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7EVM
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Cryo-EM structure of the compound 2-bound human GLP-1 receptor-Gs complex
分子名称: CHOLESTEROL, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Cong, Z, Chen, L, Ma, H, Zhou, Q, Zou, X, Ye, C, Dai, A, Liu, Q, Huang, W, Sun, X, Wang, X, Xu, P, Zhao, L, Xia, T, Zhong, W, Yang, D, Xu, H.E, Zhang, Y, Wang, M.
登録日2021-05-21
公開日2021-08-11
実験手法ELECTRON MICROSCOPY (2.5 Å)
主引用文献Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor.
Nat Commun, 12, 2021
7T10
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CryoEM structure of somatostatin receptor 2 in complex with somatostatin-14 and Gi3
分子名称: 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(i) subunit alpha-3, ...
著者Robertson, M.J, Skinotis, G.
登録日2021-11-30
公開日2022-03-09
最終更新日2022-03-30
実験手法ELECTRON MICROSCOPY (2.5 Å)
主引用文献Plasticity in ligand recognition at somatostatin receptors.
Nat.Struct.Mol.Biol., 29, 2022
7T2G
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CryoEM structure of mu-opioid receptor - Gi protein complex bound to mitragynine pseudoindoxyl (MP)
分子名称: CHOLESTEROL, 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, ...
著者Seven, A.B, Qu, Q, Robertson, M.J, Wang, H, Kobilka, B.K, Skiniotis, G.
登録日2021-12-04
公開日2022-12-07
最終更新日2023-02-15
実験手法ELECTRON MICROSCOPY (2.5 Å)
主引用文献Insights into distinct signaling profiles of the mu OR activated by diverse agonists.
Nat.Chem.Biol., 2022
8U26
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Gaussian Mixture Models based single particle refinement - GPCR (Substance P bound to active human neurokinin 1 receptor in complex with miniGs399 from EMPIAR-10786)
分子名称: 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, ...
著者Chen, M, Pintilie, G.
登録日2023-09-05
公開日2023-11-15
最終更新日2024-01-24
実験手法ELECTRON MICROSCOPY (2.5 Å)
主引用文献Improving resolution and resolvability of single-particle cryoEM structures using Gaussian mixture models.
Nat.Methods, 21, 2024
7TRQ
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Human M4 muscarinic acetylcholine receptor complex with Gi1 and the agonist iperoxo and positive allosteric modulator VU0467154
分子名称: 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, 5-amino-3,4-dimethyl-N-{[4-(trifluoromethanesulfonyl)phenyl]methyl}thieno[2,3-c]pyridazine-6-carboxamide, Antibody fragment scFv16, ...
著者Vuckovic, Z, Mobbs, J.I, Belousoff, M.J, Glukhova, A, Sexton, P.M, Danev, R, Thal, D.M.
登録日2022-01-30
公開日2023-05-17
実験手法ELECTRON MICROSCOPY (2.5 Å)
主引用文献Structural and dynamic mechanisms of allostery at the M4 muscarinic acetylcholine receptor
Elife, 2023
7KI1
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Taspoglutide-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in Complex with Gs Protein
分子名称: 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, ...
著者Zhang, X, Belousoff, M.J, Danev, R, Sexton, P.M, Wootten, D.
登録日2020-10-22
公開日2021-08-04
実験手法ELECTRON MICROSCOPY (2.5 Å)
主引用文献Structure and dynamics of semaglutide- and taspoglutide-bound GLP-1R-Gs complexes.
Cell Rep, 36, 2021
7KI0
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Semaglutide-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in Complex with Gs protein
分子名称: 17-amino-10-oxo-3,6,12,15-tetraoxa-9-azaheptadecan-1-oic acid, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Zhang, X, Belousoff, M.J, Danev, R, Sexton, P.M, Wootten, D.
登録日2020-10-22
公開日2021-08-04
実験手法ELECTRON MICROSCOPY (2.5 Å)
主引用文献Structure and dynamics of semaglutide- and taspoglutide-bound GLP-1R-Gs complexes.
Cell Rep, 36, 2021
1OMW
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Crystal Structure of the complex between G Protein-Coupled Receptor Kinase 2 and Heterotrimeric G Protein beta 1 and gamma 2 subunits
分子名称: G-protein coupled receptor kinase 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit, Guanine nucleotide-binding protein G(I)/G(S)/G(T) beta subunit 1
著者Lodowski, D.T, Pitcher, J.A, Capel, W.D, Lefkowitz, R.J, Tesmer, J.J.G.
