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PDB: 36 件

5DSG
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Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium
分子名称: (1R,2R,4S,5S,7S)-7-{[hydroxy(dithiophen-2-yl)acetyl]oxy}-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0~2,4~]nonane, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE, ...
著者Thal, D.M, Kobilka, B.K, Sexton, P.M, Christopoulos, A.
登録日2015-09-17
公開日2016-03-16
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.
Nature, 531, 2016
3V5W
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Human G Protein-Coupled Receptor Kinase 2 in Complex with Soluble Gbetagamma Subunits and Paroxetine
分子名称: G-protein coupled receptor kinase 2, 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Thal, D.M, Tesmer, J.J.G.
登録日2011-12-17
公開日2012-09-26
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.07 Å)
主引用文献Paroxetine is a direct inhibitor of g protein-coupled receptor kinase 2 and increases myocardial contractility.
Acs Chem.Biol., 7, 2012
3PVU
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Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD101)
分子名称: 3-({[4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Thal, D.M, Tesmer, J.J.
登録日2010-12-07
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.48 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
3PSC
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Bovine GRK2 in complex with Gbetagamma subunits
分子名称: Beta-adrenergic receptor kinase 1, 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Thal, D.M, Tesmer, J.J.
登録日2010-12-01
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.67 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
3PVW
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Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD103A)
分子名称: Beta-adrenergic receptor kinase 1, 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Thal, D.M, Tesmer, J.J.
登録日2010-12-07
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.49 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
6OL9
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Structure of the M5 muscarinic acetylcholine receptor (M5-T4L) bound to tiotropium
分子名称: (1R,2R,4S,5S,7S)-7-{[hydroxy(dithiophen-2-yl)acetyl]oxy}-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0~2,4~]nonane, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 3,6,9,12,15,18-HEXAOXAICOSANE-1,20-DIOL, ...
著者Vuckovic, Z, Christopoulos, A, Thal, D.M.
登録日2019-04-16
公開日2019-12-11
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (2.541 Å)
主引用文献Crystal structure of the M5muscarinic acetylcholine receptor.
Proc.Natl.Acad.Sci.USA, 116, 2019
6D9H
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Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist
分子名称: ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Draper-Joyce, C.J, Khoshouei, M, Thal, D.M, Liang, Y.-L, Nguyen, A.T.N, Furness, S.G.B, Venugopal, H, Baltos, J, Plitzko, J.M, Danev, R, Baumeister, W, May, L.T, Wootten, D, Sexton, P, Glukhova, A, Christopoulos, A.
登録日2018-04-29
公開日2018-06-20
最終更新日2018-07-11
実験手法ELECTRON MICROSCOPY (3.6 Å)
主引用文献Structure of the adenosine-bound human adenosine A1receptor-Gicomplex.
Nature, 558, 2018
8FX5
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Human M4 muscarinic acetylcholine receptor complex with Gi1 and xanomeline
分子名称: Antibody fragment scFv16, 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Vuckovic, Z, Mobbs, J.I, Glukhova, A, Sexton, P.M, Danev, R, Thal, D.M.
登録日2023-01-23
公開日2023-09-13
実験手法ELECTRON MICROSCOPY (2.45 Å)
主引用文献Xanomeline displays concomitant orthosteric and allosteric binding modes at the M 4 mAChR.
Nat Commun, 14, 2023
8GHD
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The structure of h12-LOX in hexameric form bound to inhibitor ML355 and arachidonic acid
分子名称: ARACHIDONIC ACID, FE (II) ION, N-(1,3-benzothiazol-2-yl)-4-{[(2-hydroxy-3-methoxyphenyl)methyl]amino}benzene-1-sulfonamide, ...
著者Black, K.A, Mobbs, J.I, Venugopal, H, Thal, D.M, Glukhova, A.
登録日2023-03-09
公開日2023-08-09
最終更新日2023-10-11
実験手法ELECTRON MICROSCOPY (2.2 Å)
主引用文献Cryo-EM structures of human arachidonate 12S-lipoxygenase bound to endogenous and exogenous inhibitors.
Blood, 142, 2023
8GHC
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The structure of h12-LOX in dimeric form
分子名称: FE (II) ION, Polyunsaturated fatty acid lipoxygenase ALOX12
著者Black, K.A, Mobbs, J.I, Venugopal, H, Thal, D.M, Glukhova, A.
