8F2B
 
 | | Amylin 3 Receptor in complex with Gs and Pramlintide analogue peptide San45 | | 分子名称: | (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, ... | | 著者 | Cao, J, Sexton, P.M, Wootten, D.L, Belousoff, M.J. | | 登録日 | 2022-11-07 | | 公開日 | 2023-08-02 | | 最終更新日 | 2024-03-13 | | 実験手法 | ELECTRON MICROSCOPY (2 Å) | | 主引用文献 | Structural insight into selectivity of amylin and calcitonin receptor agonists.
Nat.Chem.Biol., 20, 2024
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8F2A
 | | Human Amylin3 Receptor in complex with Gs and Pramlintide analogue peptide San385 (Cluster 5 conformation) | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Calcitonin receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Cao, J, Sexton, P.M, Wootten, D.L, Radostin, D. | | 登録日 | 2022-11-07 | | 公開日 | 2023-08-02 | | 最終更新日 | 2024-02-14 | | 実験手法 | ELECTRON MICROSCOPY (2.2 Å) | | 主引用文献 | Structural insight into selectivity of amylin and calcitonin receptor agonists.
Nat.Chem.Biol., 20, 2024
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8F0K
 | | Human Amylin3 Receptor in complex with Gs and Pramlintide analogue peptide San385 | | 分子名称: | (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, ... | | 著者 | Cao, J, Sexton, P.M, Wootten, D.L. | | 登録日 | 2022-11-03 | | 公開日 | 2023-08-02 | | 最終更新日 | 2024-02-14 | | 実験手法 | ELECTRON MICROSCOPY (1.9 Å) | | 主引用文献 | Structural insight into selectivity of amylin and calcitonin receptor agonists.
Nat.Chem.Biol., 20, 2024
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8AX7
 | | Crystal structure of a CGRP receptor ectodomain heterodimer bound to macrocyclic inhibitor HTL0031448 | | 分子名称: | (1~{S},10~{R},20~{E})-10-[(1,7-dimethylindazol-5-yl)methyl]-12-methyl-15,18-dioxa-9,12,24,26-tetrazapentacyclo[20.5.2.1^{1,4}.1^{3,7}.0^{25,28}]hentriaconta-3(30),4,6,20,22,24,28-heptaene-8,11,27-trione, ACETATE ION, Maltose/maltodextrin-binding periplasmic protein,Receptor activity-modifying protein 1,Calcitonin gene-related peptide type 1 receptor, ... | | 著者 | Southall, S.M, Watson, S.P. | | 登録日 | 2022-08-30 | | 公開日 | 2022-12-07 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.
Acs Med.Chem.Lett., 13, 2022
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8AX6
 | | Crystal structure of a CGRP receptor ectodomain heterodimer bound to macrocyclic inhibitor HTL0029882 | | 分子名称: | (1~{S},10~{R},20~{E})-12-methyl-10-[(7-methyl-2~{H}-indazol-5-yl)methyl]-15,18-dioxa-9,12,24,26-tetrazapentacyclo[20.5.2.1^{1,4}.1^{3,7}.0^{25,28}]hentriaconta-3(30),4,6,20,22,24,28-heptaene-8,11,27-trione, Maltose/maltodextrin-binding periplasmic protein,Receptor activity-modifying protein 1,Calcitonin gene-related peptide type 1 receptor, TETRAETHYLENE GLYCOL, ... | | 著者 | Southall, S.M, Watson, S.P. | | 登録日 | 2022-08-30 | | 公開日 | 2022-12-07 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.
