1VGH
 
 | | HEPARIN-BINDING DOMAIN FROM VASCULAR ENDOTHELIAL GROWTH FACTOR, NMR, 20 STRUCTURES | | Descriptor: | VASCULAR ENDOTHELIAL GROWTH FACTOR-165 | | Authors: | Fairbrother, W.J, Champe, M.A, Christinger, H.W, Keyt, B.A, Starovasnik, M.A. | | Deposit date: | 1997-12-17 | | Release date: | 1998-04-08 | | Last modified: | 2024-11-20 | | Method: | SOLUTION NMR | | Cite: | Solution structure of the heparin-binding domain of vascular endothelial growth factor.
Structure, 6, 1998
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2VGH
 | | HEPARIN-BINDING DOMAIN FROM VASCULAR ENDOTHELIAL GROWTH FACTOR, NMR, MINIMIZED AVERAGE STRUCTURE | | Descriptor: | VASCULAR ENDOTHELIAL GROWTH FACTOR-165 | | Authors: | Fairbrother, W.J, Champe, M.A, Christinger, H.W, Keyt, B.A, Starovasnik, M.A. | | Deposit date: | 1997-12-17 | | Release date: | 1998-04-08 | | Last modified: | 2024-11-20 | | Method: | SOLUTION NMR | | Cite: | Solution structure of the heparin-binding domain of vascular endothelial growth factor.
Structure, 6, 1998
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1MGS
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1ANP
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2I3H
 | | Structure of an ML-IAP/XIAP chimera bound to a 4-mer peptide (AVPW) | | Descriptor: | 1,2-ETHANEDIOL, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, AVPW peptide, ... | | Authors: | Fairbrother, W.J, Franklin, M.C. | | Deposit date: | 2006-08-18 | | Release date: | 2006-09-19 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.62 Å) | | Cite: | Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.
Acs Chem.Biol., 1, 2006
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2I3I
 | | Structure of an ML-IAP/XIAP chimera bound to a peptidomimetic | | Descriptor: | (3R,6R,9AR)-2,2-DIMETHYL-6-[(N-METHYL-L-ALANYL)AMINO]-N-(3-METHYL-1-PHENYL-1H-PYRAZOL-5-YL)-5-OXO-2,3,5,6,9,9A-HEXAHYDRO[1,3]THIAZOLO[3,2-A]AZEPINE-3-CARBOXAMIDE, 1,2-ETHANEDIOL, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ... | | Authors: | Fairbrother, W.J, Franklin, M.C. | | Deposit date: | 2006-08-18 | | Release date: | 2006-09-19 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.
Acs Chem.Biol., 1, 2006
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3GTA
 | | Structure of an ML-IAP/XIAP chimera bound to a peptidomimetic | | Descriptor: | 1,2-ETHANEDIOL, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Baculoviral IAP repeat-containing 7, ... | | Authors: | Franklin, M.C, Fairbrother, W.J, Cohen, F. | | Deposit date: | 2009-03-27 | | Release date: | 2010-03-09 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.
Bioorg.Med.Chem.Lett., 20, 2010
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3GT9
 | | Structure of an ML-IAP/XIAP chimera bound to a peptidomimetic | | Descriptor: | Baculoviral IAP repeat-containing 7, N-{(1S)-1-cyclohexyl-2-[(2S)-2-(4-naphthalen-1-yl-1,3-thiazol-2-yl)pyrrolidin-1-yl]-2-oxoethyl}-N~2~-methyl-L-alaninamide, ZINC ION | | Authors: | Franklin, M.C, Fairbrother, W.J, Cohen, F. | | Deposit date: | 2009-03-27 | | Release date: | 2010-03-09 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.
Bioorg.Med.Chem.Lett., 20, 2010
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1VPP
 | | COMPLEX BETWEEN VEGF AND A RECEPTOR BLOCKING PEPTIDE | | Descriptor: | PROTEIN (PEPTIDE V108), PROTEIN (VASCULAR ENDOTHELIAL GROWTH FACTOR) | | Authors: | Wiesmann, C, Christinger, H.W, Cochran, A.G, Cunningham, B.C, Fairbrother, W.J, Keenan, C.J, Meng, G, de Vos, A.M. | | Deposit date: | 1998-10-09 | | Release date: | 1999-02-23 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Crystal structure of the complex between VEGF and a receptor-blocking peptide.
Biochemistry, 37, 1998
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3F7I
 | | Structure of an ML-IAP/XIAP chimera bound to a peptidomimetic | | Descriptor: | 1,2-ETHANEDIOL, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Baculoviral IAP repeat-containing protein 7, ... | | Authors: | Franklin, M.C, Fairbrother, W.J, Cohen, F. | | Deposit date: | 2008-11-09 | | Release date: | 2009-03-17 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold
J.Med.Chem., 52, 2009
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3F7H
 | | Structure of an ML-IAP/XIAP chimera bound to a peptidomimetic | | Descriptor: | 1,2-ETHANEDIOL, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Baculoviral IAP repeat-containing protein 7, ... | | Authors: | Franklin, M.C, Fairbrother, W.J, Cohen, F. | | Deposit date: | 2008-11-09 | | Release date: | 2009-03-17 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold
J.Med.Chem., 52, 2009
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3F7G
 | | Structure of the BIR domain from ML-IAP bound to a peptidomimetic | | Descriptor: | 3,6,9,12,15,18-HEXAOXAICOSANE-1,20-DIOL, Baculoviral IAP repeat-containing protein 7, L-alanyl-L-valyl-N-(2,2-diphenylethyl)-L-prolinamide, ... | | Authors: | Franklin, M.C, Fairbrother, W.J, Cohen, F. | | Deposit date: | 2008-11-09 | | Release date: | 2009-03-17 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold
J.Med.Chem., 52, 2009
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3T6P
 | | IAP antagonist-induced conformational change in cIAP1 promotes E3 ligase activation via dimerization | | Descriptor: | Baculoviral IAP repeat-containing protein 2, ZINC ION | | Authors: | Dueber, E.C, Schoeffler, A.J, Lingel, A, Elliott, M, Fedorova, A.V, Giannetti, A.M, Zobel, K, Maurer, B, Varfolomeev, E, Wu, P, Wallweber, H, Hymowitz, S, Deshayes, K, Vucic, D, Fairbrother, W.J. | | Deposit date: | 2011-07-28 | | Release date: | 2011-11-02 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (1.897 Å) | | Cite: | Antagonists induce a conformational change in cIAP1 that promotes autoubiquitination.
