1QE6
 
 | | INTERLEUKIN-8 WITH AN ADDED DISULFIDE BETWEEN RESIDUES 5 AND 33 (L5C/H33C) | | Descriptor: | INTERLEUKIN-8 VARIANT, SULFATE ION | | Authors: | Gerber, N, Lowman, H, Artis, D.R, Eigenbrot, C. | | Deposit date: | 1999-07-13 | | Release date: | 2000-03-22 | | Last modified: | 2018-01-31 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | Receptor-binding conformation of the "ELR" motif of IL-8: X-ray structure of the L5C/H33C variant at 2.35 A resolution.
Proteins, 38, 2000
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1ICW
 | | INTERLEUKIN-8, MUTANT WITH GLU 38 REPLACED BY CYS AND CYS 50 REPLACED BY ALA | | Descriptor: | INTERLEUKIN-8 | | Authors: | Eigenbrot, C, Lowman, H.B, Chee, L, Artis, D.R. | | Deposit date: | 1996-09-18 | | Release date: | 1997-03-12 | | Last modified: | 2021-11-03 | | Method: | X-RAY DIFFRACTION (2.01 Å) | | Cite: | Structural change and receptor binding in a chemokine mutant with a rearranged disulfide: X-ray structure of E38C/C50AIL-8 at 2 A resolution.
Proteins, 27, 1997
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1TB5
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With AMP | | Descriptor: | ADENOSINE MONOPHOSPHATE, MAGNESIUM ION, ZINC ION, ... | | Authors: | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | | Deposit date: | 2004-05-19 | | Release date: | 2004-08-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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1TB7
 | | Catalytic Domain Of Human Phosphodiesterase 4D In Complex With AMP | | Descriptor: | 1,2-ETHANEDIOL, 2-[3-(2-HYDROXY-1,1-DIHYDROXYMETHYL-ETHYLAMINO)-PROPYLAMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ADENOSINE MONOPHOSPHATE, ... | | Authors: | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | | Deposit date: | 2004-05-19 | | Release date: | 2004-08-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.63 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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1TBF
 | | Catalytic Domain Of Human Phosphodiesterase 5A in Complex with Sildenafil | | Descriptor: | 5-{2-ETHOXY-5-[(4-METHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-1-METHYL-3-PROPYL-1H,6H,7H-PYRAZOLO[4,3-D]PYRIMIDIN-7-ONE, GLYCEROL, MAGNESIUM ION, ... | | Authors: | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | | Deposit date: | 2004-05-20 | | Release date: | 2004-08-03 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.3 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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1T9R
 | | Catalytic Domain Of Human Phosphodiesterase 5A | | Descriptor: | CITRIC ACID, PHOSPHATE ION, ZINC ION, ... | | Authors: | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | | Deposit date: | 2004-05-18 | | Release date: | 2004-08-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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1TAZ
 | | Catalytic Domain Of Human Phosphodiesterase 1B | | Descriptor: | Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B, MAGNESIUM ION, ZINC ION | | Authors: | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | | Deposit date: | 2004-05-19 | | Release date: | 2004-08-03 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.77 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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1T9S
 | | Catalytic Domain Of Human Phosphodiesterase 5A in Complex with GMP | | Descriptor: | GUANOSINE-5'-MONOPHOSPHATE, MAGNESIUM ION, ZINC ION, ... | | Authors: | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | | Deposit date: | 2004-05-18 | | Release date: | 2004-08-03 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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1TBB
 | | Catalytic Domain Of Human Phosphodiesterase 4D In Complex With Rolipram | | Descriptor: | 1,2-ETHANEDIOL, MAGNESIUM ION, ROLIPRAM, ... | | Authors: | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | | Deposit date: | 2004-05-19 | | Release date: | 2004-08-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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4I5M
 | | Selective & Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors that Reduce -Synuclein Phosphorylation in Rat Brain | | Descriptor: | 4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide, Serine/threonine-protein kinase PLK2 | | Authors: | Aubele, D.L, Hom, R.K, Adler, M, Galemmo Jr, R.A, Bowers, S, Truong, A.P, Pan, H, Beroza, P, Neitz, R.J, Yao, N, Lin, M, Tonn, G, Zhang, H, Bova, M.P, Ren, Z, Tam, D, Ruslim, L, Baker, J, Diep, L, Fitzgerald, K, Hoffman, J, Motter, R, Fauss, D, Tanaka, P, Dappen, M, Jagodzinski, J, Chan, W, Konradi, A.W, Latimer, L, Zhu, Y.L, Artis, D.R, Sham, H.L, Anderson, J.P, Bergeron, M. | | Deposit date: | 2012-11-28 | | Release date: | 2013-12-25 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (1.801 Å) | | Cite: | Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce alpha-synuclein phosphorylation in rat brain.
Chemmedchem, 8, 2013
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4I11
 | | Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates. | | Descriptor: | Beta-secretase 1, N-(3,3-dimethyl-3,4-dihydroisoquinolin-1-yl)-L-phenylalanine, ZINC ION | | Authors: | Bowers, B, Xu, Y, Yuan, S, Probst, G.D, Hom, R.K, Chan, W, Konradi, A.W, Sham, H.L, Zhu, Y.L, Beroza, P, Pan, H, Brecht, E, Yao, N, Lougheed, J, Artis, D.R, Tam, D, Bova, M. | | Deposit date: | 2012-11-19 | | Release date: | 2013-03-06 | | Last modified: | 2013-04-24 | | Method: | X-RAY DIFFRACTION (1.89 Å) | | Cite: | Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.