登録日2023-03-09
公開日2023-08-09
最終更新日2023-10-11
実験手法ELECTRON MICROSCOPY (2.3 Å)
主引用文献Cryo-EM structures of human arachidonate 12S-lipoxygenase bound to endogenous and exogenous inhibitors.
Blood, 142, 2023
8GHE
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The structure of h12-LOX in tetrameric form bound to endogenous inhibitor oleoyl-CoA
分子名称: FE (II) ION, Polyunsaturated fatty acid lipoxygenase ALOX12, S-{(3R,5R,9R)-1-[(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-4-hydroxy-3-(phosphonooxy)tetrahydrofuran-2-yl]-3,5,9-trihydroxy-8,8-dimethyl-3,5-dioxido-10,14-dioxo-2,4,6-trioxa-11,15-diaza-3lambda~5~,5lambda~5~-diphosphaheptadecan-17-yl} (9Z)-octadec-9-enethioate (non-preferred name)
著者Black, K.A, Mobbs, J.I, Venugopal, H, Thal, D.M, Glukhova, A.
登録日2023-03-09
公開日2023-08-09
最終更新日2023-10-11
実験手法ELECTRON MICROSCOPY (2.05 Å)
主引用文献Cryo-EM structures of human arachidonate 12S-lipoxygenase bound to endogenous and exogenous inhibitors.
Blood, 142, 2023
7TRK
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Human M4 muscarinic acetylcholine receptor complex with Gi1 and the agonist iperoxo
分子名称: 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Antibody fragment scFv16, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Vuckovic, Z, Mobbs, J.I, Belousoff, M.J, Glukhova, A, Sexton, P.M, Danev, R, Thal, D.M.
登録日2022-01-29
公開日2023-05-17
実験手法ELECTRON MICROSCOPY (2.8 Å)
主引用文献Structural and dynamic mechanisms of allostery at the M4 muscarinic acetylcholine receptor
Elife, 2023
7TRP
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Human M4 muscarinic acetylcholine receptor complex with Gi1 and the agonist iperoxo and positive allosteric modulator LY2033298
分子名称: 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, ...
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 (2.4 Å)
主引用文献Structural and dynamic mechanisms of allostery at the M4 muscarinic acetylcholine receptor
Elife, 2023
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
7TRS
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Human M4 muscarinic acetylcholine receptor complex with Gi1 and the endogenous agonist acetylcholine
分子名称: ACETYLCHOLINE, Antibody fragment scFv16, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
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 (2.8 Å)
主引用文献Structural and dynamic mechanisms of allostery at the M4 muscarinic acetylcholine receptor
Elife, 2023
7RMI
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SP6-11 biased agonist bound to active human neurokinin 1 receptor in complex with miniGs/q70
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Harris, J.A, Faust, B, Gondin, A.B, Daemgen, M.A, Suomivuori, C.M, Veldhuis, N.A, Cheng, Y, Dror, R.O, Thal, D, Manglik, A.
登録日2021-07-27
公開日2021-11-03
最終更新日2022-01-05
実験手法ELECTRON MICROSCOPY (3.2 Å)
主引用文献Selective G protein signaling driven by substance P-neurokinin receptor dynamics.
Nat.Chem.Biol., 18, 2022
7RMG
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Substance P bound to active human neurokinin 1 receptor in complex with miniGs/q70
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Harris, J.A, Faust, B, Gondin, A.B, Daemgen, M.A, Suomivuori, C.M, Veldhuis, N.A, Cheng, Y, Dror, R.O, Thal, D, Manglik, A.
登録日2021-07-27
公開日2021-11-03
最終更新日2022-01-05
実験手法ELECTRON MICROSCOPY (3 Å)
主引用文献Selective G protein signaling driven by substance P-neurokinin receptor dynamics.
Nat.Chem.Biol., 18, 2022
7RMH
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Substance P bound to active human neurokinin 1 receptor in complex with miniGs399
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Harris, J.A, Faust, B, Gondin, A.B, Daemgen, M.A, Suomivuori, C.M, Veldhuis, N.A, Cheng, Y, Dror, R.O, Thal, D, Manglik, A.