Science, 334, 2011
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6OXB
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6E26
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6E25
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1TW6
 | | Structure of an ML-IAP/XIAP chimera bound to a 9mer peptide derived from Smac | | Descriptor: | 1,2-ETHANEDIOL, 2-[BIS-(2-HYDROXY-ETHYL)-AMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Baculoviral IAP repeat-containing protein 7, ... | | Authors: | Franklin, M.C, Vucic, D, Wallweber, H.J.A, Das, K, Shin, H, Elliott, L.O, Kadkhodayan, S, Deshayes, K, Salvesen, G.S, Fairbrother, W.J. | | Deposit date: | 2004-06-30 | | Release date: | 2004-11-02 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.713 Å) | | Cite: | Engineering ML-IAP to produce an extraordinarily potent caspase 9 inhibitor: implications for Smac-dependent anti-apoptotic activity of ML-IAP
Biochem.J., 385, 2005
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2AW0
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6E27
 | | The CARD9 CARD domain-swapped dimer with a zinc ion bound to one of the two zinc binding sites | | Descriptor: | Caspase recruitment domain-containing protein 9, ZINC ION | | Authors: | Holliday, M.J, Ferrao, R, Boenig, G, Deuber, E.C, Fairbrother, W.J. | | Deposit date: | 2018-07-10 | | Release date: | 2018-09-26 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.811 Å) | | Cite: | Picomolar zinc binding modulates formation of Bcl10-nucleating assemblies of the caspase recruitment domain (CARD) of CARD9.
J. Biol. Chem., 293, 2018
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6E28
 | | The CARD9 CARD domain-swapped dimer | | Descriptor: | Caspase recruitment domain-containing protein 9 | | Authors: | Holliday, M.J, Ferrao, R, Boenig, G, Deuber, E.C, Fairbrother, W.J. | | Deposit date: | 2018-07-10 | | Release date: | 2018-09-26 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (1.36 Å) | | Cite: | Picomolar zinc binding modulates formation of Bcl10-nucleating assemblies of the caspase recruitment domain (CARD) of CARD9.
J. Biol. Chem., 293, 2018
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9BJU
 | | Crystal structure of the complex between VHL, ElonginB, ElonginC, and compound 5 | | Descriptor: | 1,2-ETHANEDIOL, 3-PYRIDIN-4-YL-2,4-DIHYDRO-INDENO[1,2-.C.]PYRAZOLE, ACETATE ION, ... | | Authors: | Murray, J.M, Wu, H, Fuhrmann, J, Fairbrother, W.J, DiPasquale, A. | | Deposit date: | 2024-04-25 | | Release date: | 2024-05-29 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (2.47 Å) | | Cite: | Potency-Enhanced Peptidomimetic VHL Ligands with Improved Oral Bioavailability.
J.Med.Chem., 67, 2024
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9BOL
 | | Crystal structure of the complex between VHL, ElonginB, ElonginC, and compound 5 | | Descriptor: | (4R)-1-[(2S)-2-(4-cyclopropyl-1H-1,2,3-triazol-1-yl)-3,3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}-L-prolinamide, 1,2-ETHANEDIOL, CHLORIDE ION, ... | | Authors: | Murray, J.M, Wu, H, Fuhrmann, J, Fairbrother, W.J, DiPasquale, A. | | Deposit date: | 2024-05-03 | | Release date: | 2024-05-29 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (1.99 Å) | | Cite: | Potency-Enhanced Peptidomimetic VHL Ligands with Improved Oral Bioavailability.
J.Med.Chem., 67, 2024
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6N2P
 | | Helical assembly of the CARD9 CARD | | Descriptor: | Caspase recruitment domain-containing protein 9 | | Authors: | Holliday, M.J, Rohou, A, Arthur, C.P, Dueber, E.C, Fairbrother, W.J. | | Deposit date: | 2018-11-13 | | Release date: | 2019-07-03 | | Last modified: | 2024-03-20 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Structures of autoinhibited and polymerized forms of CARD9 reveal mechanisms of CARD9 and CARD11 activation.
Nat Commun, 10, 2019
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6N2M
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5EMW
 | | Crystal structure of the palmitoylated human TEAD3 transcription factor | | Descriptor: | CALCIUM ION, Transcriptional enhancer factor TEF-5 | | Authors: | Noland, C.L, Gierke, S, Schnier, P.D, Murray, J, Sandoval, W.N, Sagolla, M, Dey, A, Hannoush, R.N, Fairbrother, W.J, Cunningham, C.N. | | Deposit date: | 2015-11-06 | | Release date: | 2015-12-23 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Palmitoylation of TEAD Transcription Factors Is Required for Their Stability and Function in Hippo Pathway Signaling.
Structure, 24, 2016
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