登録日2003-02-26
公開日2003-06-03
最終更新日2023-08-16
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Keeping G proteins at Bay: A Complex Between G Protein-Coupled Receptor Kinase 2 and G-Beta-Gamma
Science, 300, 2003
7S3I
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Ex4-D-Ala bound to the glucagon-like peptide-1 receptor/g protein complex (conformer 2)
分子名称: 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, ...
著者Belousoff, M.J, Piper, S.J, Danev, R.
登録日2021-09-07
公開日2022-01-05
最終更新日2022-03-16
実験手法ELECTRON MICROSCOPY (2.51 Å)
主引用文献Structural and functional diversity among agonist-bound states of the GLP-1 receptor.
Nat.Chem.Biol., 18, 2022
7K7L
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Structure of a hit for G Protein Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure
分子名称: 3-benzyl-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Spurlino, J.C, Milligan, C.
登録日2020-09-23
公開日2020-10-28
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (2.539 Å)
主引用文献Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor.
Bioorg.Med.Chem.Lett., 30, 2020
8WG7
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Cryo-EM structures of peptide free and Gs-coupled GLP-1R
分子名称: 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, ...
著者Cong, Z.T, Zhao, F.H, Li, Y, Luo, G, Zhou, Q.T, Yang, D.H, Wang, M.W.
登録日2023-09-20
公開日2024-03-06
実験手法ELECTRON MICROSCOPY (2.54 Å)
主引用文献Molecular features of the ligand-free GLP-1R, GCGR and GIPR in complex with G s proteins.
Cell Discov, 10, 2024
7S8M
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CryoEM structure of Gi-coupled MRGPRX2 with peptide agonist Cortistatin-14
分子名称: Cortistatin 14, 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, ...
著者Cao, C, Fay, J.F, Gumpper, R.H, Roth, B.L.
登録日2021-09-18
公開日2021-11-17
最終更新日2021-12-15
実験手法ELECTRON MICROSCOPY (2.54 Å)
主引用文献Structure, function and pharmacology of human itch GPCRs.
Nature, 600, 2021
8FEG
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CryoEM structure of Kappa Opioid Receptor bound to a semi-peptide and Gi1
分子名称: ACE-TYR-ALA-DTY-THR-THR-CYS-THR-DPN-XT9, 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, ...
著者Fay, J.F, Che, T.
登録日2022-12-06
公開日2023-12-06
最終更新日2024-01-17
実験手法ELECTRON MICROSCOPY (2.54 Å)
主引用文献Design and structural validation of peptide-drug conjugate ligands of the kappa-opioid receptor.
Nat Commun, 14, 2023
8J6P
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Cryo-EM structure of the MK-6892-bound human HCAR2-Gi1 complex
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, 7-methyl-N-[(2R)-1-phenoxypropan-2-yl]-3-(4-propan-2-ylphenyl)pyrazolo[1,5-a]pyrimidine-6-carboxamide, CHOLESTEROL, ...
著者Mao, C, Gao, M, Zang, S, Zhu, Y, Ma, X, Zhang, Y.
登録日2023-04-26
公開日2023-12-06
実験手法ELECTRON MICROSCOPY (2.55 Å)
主引用文献Orthosteric and allosteric modulation of human HCAR2 signaling complex.
Nat Commun, 14, 2023
8FLQ
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Human PTH1R in complex with PTH(1-34) and Gs
分子名称: 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, ...
著者Cary, B.P, Belousoff, M.J, Piper, S.J, Wootten, D, Sexton, P.M.
登録日2022-12-22
公開日2023-04-26
最終更新日2023-06-14
実験手法ELECTRON MICROSCOPY (2.55 Å)
主引用文献Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
7TYX
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Human Amylin2 Receptor in complex with Gs and rat amylin peptide
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, Calcitonin receptor, ...
著者Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M.
登録日2022-02-14
公開日2022-03-30
最終更新日2022-04-06
実験手法ELECTRON MICROSCOPY (2.55 Å)
主引用文献A structural basis for amylin receptor phenotype.
Science, 375, 2022
8X7A
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Treprostinil bound Prostacyclin Receptor G protein complex
分子名称: 2-[[(1~{R},2~{R},3~{a}~{S},9~{a}~{S})-2-oxidanyl-1-[(3~{S})-3-oxidanyloctyl]-2,3,3~{a},4,9,9~{a}-hexahydro-1~{H}-cyclopenta[g]naphthalen-5-yl]oxy]ethanoic acid, 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, ...
著者Wang, J.J, Jin, S, Zhang, H, Xu, Y, Hu, W, Jiang, Y, Chen, C, Wang, D.W, Xu, H.E, Wu, C.
登録日2023-11-23
公開日2024-03-06
実験手法ELECTRON MICROSCOPY (2.56 Å)
主引用文献Molecular recognition and activation of the prostacyclin receptor by anti-pulmonary arterial hypertension drugs.