登録日2021-07-27
公開日2021-11-03
最終更新日2022-01-05
実験手法ELECTRON MICROSCOPY (3.1 Å)
主引用文献Selective G protein signaling driven by substance P-neurokinin receptor dynamics.
Nat.Chem.Biol., 18, 2022
8GHB
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The structure of h12-LOX in monomeric form
分子名称: FE (II) ION, Polyunsaturated fatty acid lipoxygenase ALOX12
著者Black, K.A, Mobbs, J.I, Venugopal, H, Thal, D.M, Glukhova, A.
登録日2023-03-09
公開日2023-08-09
最終更新日2024-05-01
実験手法ELECTRON MICROSCOPY (2.76 Å)
主引用文献Cryo-EM structures of human arachidonate 12S-lipoxygenase bound to endogenous and exogenous inhibitors.
Blood, 142, 2023
7MBX
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Human Cholecystokinin 1 receptor (CCK1R) Gs complex
分子名称: CHOLESTEROL HEMISUCCINATE, Cholecystokinin receptor type A, Cholecystokinin-8, ...
著者Mobbs, J.I, Belousoff, M.J, Danev, R, Thal, D.M, Sexton, P.M.
登録日2021-04-01
公開日2021-05-26
最終更新日2021-07-14
実験手法ELECTRON MICROSCOPY (1.95 Å)
主引用文献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
7MBY
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Human Cholecystokinin 1 receptor (CCK1R) Gq chimera (mGsqi) complex
分子名称: CHOLESTEROL HEMISUCCINATE, Cholecystokinin receptor type A, Cholecystokinin-8, ...
著者Mobbs, J.I, Belousoff, M.J, Danev, R, Thal, D.M, Sexton, P.M.
登録日2021-04-01
公開日2021-05-26
最終更新日2021-07-14
実験手法ELECTRON MICROSCOPY (2.44 Å)
主引用文献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
7LD3
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Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist and an allosteric ligand
分子名称: ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Draper-Joyce, C.J, Danev, R, Thal, D.M, Christopoulos, A, Glukhova, A.
登録日2021-01-12
公開日2021-09-08
最終更新日2021-10-13
実験手法ELECTRON MICROSCOPY (3.2 Å)
主引用文献Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia.
Nature, 597, 2021
7LD4
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Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist
分子名称: ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Draper-Joyce, C.J, Danev, R, Thal, D.M, Christopoulos, A, Glukhova, A.
登録日2021-01-12
公開日2021-09-08
最終更新日2021-10-13
実験手法ELECTRON MICROSCOPY (3.3 Å)
主引用文献Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia.
Nature, 597, 2021
5UZ7
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Volta phase plate cryo-electron microscopy structure of a calcitonin receptor-heterotrimeric Gs protein complex
分子名称: Calcitonin 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Liang, Y.L, Khoshouei, M, Radjainia, M, Zhang, Y, Glukhova, A, Tarrasch, J, Thal, D.M, Furness, S.G.B, Christopoulos, G, Coudrat, T, Danev, R, Baumeister, W, Miller, L.J, Christopoulos, A, Kobilka, B.K, Wootten, D, Skiniotis, G, Sexton, P.M.
登録日2017-02-24
公開日2017-05-03
最終更新日2018-07-18
実験手法ELECTRON MICROSCOPY (4.1 Å)
主引用文献Phase-plate cryo-EM structure of a class B GPCR-G-protein complex.
Nature, 546, 2017
5UEN
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Crystal structure of the human adenosine A1 receptor A1AR-bRIL in complex with the covalent antagonist DU172 at 3.2A resolution
分子名称: 4-{[3-(8-cyclohexyl-2,6-dioxo-1-propyl-1,2,6,7-tetrahydro-3H-purin-3-yl)propyl]carbamoyl}benzene-1-sulfonyl fluoride, Adenosine receptor A1,Soluble cytochrome b562,Adenosine receptor A1, OLEIC ACID
著者Glukhova, A, Thal, D.M, Nguyen, A.T, Vecchio, E.A, Jorg, M, Scammells, P.J, May, L.T, Sexton, P.M, Christopoulos, A.
登録日2017-01-03
公開日2017-03-01
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (3.2 Å)
主引用文献Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity.
Cell, 168, 2017

 

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