Exendin-4-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in complex with Gs protein
Resolution: 3.7 Å
EM Method: Single-particle
Fitted PDBs: 7lll
Q-score: 0.479
Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D
Nat Commun (2022) 13 pp. 92-92 [ DOI: doi:10.1038/s41467-021-27760-0 Pubmed: 35013280 ]
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)
- Nb35 (13 kDa, Protein from Lama glama)
- Exendin-4 (4 kDa, Protein from Heloderma suspectum)
- Exendin-4-glp-1r-gs complex (Complex from Homo sapiens)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
Oxyntomodulin-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in complex with Gs protein
Resolution: 3.3 Å
EM Method: Single-particle
Fitted PDBs: 7lly
Q-score: 0.452
Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D
Nat Commun (2022) 13 pp. 92-92 [ DOI: doi:10.1038/s41467-021-27760-0 Pubmed: 35013280 ]
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)
- Oxyntomodulin-glp-1r-gs complex (Complex from Homo sapiens)
- Nb35 (13 kDa, Protein from Lama glama)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
- Pro-glucagon (4 kDa, Protein from Sus scrofa)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
PF 06882961 bound to the glucagon-like peptide-1 receptor (GLP-1R):Gs complex
Resolution: 2.9 Å
EM Method: Single-particle
Fitted PDBs: 7lci
Q-score: 0.428
Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ
Structure (2021) 29 pp. 963- [ DOI: doi:10.1016/j.str.2021.04.008 Pubmed: 33957078 ]
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
- Water (18 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)
- Glp-1:gs complex with small molecule agonist bound (pf-06882961) (Complex from Homo sapiens)
- 2-[(4-{6-[(4-cyano-2-fluorophenyl)methoxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-{[(2s)-oxetan-2-yl]methyl}-1h-benzimidazole-6-carboxylic acid (555 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
PF 06882961 bound to the glucagon-like peptide-1 receptor (GLP-1R):Gs complex
Resolution: 2.82 Å
EM Method: Single-particle
Fitted PDBs: 7lcj
Q-score: 0.533
Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ
Structure (2021) 29 pp. 963- [ DOI: doi:10.1016/j.str.2021.04.008 Pubmed: 33957078 ]
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- 2-[(4-{6-[(4-cyano-2-fluorophenyl)methoxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-{[(2s)-oxetan-2-yl]methyl}-1h-benzimidazole-6-carboxylic acid (555 Da, Ligand)
- Receptor only portion of glp1:gs complex with a small molecule agonist bound: pf-06882961 (Complex from Homo sapiens)
- Water (18 Da, Ligand)
PF 06882961 bound to the glucagon-like peptide-1 receptor (GLP-1R)
Resolution: 3.24 Å
EM Method: Single-particle
Fitted PDBs: 7lck
Q-score: 0.477
Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ
Structure (2021) 29 pp. 963- [ DOI: doi:10.1016/j.str.2021.04.008 Pubmed: 33957078 ]
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- 2-[(4-{6-[(4-cyano-2-fluorophenyl)methoxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-{[(2s)-oxetan-2-yl]methyl}-1h-benzimidazole-6-carboxylic acid (555 Da, Ligand)
- Glp-1:gs complex with small molecule agonist (pf-06882961) bound (Complex from Homo sapiens)
- Water (18 Da, Ligand)
GLP-1 peptide hormone bound to Glucagon-Like peptide-1 (GLP-1) Receptor
Resolution: 2.1 Å
EM Method: Single-particle
Fitted PDBs: 6x18
Q-score: 0.563
Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D
Mol Cell (2020) 80 pp. 485- [ Pubmed: 33027691 DOI: doi:10.1016/j.molcel.2020.09.020 ]
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- Nanobody 35 (Complex from Lama glama)
- Water (18 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short, guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1, guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2, glucagon-like peptide 1 receptor (Complex from Homo sapiens)
- Glucagon (3 kDa, Protein from Homo sapiens)
- Glp-1 peptide hormone bound to glucagon-like peptide-1 (glp-1) receptor (120 kDa, Complex)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
- Nanobody35 (13 kDa, Protein from Lama glama)
Non peptide agonist CHU-128, bound to Glucagon-Like peptide-1 (GLP-1) Receptor
