6X1A
 
 | | Non peptide agonist PF-06882961, bound to Glucagon-Like peptide-1 (GLP-1) Receptor | | Descriptor: | 2-[(4-{6-[(4-cyano-2-fluorophenyl)methoxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-{[(2S)-oxetan-2-yl]methyl}-1H-benzimidazole-6-carboxylic acid, 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: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (2.5 Å) | | Cite: | Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.
Mol.Cell, 80, 2020
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7CKF
 | | The N-terminus of interferon-inducible antiviral protein-dimer | | Descriptor: | ALUMINUM FLUORIDE, GUANOSINE-5'-DIPHOSPHATE, Guanylate-binding protein 5, ... | | Authors: | Cui, W, Yang, H.T. | | Deposit date: | 2020-07-16 | | Release date: | 2021-05-05 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.284 Å) | | Cite: | Structural basis for GTP-induced dimerization and antiviral function of guanylate-binding proteins.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7S3I
 | | Ex4-D-Ala bound to the glucagon-like peptide-1 receptor/g protein complex (conformer 2) | | 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: | Belousoff, M.J, Piper, S.J, Danev, R. | | Deposit date: | 2021-09-07 | | Release date: | 2022-01-05 | | Last modified: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (2.51 Å) | | Cite: | Structural and functional diversity among agonist-bound states of the GLP-1 receptor.
Nat.Chem.Biol., 18, 2022
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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: | 2024-10-23 | | 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: | 2024-10-30 | | 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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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: | 2024-10-23 | | 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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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: | 2024-10-30 | | 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: | 2024-10-23 | | 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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7RHY
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7RHZ
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7RHX
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5KJ2
 | | The novel p300/CBP inhibitor A-485 uncovers a unique mechanism of action to target AR in castrate resistant prostate cancer | | Descriptor: | Histone acetyltransferase p300, N-[(4-fluorophenyl)methyl]-2-{(1R)-5-[(methylcarbamoyl)amino]-2',4'-dioxo-2,3-dihydro-3'H-spiro[indene-1,5'-[1,3]oxazolidin]-3'-yl}-N-[(2S)-1,1,1-trifluoropropan-2-yl]acetamide, SODIUM ION | | Authors: | Jakob, C.G, Qiu, W, Edalji, R.P, Sun, C. | | Deposit date: | 2016-06-17 | | Release date: | 2017-09-27 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Nature, 550, 2017
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7N4S
 | | Bruton's tyrosine kinase in complex with compound 65 | | Descriptor: | (3R,3'R)-3-anilino-1'-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)[1,3'-bipiperidin]-2-one, Tyrosine-protein kinase BTK | | Authors: | Metrick, C.M, Marcotte, D.J. | | Deposit date: | 2021-06-04 | | Release date: | 2022-05-18 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.
Bioorg.Med.Chem., 44, 2021
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7N4R
 | | Bruton's tyrosine kinase in complex with compound 21 | | Descriptor: | DIMETHYL SULFOXIDE, N-{2-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]ethyl}-N~2~-phenylglycinamide, Tyrosine-protein kinase BTK | | Authors: | Metrick, C.M, Marcotte, D.J. | | Deposit date: | 2021-06-04 | | Release date: | 2022-05-18 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.62 Å) | | Cite: | Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.
Bioorg.Med.Chem., 44, 2021
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7N4Q
 | | Bruton's tyrosine kinase in complex with compound 45 | | Descriptor: | (2R)-2-(3-chloro-5-fluoroanilino)-2-cyclopropyl-N-[(3R)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-yl]acetamide, Tyrosine-protein kinase BTK | | Authors: | Metrick, C.M, Marcotte, D.J. | | Deposit date: | 2021-06-04 | | Release date: | 2022-05-18 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.
Bioorg.Med.Chem., 44, 2021
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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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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: | 2024-10-09 | | Method: | ELECTRON MICROSCOPY (2.2 Å) | | Cite: | 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 | | Descriptor: | Calcitonin, Calcitonin receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 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 (3.3 Å) | | Cite: | 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 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, Calcitonin receptor, ... | | Authors: | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | Deposit date: | 2022-02-14 | | Release date: | 2022-03-23 | | Last modified: | 2022-04-06 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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7TYO
 | | Calcitonin receptor in complex with Gs and human calcitonin peptide | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, Calcitonin, ... | | Authors: | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | Deposit date: | 2022-02-14 | | Release date: | 2022-03-23 | | Last modified: | 2022-04-06 | | Method: | ELECTRON MICROSCOPY (2.7 Å) | | Cite: | 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 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, Calcitonin receptor, ... | | Authors: | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | Deposit date: | 2022-02-14 | | Release date: | 2022-03-23 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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7TYL
 | | Calcitonin Receptor in complex with Gs and rat amylin peptide, bypass motif | | Descriptor: | 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, ... | | 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: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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7TYN
 | | Calcitonin Receptor in complex with Gs and salmon calcitonin 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: | 2022-03-30 | | Last modified: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | 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 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL HEMISUCCINATE, Calcitonin receptor, ... | | Authors: | Cao, J, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | Deposit date: | 2022-02-14 | | Release date: | 2022-03-30 | | Last modified: | 2024-10-16 | | Method: | ELECTRON MICROSCOPY (2.55 Å) | | Cite: | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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7TYI
 | | Calcitonin Receptor in complex with Gs and rat amylin peptide, CT-like state | | 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, Belousoff, M.J, Johnson, R.M, Wootten, D.L, Sexton, P.M. | | Deposit date: | 2022-02-13 | | Release date: | 2022-03-30 | | Last modified: | 2022-04-06 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | A structural basis for amylin receptor phenotype.
Science, 375, 2022
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