Acs Med.Chem.Lett., 13, 2022
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8AX5
 | | Crystal structure of a CGRP receptor ectodomain heterodimer bound to macrocyclic inhibitor HTL0029881 | | 分子名称: | (1~{R},10~{R},20~{E})-12-methyl-10-[(7-methyl-2~{H}-indazol-5-yl)methyl]-15,18-dioxa-9,12,24,26-tetrazapentacyclo[20.5.2.1^{1,4}.1^{3,7}.0^{25,28}]hentriaconta-3,5,7(30),20,22,24,28-heptaene-8,11,27-trione, Maltose/maltodextrin-binding periplasmic protein,Receptor activity-modifying protein 1,Calcitonin gene-related peptide type 1 receptor, TETRAETHYLENE GLYCOL, ... | | 著者 | Southall, S.M, Watson, S.P. | | 登録日 | 2022-08-30 | | 公開日 | 2022-12-07 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.75 Å) | | 主引用文献 | Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.
Acs Med.Chem.Lett., 13, 2022
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7TZF
 | | Human Amylin3 Receptor in complex with Gs and rat amylin peptide | | 分子名称: | (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, ... | | 著者 | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | 登録日 | 2022-02-15 | | 公開日 | 2022-03-23 | | 最終更新日 | 2022-04-06 | | 実験手法 | ELECTRON MICROSCOPY (2.4 Å) | | 主引用文献 | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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7TYY
 | | Human Amylin2 Receptor in complex with Gs and salmon calcitonin 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 | 2022-03-23 | | 最終更新日 | 2022-04-06 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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7TYX
 | | 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
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7TYW
 | | Human Amylin1 Receptor in complex with Gs and salmon calcitonin 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 | 2022-03-23 | | 最終更新日 | 2022-04-06 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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7TYH
 | | Human Amylin2 Receptor in complex with Gs and human calcitonin peptide | | 分子名称: | Calcitonin, Calcitonin receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | 登録日 | 2022-02-13 | | 公開日 | 2022-03-23 | | 最終更新日 | 2022-04-06 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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7TYF
 | | Human Amylin1 Receptor in complex with Gs and rat amylin peptide | | 分子名称: | (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, ... | | 著者 | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | 登録日 | 2022-02-13 | | 公開日 | 2022-03-23 | | 最終更新日 | 2022-04-06 | | 実験手法 | ELECTRON MICROSCOPY (2.2 Å) | | 主引用文献 | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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7P0I
 | | Crystal structure of a CGRP receptor ectodomain heterodimer bound to macrocyclic inhibitor Compound 13 | | 分子名称: | (1S,20E)-10-(benzofuran-3-ylmethyl)-12-methyl-15,18-dioxa-5,9,12,24,26-pentazapentacyclo[20.5.2.11,4.13,7.025,28]hentriaconta-3(30),4,6,20,22(29),23,25(28)-heptaene-8,11,27-trione, Maltose/maltodextrin-binding periplasmic protein,Receptor activity-modifying protein 1,Calcitonin gene-related peptide type 1 receptor, TETRAETHYLENE GLYCOL, ... | | 著者 | Southall, S.M. | | 登録日 | 2021-06-29 | | 公開日 | 2022-06-15 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes.
Acs Chem Neurosci, 13, 2022
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7P0F
 | | Crystal structure of a CGRP receptor ectodomain heterodimer bound to macrocyclic inhibitor HTL0028125 | | 分子名称: | (1S,10R,23E)-12-methyl-10-[(7-methyl-1H-indazol-5-yl)methyl]-15,18,21-trioxa-5,9,12,27,29-pentazapentacyclo[23.5.2.11,4.13,7.028,31]tetratriaconta-3(33),4,6,23,25(32),26,28(31)-heptaene-8,11,30-trione, Maltose/maltodextrin-binding periplasmic protein,Receptor activity-modifying protein 1,Calcitonin gene-related peptide type 1 receptor, TETRAETHYLENE GLYCOL, ... | | 著者 | Southall, S.M, Watson, S.P. | | 登録日 | 2021-06-29 | | 公開日 | 2022-06-15 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes.
