8F0K
 
 | | Human Amylin3 Receptor in complex with Gs and Pramlintide analogue peptide San385 | | Descriptor: | (2S)-2-{[(1R)-1-hydroxyhexadecyl]oxy}-3-{[(1R)-1-hydroxyoctadecyl]oxy}propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Cao, J, Sexton, P.M, Wootten, D.L. | | Deposit date: | 2022-11-03 | | Release date: | 2023-08-02 | | Last modified: | 2024-02-14 | | Method: | ELECTRON MICROSCOPY (1.9 Å) | | Cite: | Structural insight into selectivity of amylin and calcitonin receptor agonists.
Nat.Chem.Biol., 20, 2024
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7MBX
 | | Human Cholecystokinin 1 receptor (CCK1R) Gs complex | | Descriptor: | CHOLESTEROL HEMISUCCINATE, Cholecystokinin receptor type A, Cholecystokinin-8, ... | | Authors: | Mobbs, J.I, Belousoff, M.J, Danev, R, Thal, D.M, Sexton, P.M. | | Deposit date: | 2021-04-01 | | Release date: | 2021-05-26 | | Last modified: | 2021-07-14 | | Method: | ELECTRON MICROSCOPY (1.95 Å) | | Cite: | Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity.
Plos Biol., 19, 2021
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8F2B
 | | Amylin 3 Receptor in complex with Gs and Pramlintide analogue peptide San45 | | Descriptor: | (2S)-2-{[(1R)-1-hydroxyhexadecyl]oxy}-3-{[(1R)-1-hydroxyoctadecyl]oxy}propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Cao, J, Sexton, P.M, Wootten, D.L, Belousoff, M.J. | | Deposit date: | 2022-11-07 | | Release date: | 2023-08-02 | | Last modified: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (2 Å) | | Cite: | Structural insight into selectivity of amylin and calcitonin receptor agonists.
Nat.Chem.Biol., 20, 2024
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8F0J
 | | Calcitonin Receptor in complex with Gs and Pramlintide analogue peptide San45 | | Descriptor: | (2S)-2-{[(1R)-1-hydroxyhexadecyl]oxy}-3-{[(1R)-1-hydroxyoctadecyl]oxy}propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Cao, J, Sexton, P.M, Wootten, D.L, Belousoff, M.J. | | Deposit date: | 2022-11-03 | | Release date: | 2023-08-02 | | Last modified: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (2 Å) | | Cite: | Structural insight into selectivity of amylin and calcitonin receptor agonists.
Nat.Chem.Biol., 20, 2024
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6CRK
 | | Heterotrimeric G-protein in complex with an antibody fragment | | Descriptor: | CITRATE ANION, GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Maeda, S, Dawson, R, Kobilka, B. | | Deposit date: | 2018-03-19 | | Release date: | 2018-10-24 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Development of an antibody fragment that stabilizes GPCR/G-protein complexes.
Nat Commun, 9, 2018
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6X19
 | | Non peptide agonist CHU-128, bound to Glucagon-Like peptide-1 (GLP-1) Receptor | | Descriptor: | 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, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Belousoff, M.J, Zhang, X, Danev, R. | | Deposit date: | 2020-05-18 | | Release date: | 2020-09-09 | | Last modified: | 2020-11-18 | | Method: | ELECTRON MICROSCOPY (2.1 Å) | | Cite: | Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.
Mol.Cell, 80, 2020
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6X18
 | | GLP-1 peptide hormone bound to Glucagon-Like peptide-1 (GLP-1) Receptor | | Descriptor: | Glucagon, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Belousoff, M.J, Zhang, X, Danev, R. | | Deposit date: | 2020-05-18 | | Release date: | 2020-09-09 | | Last modified: | 2020-11-18 | | Method: | ELECTRON MICROSCOPY (2.1 Å) | | Cite: | Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.
Mol.Cell, 80, 2020
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7RTB
 | | Peptide-19 bound to the Glucagon-Like Peptide-1 Receptor (GLP-1R) | | Descriptor: | Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Johnson, R.M, Danev, R, Sexton, P.M, Wootten, D. | | Deposit date: | 2021-08-12 | | Release date: | 2021-10-06 | | Method: | ELECTRON MICROSCOPY (2.14 Å) | | Cite: | Cryo-EM structure of the dual incretin receptor agonist, peptide-19, in complex with the glucagon-like peptide-1 receptor.
