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6XOX
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BU of 6xox by Molmil
cryo-EM of human GLP-1R bound to non-peptide agonist LY3502970
分子名称: 3-[(1S,2S)-1-(5-[(4S)-2,2-dimethyloxan-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)-2-methylcyclopropyl]-1,2,4-oxadiazol-5(4H)-one, Alpha subunit of Gs with N-terminus swapped with equivalent residues in Gi,Guanine nucleotide-binding protein G(s) subunit alpha isoforms XLas, Glucagon-like peptide 1 receptor, ...
著者Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S.
登録日2020-07-07
公開日2020-11-18
最終更新日2020-12-09
実験手法ELECTRON MICROSCOPY (3.1 Å)
主引用文献Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist.
Proc.Natl.Acad.Sci.USA, 117, 2020
7RGP
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BU of 7rgp by Molmil
cryo-EM of human Glucagon-like peptide 1 receptor GLP-1R bound to tirzepatide
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Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S.
登録日2021-07-15
公開日2022-04-13
実験手法ELECTRON MICROSCOPY (2.9 Å)
主引用文献Structural determinants of dual incretin receptor agonism by tirzepatide.
Proc.Natl.Acad.Sci.USA, 119, 2022
7RBT
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BU of 7rbt by Molmil
cryo-EM structure of human Gastric inhibitory polypeptide receptor GIPR bound to tirzepatide
分子名称: 2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol, Gastric inhibitory polypeptide receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S.
登録日2021-07-06
公開日2022-04-13
実験手法ELECTRON MICROSCOPY (3.08 Å)
主引用文献Structural determinants of dual incretin receptor agonism by tirzepatide.
Proc.Natl.Acad.Sci.USA, 119, 2022
7RG9
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BU of 7rg9 by Molmil
cryo-EM of human Glucagon-like peptide 1 receptor GLP-1R in apo form
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Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S.
登録日2021-07-14
公開日2022-04-13
実験手法ELECTRON MICROSCOPY (3.2 Å)
主引用文献Structural determinants of dual incretin receptor agonism by tirzepatide.
Proc.Natl.Acad.Sci.USA, 119, 2022
7RA3
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BU of 7ra3 by Molmil
cryo-EM of human Gastric inhibitory polypeptide receptor GIPR bound to GIP
分子名称: Gastric inhibitory polypeptide, Gastric inhibitory polypeptide receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S.
登録日2021-06-29
公開日2022-04-13
実験手法ELECTRON MICROSCOPY (3.24 Å)
主引用文献Structural determinants of dual incretin receptor agonism by tirzepatide.
Proc.Natl.Acad.Sci.USA, 119, 2022
6VCB
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BU of 6vcb by Molmil
Cryo-EM structure of the Glucagon-like peptide-1 receptor in complex with G protein, GLP-1 peptide and a positive allosteric modulator
分子名称: 1-[(1R)-1-(2,6-dichloro-3-methoxyphenyl)ethyl]-6-{2-[(2R)-piperidin-2-yl]phenyl}-1H-benzimidazole, Glucagon-like peptide 1, Glucagon-like peptide 1 receptor, ...
著者Sun, B, Feng, D, Bueno, A, Kobilka, B, Sloop, K.
登録日2019-12-20
公開日2020-07-22
最終更新日2020-09-30
実験手法ELECTRON MICROSCOPY (3.3 Å)
主引用文献Structural insights into probe-dependent positive allosterism of the GLP-1 receptor.
Nat.Chem.Biol., 16, 2020
6ORV
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BU of 6orv by Molmil
Non-peptide agonist (TT-OAD2) bound to the Glucagon-Like peptide-1 (GLP-1) Receptor
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, Liang, Y.L, Danev, R.
登録日2019-05-01
公開日2020-01-08
最終更新日2020-01-29
実験手法ELECTRON MICROSCOPY (3 Å)
主引用文献Activation of the GLP-1 receptor by a non-peptidic agonist.
Nature, 577, 2020
4PF9
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BU of 4pf9 by Molmil
Crystal structure of insulin degrading enzyme complexed with inhibitor
分子名称: Insulin-degrading enzyme, ZINC ION, methyl [(2S)-2-[4-({5-[4-({(2S)-2-[(3S)-3-amino-2-oxopiperidin-1-yl]-2-cyclohexylacetyl}amino)phenyl]pentyl}oxy)phenyl]-3-(quinolin-3-yl)propyl]carbamate
著者Wang, Y, Guo, S.
登録日2014-04-28
公開日2015-06-17
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Dual Exosite-binding Inhibitors of Insulin-degrading Enzyme Challenge Its Role as the Primary Mediator of Insulin Clearance in Vivo.
J.Biol.Chem., 290, 2015
4PFC
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BU of 4pfc by Molmil
Crystal structure of insulin degrading enzyme complexed with inhibitor
分子名称: Insulin-degrading enzyme, ZINC ION, methyl [(2S)-2-(5-{5-[4-({(2S)-2-[(3S)-3-amino-2-oxopiperidin-1-yl]-2-cyclohexylacetyl}amino)phenyl]pentyl}-2-fluorophenyl)-3-(quinolin-3-yl)propyl]carbamate
著者Wang, Y, Guo, S.
登録日2014-04-28
公開日2015-06-17
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (2.21 Å)
主引用文献Dual Exosite-binding Inhibitors of Insulin-degrading Enzyme Challenge Its Role as the Primary Mediator of Insulin Clearance in Vivo.
J.Biol.Chem., 290, 2015
4PES
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BU of 4pes by Molmil
Crystal structure of insulin degrading enzyme complexed with inhibitor tert-butyl [(2S)-2-(2,5-difluorophenyl)-3-(quinolin-3-yl)propyl]carbamate
分子名称: Ala-Ala-Ala, Insulin-degrading enzyme, ZINC ION, ...
著者Wang, Y, Guo, S.
登録日2014-04-24
公開日2015-06-17
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (2.21 Å)
主引用文献Crystal structure of IDE complexed with an inhibitor
To Be Published
4PF7
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BU of 4pf7 by Molmil
Crystal structure of insulin degrading enzyme complexed with inhibitor
分子名称: (2S)-2-amino-N-{(1S)-1-cyclohexyl-2-[(4-methylphenyl)amino]-2-oxoethyl}-4-(methylselanyl)butanamide, Insulin-degrading enzyme, ZINC ION
著者Wang, Y, Guo, S.
登録日2014-04-28
公開日2015-06-17
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (2.33 Å)
主引用文献Dual Exosite-binding Inhibitors of Insulin-degrading Enzyme Challenge Its Role as the Primary Mediator of Insulin Clearance in Vivo.
J.Biol.Chem., 290, 2015

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件を2024-07-10に公開中

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