse heterotrimeric G-protein complex extracellular exosome lysosomal membrane photoreceptor disc membrane extracellular vesicle cytosol plasma membrane
Natural source
Organism: Homo sapiens
Molecular weight
Experimental | Theoretical | Method |
---|---|---|
- | 38 kDa | - |
Recombinant Expression
Organism | Strain | Cell | Plasmid |
---|---|---|---|
Trichoplusia ni | - | - | - |
single-chain variable fragment scFv16
Number of copies: 1
Name: Number of copies: 1
Natural source
Organism: Mus musculus
Molecular weight
Experimental | Theoretical | Method |
---|---|---|
- | 27 kDa | - |
Recombinant Expression
Organism | Strain | Cell | Plasmid |
---|---|---|---|
Spodoptera frugiperda | - | - | - |
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
Number of copies: 1
UniProtKB PDBe-KB AlphaFold DB
Name: Number of copies: 1
UniProtKB PDBe-KB AlphaFold DB
Domains
Gene Ontology [11]
Biological process:
fibroblast proliferation adenylate cyclase-activating dopamine receptor signaling pathway cellular response to prostaglandin E stimulus G protein-coupled receptor signaling pathway cellular response to catecholamine stimulus cell population proliferation
Molecular function:
G-protein beta-subunit binding
Cellular location:
membrane plasma membrane heterotrimeric G-protein complex extracellular exosome
fibroblast proliferation adenylate cyclase-activating dopamine receptor signaling pathway cellular response to prostaglandin E stimulus G protein-coupled receptor signaling pathway cellular response to catecholamine stimulus cell population proliferation
Molecular function:
G-protein beta-subunit binding
Cellular location:
membrane plasma membrane heterotrimeric G-protein complex extracellular exosome
Natural source
Organism: Homo sapiens
Molecular weight
Experimental | Theoretical | Method |
---|---|---|
- | 7 kDa | - |
Recombinant Expression
Organism | Strain | Cell | Plasmid |
---|---|---|---|
Trichoplusia ni | - | - | - |
Nanobody 35
Number of copies: 1
Name: Number of copies: 1
Natural source
Organism: Lama glama
Molecular weight
Experimental | Theoretical | Method |
---|---|---|
- | 17 kDa | - |
Recombinant Expression
Organism | Strain | Cell | Plasmid |
---|---|---|---|
Escherichia coli | - | - | - |
Glucagon-like peptide 1 receptor
Number of copies: 1
UniProtKB PDBe-KB AlphaFold DB
Name: Number of copies: 1
UniProtKB PDBe-KB AlphaFold DB
Domains
Gene Ontology [23]
Biological process:
post-translational protein targeting to membrane, translocation posttranslational protein targeting to membrane, translocation negative regulation of blood pressure hormone secretion activation of adenylate cyclase activity adenylate cyclase-modulating G protein-coupled receptor signaling pathway cell surface receptor signaling pathway positive regulation of cytosolic calcium ion concentration response to psychosocial stress positive regulation of blood pressure regulation of heart contraction adenylate cyclase-activating G protein-coupled receptor signaling pathway cAMP-mediated signaling learning or memory
Molecular function:
peptide hormone binding G protein-coupled peptide receptor activity glucagon receptor activity glucagon-like peptide 1 receptor activity transmembrane signaling receptor activity
Cellular location:
membrane integral component of plasma membrane integral component of membrane plasma membrane
post-translational protein targeting to membrane, translocation posttranslational protein targeting to membrane, translocation negative regulation of blood pressure hormone secretion activation of adenylate cyclase activity adenylate cyclase-modulating G protein-coupled receptor signaling pathway cell surface receptor signaling pathway positive regulation of cytosolic calcium ion concentration response to psychosocial stress positive regulation of blood pressure regulation of heart contraction adenylate cyclase-activating G protein-coupled receptor signaling pathway cAMP-mediated signaling learning or memory
Molecular function:
peptide hormone binding G protein-coupled peptide receptor activity glucagon receptor activity glucagon-like peptide 1 receptor activity transmembrane signaling receptor activity
Cellular location:
membrane integral component of plasma membrane integral component of membrane plasma membrane
Natural source
Organism: Homo sapiens
Molecular weight
Experimental | Theoretical | Method |
---|---|---|
- | 51 kDa | - |
Recombinant Expression
Organism | Strain | Cell | Plasmid |
---|---|---|---|
Spodoptera frugiperda | - | - | - |
3-[(1S,2S)-1-(5-[(4S)-2,2-dimethyloxan-4-yl]-2-{(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl]-4-methyl-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carbonyl}-1H-indol-1-yl)-2-methylcyclopropyl]-1,2,4-oxadiazol-5(4H)-one
HET code: V6G
Number of copies: 1
ChEMBL
Name: HET code: V6G
Number of copies: 1
ChEMBL
Molecular weight
Experimental | Theoretical | Method |
---|---|---|
- | 882 Da | - |