Biochem.Biophys.Res.Commun., 578, 2021
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5UKL
 | | Human GRK2 in complex with Gbetagamma subunits and CCG222886 (14bd) | | Descriptor: | 2-{5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluorophenyl}-N-[2-(1H-pyrazol-4-yl)ethyl]acetamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | | Deposit date: | 2017-01-23 | | Release date: | 2017-04-05 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
J. Med. Chem., 60, 2017
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8F2A
 | | Human Amylin3 Receptor in complex with Gs and Pramlintide analogue peptide San385 (Cluster 5 conformation) | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Calcitonin receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cao, J, Sexton, P.M, Wootten, D.L, Radostin, D. | | Deposit date: | 2022-11-07 | | Release date: | 2023-08-02 | | Last modified: | 2024-02-14 | | Method: | ELECTRON MICROSCOPY (2.2 Å) | | Cite: | Structural insight into selectivity of amylin and calcitonin receptor agonists.
Nat.Chem.Biol., 20, 2024
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7TYF
 | | Human Amylin1 Receptor in complex with Gs and rat amylin peptide | | Descriptor: | (2S)-2-{[(1R)-1-hydroxyhexadecyl]oxy}-3-{[(1R)-1-hydroxyoctadecyl]oxy}propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | Deposit date: | 2022-02-13 | | Release date: | 2022-03-23 | | Last modified: | 2022-04-06 | | Method: | ELECTRON MICROSCOPY (2.2 Å) | | Cite: | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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8E3X
 | | Cryo-EM structure of the PAC1R-PACAP27-Gs complex | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | Authors: | Piper, S.J, Danev, R, Sexton, P, Wootten, D. | | Deposit date: | 2022-08-17 | | Release date: | 2022-11-23 | | Last modified: | 2024-05-01 | | Method: | ELECTRON MICROSCOPY (2.3 Å) | | Cite: | Understanding VPAC receptor family peptide binding and selectivity.
Nat Commun, 13, 2022
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8E3Y
 | | Cryo-EM structure of the VPAC1R-PACAP27-Gs complex | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | Authors: | Piper, S.J, Danev, R, Sexton, P, Wootten, D. | | Deposit date: | 2022-08-17 | | Release date: | 2022-11-23 | | Last modified: | 2024-05-01 | | Method: | ELECTRON MICROSCOPY (2.3 Å) | | Cite: | Understanding VPAC receptor family peptide binding and selectivity.
Nat Commun, 13, 2022
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6UVA
 | | CryoEM Structure of the active Adrenomedullin 2 receptor G protein complex with adrenomedullin 2 peptide | | Descriptor: | Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | Deposit date: | 2019-11-01 | | Release date: | 2020-04-01 | | Last modified: | 2020-04-29 | | Method: | ELECTRON MICROSCOPY (2.3 Å) | | Cite: | Structure and Dynamics of Adrenomedullin Receptors AM1and AM2Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying Proteins.
Acs Pharmacol Transl Sci, 3, 2020
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6WZG
 | | Human secretin receptor Gs complex | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | Authors: | Piper, S.J, Belousoff, M.J, Danev, R. | | Deposit date: | 2020-05-13 | | Release date: | 2020-08-12 | | Last modified: | 2020-09-02 | | Method: | ELECTRON MICROSCOPY (2.3 Å) | | Cite: | Structure and dynamics of the active Gs-coupled human secretin receptor.
Nat Commun, 11, 2020
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8IKL
 | | Cryo-EM structure of the CD97-G13 complex | | Descriptor: | Adhesion G protein-coupled receptor E5, Guanine nucleotide-binding protein G(13) subunit alpha isoforms short, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Mao, C, Zhao, R, Dong, Y, Gao, M, Chen, L, Zhang, C, Xiao, P. | | Deposit date: | 2023-02-28 | | Release date: | 2024-01-24 | | Last modified: | 2024-02-14 | | Method: | ELECTRON MICROSCOPY (2.33 Å) | | Cite: | Conformational transitions and activation of the adhesion receptor CD97.
Mol.Cell, 84, 2024
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7WCM
 | | Cryo-EM structure of GPR119-Gs Complex with small molecule agonist MBX-2982 | | Descriptor: | 2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(1,2,3,4-tetrazol-1-yl)phenoxy]methyl]-1,3-thiazole, Glucose-dependent insulinotropic receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Qiao, A.N, Wu, S, Ye, S. | | Deposit date: | 2021-12-20 | | Release date: | 2022-12-21 | | Last modified: | 2022-12-28 | | Method: | ELECTRON MICROSCOPY (2.33 Å) | | Cite: | Activation and signaling mechanism revealed by GPR119-G s complex structures.
