GPR3 Orphan G-coupled Protein Receptor in complex with Dominant Negative Gs.
Resolution: 3.49 Å
EM Method: Single-particle
Fitted PDBs: 8u8f
Q-score: 0.422
Russell IC, Zhang X, Bumbak F, McNeill SM, Josephs TM, Leeming MG, Christopoulos G, Venugopal H, Flocco MM, Sexton PM, Wootten D, Belousoff MJ
Biochemistry (2024) 63 pp. 625-631 [ DOI: doi:10.1021/acs.biochem.3c00647 Pubmed: 38376112 ]
- Active state, gpr3 complex with dominant negative g-alphas. (Complex from Homo sapiens)
- Palmitic acid (256 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(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
- G-protein coupled receptor 3 (41 kDa, Protein from Homo sapiens)
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 [ Pubmed: 35013280 DOI: doi:10.1038/s41467-021-27760-0 ]
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- Exendin-4 (4 kDa, Protein from Heloderma suspectum)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
- Nb35 (13 kDa, Protein from Lama glama)
- Exendin-4-glp-1r-gs complex (Complex 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 ]
- 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)
- Glucagon-like peptide 1 receptor (56 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)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)
Resolution: 3.2 Å
EM Method: Single-particle
Fitted PDBs: 7ld3
Q-score: 0.518
Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A
Nature (2021) 597 pp. 571-576 [ DOI: doi:10.1038/s41586-021-03897-2 Pubmed: 34497422 ]
- {2-amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone (449 Da, Ligand)
- Human adenosine a1 receptor-gi2-protein complex bound to its endogenous agonist adenosine (Complex from Homo sapiens)
- Guanine nucleotide-binding protein g(i) subunit alpha-2 (40 kDa, Protein from Homo sapiens)
- Adenosine (267 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Homo sapiens)
- Water (18 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (38 kDa, Protein from Homo sapiens)
- Chimera protein of muscarinic acetylcholine receptor m4 and adenosine receptor a1 (43 kDa, Protein from Homo sapiens)
Resolution: 3.3 Å
EM Method: Single-particle
Fitted PDBs: 7ld4
Q-score: 0.502
Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A
Nature (2021) 597 pp. 571-576 [ DOI: doi:10.1038/s41586-021-03897-2 Pubmed: 34497422 ]
- Human adenosine a1 receptor-gi2-protein complex bound to its endogenous agonist adenosine (Complex from Homo sapiens)
- Guanine nucleotide-binding protein g(i) subunit alpha-2 (40 kDa, Protein from Homo sapiens)
- Adenosine (267 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Homo sapiens)
- Water (18 Da, Ligand)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (38 kDa, Protein from Homo sapiens)
- Chimera protein of muscarinic acetylcholine receptor m4 and adenosine receptor a1 (43 kDa, Protein from Homo sapiens)
Cryo-EM of GLP-1 receptor bound to GLP-1 and Gs protein
Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Šenel 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. 485-500.e7 [ Pubmed: 33027691 DOI: 10.1016/j.molcel.2020.09.020 ]
Image sets:
Human Cholecystokinin 1 receptor (CCK1R) Gs complex
Resolution: 1.95 Å
EM Method: Single-particle
Fitted PDBs: 7mbx
Q-score: 0.619
Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM
PLoS Biol (2021) 19 pp. e3001295-e3001295 [ DOI: doi:10.1371/journal.pbio.3001295 Pubmed: 34086670 ]
- Cck1r/cck-8/gas complex (140 MDa, Complex)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Rattus norvegicus)
- Cholecystokinin-8 (Complex from Homo sapiens)
- Cholecystokinin-8 (1 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Homo sapiens)
- Cholecystokinin receptor type a (48 kDa, Protein from Homo sapiens)
- Cholesterol hemisuccinate (486 Da, Ligand)
- Nanobody35 (15 kDa, Protein from Lama glama)
- Water (18 Da, Ligand)
- Nanobody35 (Complex from Lama glama)
- Guanine nucleotide-binding protein g(s) subunits alpha and gamma (Complex from Homo sapiens)
- Cholecystokinin receptor type a (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 (Complex from Rattus norvegicus)
Human Cholecystokinin 1 receptor (CCK1R) Gq chimera (mGsqi) complex
Resolution: 2.44 Å
EM Method: Single-particle
Fitted PDBs: 7mby
Q-score: 0.413
Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM
PLoS Biol (2021) 19 pp. e3001295-e3001295 [ Pubmed: 34086670 DOI: doi:10.1371/journal.pbio.3001295 ]
- Cholecystokinin receptor type a (47 kDa, Protein from Homo sapiens)
- Cholesterol hemisuccinate (486 Da, Ligand)
- Scfv16 (Complex from Mus musculus)
- Cck-8 (Complex from Homo sapiens)
- Cholecystokinin-8 (1 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i) subunit alpha-1,guanine nucleotide-binding protein g(s) subunit alpha isoforms short,with certain residues mutated to match guanine nucleotide-binding protein g(q) subunit (29 kDa, Protein from Homo sapiens)
- G protein subunit beta-1 (Complex from Rattus norvegicus)
- Cck1r (Complex from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (7 kDa, Protein from Homo sapiens)
- G(sqi)-alpha/g protein subunit gamma-2 (Complex from Homo sapiens)
- Cck1r/cck-8/mgsqi complex (150 MDa, Complex)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Rattus norvegicus)
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- [ DOI: doi:10.1016/j.molcel.2020.09.020 Pubmed: 33027691 ]
- Nanobody 35 (Complex 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, guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2, glucagon-like peptide 1 receptor (Complex from Homo sapiens)
- Glp-1 peptide hormone bound to glucagon-like peptide-1 (glp-1) receptor (120 kDa, Complex)
- Nanobody35 (13 kDa, Protein from Lama glama)
- Guanine nucleotide-binding protein g(s) subunit alpha isoforms short (45 kDa, Protein from Homo sapiens)
- Glucagon (3 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
- Water (18 Da, Ligand)
- Glucagon-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
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- [ DOI: doi:10.1016/j.molcel.2020.09.020 Pubmed: 33027691 ]
- 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-like peptide 1 receptor (56 kDa, Protein from Homo sapiens)
- Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1 (37 kDa, Protein from Homo sapiens)
- Water (18 Da, Ligand)
- Nanobody35 (Complex from Lama glama)
- Nanobody35 (13 kDa, Protein 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)
- 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(i)/g(s)/g(o) subunit gamma-2 (6 kDa, Protein from Homo sapiens)