Sci Adv, 10, 2024
5HE0
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Bovine GRK2 in complex with Gbetagamma subunits and CCG215022
分子名称: (4S)-4-{4-fluoro-3-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G.
登録日2016-01-05
公開日2016-05-11
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (2.56 Å)
主引用文献Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
J.Med.Chem., 59, 2016
4PNK
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G protein-coupled receptor kinase 2 in complex with GSK180736A
分子名称: (4S)-4-(4-fluorophenyl)-N-(2H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Homan, K.T, Larimore, K.M, Elkins, J, Knapp, S, Tesmer, J.J.G.
登録日2014-05-23
公開日2014-10-08
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (2.56 Å)
主引用文献Identification and structure-function analysis of subfamily selective g protein-coupled receptor kinase inhibitors.
Acs Chem.Biol., 10, 2015
8JR9
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Small molecule agonist (PCO371) bound to human parathyroid hormone receptor type 1 (PTH1R)
分子名称: 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-1, ...
著者Zhao, L, He, Q, Yuan, Q, Gu, Y, He, X, Shan, H, Li, J, Wang, K, Li, Y, Hu, W, Wu, K, Shen, J, Xu, H.E.
登録日2023-06-16
公開日2023-08-02
最終更新日2023-10-04
実験手法ELECTRON MICROSCOPY (2.57 Å)
主引用文献Conserved class B GPCR activation by a biased intracellular agonist.
Nature, 621, 2023
8JIR
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Cryo-EM structure of the GLP-1R/GCGR dual agonist SAR425899-bound human GLP-1R-Gs complex
分子名称: 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, ...
著者Yang, L, Zhou, Q.T, Dai, A.T, Zhao, F.H, Chang, R.L, Ying, T.L, Wu, B.L, Yang, D.H, Wang, M.W, Cong, Z.T.
登録日2023-05-27
公開日2023-09-06
実験手法ELECTRON MICROSCOPY (2.57 Å)
主引用文献Structural analysis of the dual agonism at GLP-1R and GCGR.
Proc.Natl.Acad.Sci.USA, 120, 2023
7PIU
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Cryo-EM structure of the agonist setmelanotide bound to the active melanocortin-4 receptor (MC4R) in complex with the heterotrimeric Gs protein at 2.6 A resolution.
分子名称: CALCIUM ION, Camelid antibody fragment - nanobody 35, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Heyder, N.A, Schmidt, A, Kleinau, G, Hilal, T, Scheerer, P.
登録日2021-08-23
公開日2021-11-17
実験手法ELECTRON MICROSCOPY (2.58 Å)
主引用文献Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-alpha-MSH and setmelanotide.
Cell Res., 31, 2021
7S8O
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CryoEM structure of Gi-coupled MRGPRX2 with small molecule agonist (R)-Zinc-3573
分子名称: (3R)-N,N-dimethyl-1-[(8S)-5-phenylpyrazolo[1,5-a]pyrimidin-7-yl]pyrrolidin-3-amine, 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, ...
著者Cao, C, Fay, J.F, Gumpper, R.H, Roth, B.L.
登録日2021-09-18
公開日2021-11-17
最終更新日2021-12-15
実験手法ELECTRON MICROSCOPY (2.58 Å)
主引用文献Structure, function and pharmacology of human itch GPCRs.
Nature, 600, 2021
8IOD
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Cryo-EM structure of the PG-901-bound human melanocortin receptor 5 (MC5R)-Gs complex
分子名称: CALCIUM ION, 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,HiBiT, ...
著者Feng, W.B, Zhou, Q.T, Chen, X.Y, Dai, A.T, Cai, X.Q, Liu, X, Zhao, F.H, Chen, Y, Ye, C.Y, Xu, Y.N, Cong, Z.T, Li, H, Lin, S, Yang, D.H, Wang, M.W.
登録日2023-03-10
公開日2023-09-20
最終更新日2023-11-15
実験手法ELECTRON MICROSCOPY (2.59 Å)
主引用文献Structural insights into ligand recognition and subtype selectivity of the human melanocortin-3 and melanocortin-5 receptors.
Cell Discov, 9, 2023
8FMZ
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Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator
分子名称: 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, MiniGq, ...
著者Krumm, B.E, Diberto, J.F, Olsen, R.H.J, Kang, H, Slocum, S.T, Zhang, S, Strachan, R.T, Fay, J.F, Roth, B.L.
登録日2022-12-26
公開日2023-03-29
最終更新日2023-04-19
実験手法ELECTRON MICROSCOPY (2.59 Å)
主引用文献Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator.
Biochemistry, 62, 2023

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件を2024-05-15に公開中

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