Acs Chem Neurosci, 13, 2022
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7KNU
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7KNT
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6ZIS
 | | Crystal structure of a CGRP receptor ectodomain heterodimer with bound high affinity inhibitor | | 分子名称: | Maltose/maltodextrin-binding periplasmic protein,Receptor activity-modifying protein 1,Calcitonin gene-related peptide type 1 receptor, N-{(1S)-5-amino-1-[(4-pyridin-4-ylpiperazin-1-yl)carbonyl]pentyl}-3,5-dibromo-Nalpha-{[4-(2-oxo-1,4-dihydroquinazolin-3 (2H)-yl)piperidin-1-yl]carbonyl}-D-tyrosinamide, TETRAETHYLENE GLYCOL, ... | | 著者 | Southall, S.M. | | 登録日 | 2020-06-26 | | 公開日 | 2020-07-15 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (1.73 Å) | | 主引用文献 | Structure-Based Drug Discovery ofN-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine.
J.Med.Chem., 63, 2020
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6ZHO
 | | Crystal structure of a CGRP receptor ectodomain heterodimer with bound high affinity inhibitor | | 分子名称: | Maltose/maltodextrin-binding periplasmic protein,Receptor activity-modifying protein 1,Calcitonin gene-related peptide type 1 receptor, TETRAETHYLENE GLYCOL, alpha-D-glucopyranose-(1-4)-alpha-D-glucopyranose, ... | | 著者 | Southall, S.M. | | 登録日 | 2020-06-23 | | 公開日 | 2020-07-15 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Structure-Based Drug Discovery ofN-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine.
J.Med.Chem., 63, 2020
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6V2E
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6UVA
 | | CryoEM Structure of the active Adrenomedullin 2 receptor G protein complex with adrenomedullin 2 peptide | | 分子名称: | 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, ... | | 著者 | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | 登録日 | 2019-11-01 | | 公開日 | 2020-04-01 | | 最終更新日 | 2020-04-29 | | 実験手法 | ELECTRON MICROSCOPY (2.3 Å) | | 主引用文献 | 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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6UUS
 | | CryoEM Structure of the active Adrenomedullin 2 receptor G protein complex with adrenomedullin peptide | | 分子名称: | ADM, Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | 登録日 | 2019-10-31 | | 公開日 | 2020-04-01 | | 最終更新日 | 2020-04-29 | | 実験手法 | ELECTRON MICROSCOPY (2.4 Å) | | 主引用文献 | 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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6UUN
 | | CryoEM Structure of the active Adrenomedullin 1 receptor G protein complex with adrenomedullin peptide | | 分子名称: | ADM, Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | 登録日 | 2019-10-30 | | 公開日 | 2020-03-25 | | 最終更新日 | 2020-04-29 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | 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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6UMG
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6E3Y
 | | Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor | | 分子名称: | Calcitonin gene-related peptide 1, Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Liang, Y.L, Khoshouei, M, Deganutti, G, Glukhova, A, Koole, C, Peat, T.S, Radjainia, M, Plitzko, J.M, Baumeister, W, Miller, L.J, Hay, D.L, Christopoulos, A, Reynolds, C.A, Wootten, D, Sexton, P.M. | | 登録日 | 2018-07-16 | | 公開日 | 2018-09-19 | | 最終更新日 | 2020-01-15 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor.
Nature, 561, 2018
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6D1U
 | | Crystal structure of the human CLR:RAMP1 extracellular domain heterodimer in complex with adrenomedullin 2/intermedin | | 分子名称: | ADM2, Maltose-binding periplasmic protein,Receptor activity-modifying protein 1,Calcitonin gene-related peptide type 1 receptor, SODIUM ION, ... | | 著者 | Pioszak, A, Roehrkasse, A. | | 登録日 | 2018-04-12 | | 公開日 | 2018-09-05 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.05 Å) | | 主引用文献 | Structure-function analyses reveal a triple beta-turn receptor-bound conformation of adrenomedullin 2/intermedin and enable peptide antagonist design.
J. Biol. Chem., 293, 2018
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