Nat Commun, 13, 2022
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7TRP
 | | Human M4 muscarinic acetylcholine receptor complex with Gi1 and the agonist iperoxo and positive allosteric modulator LY2033298 | | Descriptor: | 3-amino-5-chloro-N-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamide, 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Antibody fragment scFv16, ... | | Authors: | Vuckovic, Z, Mobbs, J.I, Belousoff, M.J, Glukhova, A, Sexton, P.M, Danev, R, Thal, D.M. | | Deposit date: | 2022-01-30 | | Release date: | 2023-05-17 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | Structural and dynamic mechanisms of allostery at the M4 muscarinic acetylcholine receptor
Elife, 2023
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8PJK
 | | ST171-bound serotonin 5-HT1A receptor - Gi Protein Complex | | Descriptor: | (2R)-1-(heptadecanoyloxy)-3-{[(R)-hydroxy{[(1R,2R,3R,4R,5S,6R)-2,3,5,6-tetrahydroxy-4-(phosphonooxy)cyclohexyl]oxy}phosphoryl]oxy}propan-2-yl (5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoate, 5-hydroxytryptamine receptor 1A, 6-[3-[2-(2-methoxyphenoxy)ethylamino]propoxy]-4~{H}-1,4-benzoxazin-3-one, ... | | Authors: | Schneider, J, Gmeiner, P, Rasmussen, T, Boettcher, B. | | Deposit date: | 2023-06-23 | | Release date: | 2024-05-29 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | Discovery of a functionally selective serotonin 1A receptor agonist
for the treatment of pain
To Be Published
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6UUS
 | | CryoEM Structure of the active Adrenomedullin 2 receptor G protein complex with adrenomedullin peptide | | Descriptor: | ADM, Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | Deposit date: | 2019-10-31 | | Release date: | 2020-04-01 | | Last modified: | 2020-04-29 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | Structure and Dynamics of Adrenomedullin Receptors AM1and AM2Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying Proteins.
Acs Pharmacol Transl Sci, 3, 2020
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7EJX
 | | Structure of the GPR88-Gi1 signaling complex bound to a synthetic ligand | | Descriptor: | (1R,2R)-N-[(2S,3S)-2-azanyl-3-methyl-pentyl]-N-[4-(4-propylphenyl)phenyl]-2-pyridin-2-yl-cyclopropane-1-carboxamide, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Xu, J, Chen, G, Liu, Z, Du, Y. | | Deposit date: | 2021-04-02 | | Release date: | 2022-04-13 | | Last modified: | 2022-10-26 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | Activation and allosteric regulation of the orphan GPR88-Gi1 signaling complex.
Nat Commun, 13, 2022
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7TZF
 | | Human Amylin3 Receptor in complex with Gs and rat amylin peptide | | Descriptor: | (2S)-2-{[(1R)-1-hydroxyhexadecyl]oxy}-3-{[(1R)-1-hydroxyoctadecyl]oxy}propyl 2-(trimethylammonio)ethyl phosphate, 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | Deposit date: | 2022-02-15 | | Release date: | 2022-03-23 | | Last modified: | 2022-04-06 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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8WST
 | | Cryo-EM structure of Melanin-Concentrating Hormone Receptor 2 with MCH | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(q) subunit alpha-1, ... | | Authors: | Zhao, L, He, Q, Yuan, Q, Gu, Y, Shan, H, Hu, W, Wu, K, Xu, H.E, Zhang, Y, Wu, C. | | Deposit date: | 2023-10-17 | | Release date: | 2024-06-19 | | Last modified: | 2024-06-26 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | Mechanisms of ligand recognition and activation of melanin-concentrating hormone receptors.
Cell Discov, 10, 2024
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7UTZ
 | | Human thyrotropin analog TR1402 bound to human Thyrotropin receptor in complex with miniGs399 (composite structure) | | Descriptor: | (2S)-3-hydroxypropane-1,2-diyl dihexadecanoate, 2-acetamido-2-deoxy-beta-D-glucopyranose, Glycoprotein hormones alpha chain analog TR1402, ... | | Authors: | Faust, B, Cheng, Y, Manglik, A. | | Deposit date: | 2022-04-28 | | Release date: | 2022-08-03 | | Last modified: | 2022-10-05 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | Autoantibody mimicry of hormone action at the thyrotropin receptor.
Nature, 609, 2022
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9AUC
 | | Human Amylin1 Receptor in Complex with Gs and human Calcitonin Gene-Related Peptide | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, Calcitonin gene-related peptide 1, ... | | Authors: | Cao, J, Belousoff, M.J, Wootten, D.L, Sexton, P.M. | | Deposit date: | 2024-02-28 | | Release date: | 2024-04-24 | | Last modified: | 2024-05-22 | | Method: | ELECTRON MICROSCOPY (2.4 Å) | | Cite: | Cryo-EM Structure of the Human Amylin 1 Receptor in Complex with CGRP and Gs Protein.
Biochemistry, 63, 2024
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