Resolution: 2.1 Å
EM Method: Single-particle
Fitted PDBs: 6x19
Q-score: 0.579
Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D
Mol Cell (2020) 80 pp. 485- [ Pubmed: 33027691 DOI: doi:10.1016/j.molcel.2020.09.020 ]
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- Water (18 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)
- 3-{(1s)-1-[5-(2,2-dimethylmorpholin-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]butyl}-1,2,4-oxadiazol-5(4h)-one (885 Da, Ligand)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short, guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1, guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2, glucagon-like peptide 1 receptor (Complex from Homo sapiens)
- Nanobody35 (Complex from Lama glama)
- Chu-128:glp-1r:gs complex (120 kDa, Complex)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
- Nanobody35 (13 kDa, Protein from Lama glama)
Non peptide agonist PF-06882961, bound to Glucagon-Like peptide-1 (GLP-1) Receptor
Resolution: 2.5 Å
EM Method: Single-particle
Fitted PDBs: 6x1a
Q-score: 0.522
Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D
Mol Cell (2020) 80 pp. 485- [ Pubmed: 33027691 DOI: doi:10.1016/j.molcel.2020.09.020 ]
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- Water (18 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short, guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1, guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2, glucagon-like peptide 1 receptor (Complex from Homo sapiens)
- Nanobody35 (Complex from Lama glama)
- 2-[(4-{6-[(4-cyano-2-fluorophenyl)methoxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-{[(2s)-oxetan-2-yl]methyl}-1h-benzimidazole-6-carboxylic acid (555 Da, Ligand)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
- Pf-06882961:glp-1r:gs complex (120 kDa, Complex)
- Nanobody35 (13 kDa, Protein from Lama glama)
CryoEM Structure of the glucagon receptor with a dual-agonist peptide
Resolution: 3.4 Å
EM Method: Single-particle
Fitted PDBs: 6whc
Q-score: 0.445
Chang R, Zhang X, Qiao A, Dai A, Belousoff MJ, Tan Q, Shao L, Zhong L, Lin G, Liang YL, Ma L, Han S, Yang D, Danev R, Wang MW, Wootten D, Wu B, Sexton PM
J Biol Chem (2020) 295 pp. 9313-9325 [ DOI: doi:10.1074/jbc.RA120.013793 Pubmed: 32371397 ]
- Nanobody 35 (Complex from Lama glama)
- Glucagon receptor (54 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Homo sapiens)
- Dual-agonist peptide (Complex from synthetic construct)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
- Glucagon receptor complex (Complex)
- Nanobody35 (15 kDa, Protein from Lama glama)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short, guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1, receptor activity-modifying protein 3, guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2, calcitonin gene-related peptide type 1 receptor, glucagon receptor (Complex from Homo sapiens)
- Dual-agonist peptide (3 kDa, Protein from synthetic construct)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
Non-peptide agonist (TT-OAD2) bound to the Glucagon-Like peptide-1 (GLP-1) Receptor
Resolution: 3.0 Å
EM Method: Single-particle
Fitted PDBs: 6orv
Q-score: 0.538
Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D
Nature (2020) 577 pp. 432-436 [ Pubmed: 31915381 DOI: doi:10.1038/s41586-019-1902-z ]
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- Tt-oad2:glp-1r:gs complex (120 kDa, Complex)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Homo sapiens)
- Nanobody 35 (Complex from Homo sapiens)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short, guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1, guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2, glucagon-like peptide 1 receptor (Complex from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (38 kDa, Protein from Homo sapiens)
- N-{(3s,8s)-3-{4-[(3,4-dichlorophenyl)methoxy]phenyl}-7-[(1s)-1-phenylpropyl]-2,3,6,7,8,9-hexahydro[1,4]dioxino[2,3-g]isoquinoline-8-carbonyl}-4-(2,3-dimethylpyridin-4-yl)-l-phenylalanine (856 Da, Ligand)
- Nanobody 35 (15 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)