Bioorg.Med.Chem.Lett., 23, 2013
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1XM4
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Piclamilast | | Descriptor: | 3-(CYCLOPENTYLOXY)-N-(3,5-DICHLOROPYRIDIN-4-YL)-4-METHOXYBENZAMIDE, MAGNESIUM ION, ZINC ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-10-01 | | Release date: | 2004-12-14 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.31 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
STRUCTURE, 12, 2004
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1XLZ
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Filaminast | | Descriptor: | (1E)-1-[3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL]ETHANONE O-(AMINOCARBONYL)OXIME, MAGNESIUM ION, ZINC ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-09-30 | | Release date: | 2004-12-14 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.06 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
STRUCTURE, 12, 2004
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1XOT
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Vardenafil | | Descriptor: | 2-{2-ETHOXY-5-[(4-ETHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-5-METHYL-7-PROPYLIMIDAZO[5,1-F][1,2,4]TRIAZIN-4(1H)-ONE, MAGNESIUM ION, ZINC ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-10-06 | | Release date: | 2004-12-14 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.34 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
STRUCTURE, 12, 2004
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1XLX
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Cilomilast | | Descriptor: | CILOMILAST, MAGNESIUM ION, ZINC ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-09-30 | | Release date: | 2004-12-14 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.19 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
Structure, 12, 2004
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1XM6
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With (R)-Mesopram | | Descriptor: | (5R)-5-(4-methoxy-3-propoxyphenyl)-5-methyl-1,3-oxazolidin-2-one, MAGNESIUM ION, ZINC ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-10-01 | | Release date: | 2004-12-14 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.92 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
STRUCTURE, 12, 2004
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1XOS
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Sildenafil | | Descriptor: | 5-{2-ETHOXY-5-[(4-METHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-1-METHYL-3-PROPYL-1H,6H,7H-PYRAZOLO[4,3-D]PYRIMIDIN-7-ONE, MAGNESIUM ION, SULFATE ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-10-06 | | Release date: | 2004-12-14 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.28 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
STRUCTURE, 12, 2004
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1XOZ
 | | Catalytic Domain Of Human Phosphodiesterase 5A In Complex With Tadalafil | | Descriptor: | 6-BENZO[1,3]DIOXOL-5-YL-2-METHYL-2,3,6,7,12,12A-HEXAHYDRO-PYRAZINO[1',2':1,6]PYRIDO[3,4-B]INDOLE-1,4-DIONE, MAGNESIUM ION, ZINC ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-10-07 | | Release date: | 2004-12-14 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.37 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
STRUCTURE, 12, 2004
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1XOR
 | | Catalytic Domain Of Human Phosphodiesterase 4D In Complex With Zardaverine | | Descriptor: | 6-(4-DIFLUOROMETHOXY-3-METHOXY-PHENYL)-2H-PYRIDAZIN-3-ONE, MAGNESIUM ION, ZINC ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-10-06 | | Release date: | 2004-12-14 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.54 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
STRUCTURE, 12, 2004
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1YGC
 | | Short Factor VIIa with a small molecule inhibitor | | Descriptor: | (R)-4-[2-(3-AMINO-BENZENESULFONYLAMINO)-1-(3,5-DIETHOXY-2-FLUOROPHENYL)-2-OXO-ETHYLAMINO]-2-HYDROXY-BENZAMIDINE, CALCIUM ION, Coagulation factor VII, ... | | Authors: | Olivero, A.G, Eigenbrot, C, Goldsmith, R, Robarge, K, Artis, D.R, Flygare, J, Rawson, T, Refino, C, Bunting, S, Kirchhofer, D. | | Deposit date: | 2005-01-04 | | Release date: | 2005-01-18 | | Last modified: | 2024-10-09 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
J.Biol.Chem., 280, 2005
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1Y2E
 | | Catalytic Domain Of Human Phosphodiesterase 4D In Complex With 1-(4-amino-phenyl)-3,5-dimethyl-1H-pyrazole-4-carboxylic acid ethyl ester | | Descriptor: | 1,2-ETHANEDIOL, 1-(4-AMINOPHENYL)-3,5-DIMETHYL-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ... | | Authors: | Card, G.L, Blasdel, L, England, B.P, Zhang, C, Suzuki, Y, Gillette, S, Fong, D, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 2005
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1Y2J
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With 3,5-dimethyl-1-(3-nitro-phenyl)-1H-pyrazole-4-carboxylic acid ethyl ester | | Descriptor: | 3,5-DIMETHYL-1-(3-NITROPHENYL)-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ZINC ION, ... | | Authors: | Card, G.L, Blasdel, L, England, B.P, Zhang, C, Suzuki, Y, Gillette, S, Fong, D, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 2005
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1Y2D
 | | Catalytic Domain Of Human Phosphodiesterase 4D In Complex With 1-(4-methoxy-phenyl)-3,5-dimethyl-1H-pyrazole-4-carboxylic acid ethyl ester | | Descriptor: | 1,2-ETHANEDIOL, 1-(4-METHOXYPHENYL)-3,5-DIMETHYL-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, 2-[3-(2-HYDROXY-1,1-DIHYDROXYMETHYL-ETHYLAMINO)-PROPYLAMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ... | | Authors: | Card, G.L, Blasdel, L, England, B.P, Zhang, C, Suzuki, Y, Gillette, S, Fong, D, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 2005
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1XMU
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Roflumilast | | Descriptor: | 3-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLOROPYRIDIN-4-YL)-4-(DIFLUOROMETHOXY)BENZAMIDE, MAGNESIUM ION, ZINC ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-10-04 | | Release date: | 2004-12-14 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
STRUCTURE, 12, 2004
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1XOQ
 | | Catalytic Domain Of Human Phosphodiesterase 4D In Complex With Roflumilast | | Descriptor: | 1,2-ETHANEDIOL, 3-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLOROPYRIDIN-4-YL)-4-(DIFLUOROMETHOXY)BENZAMIDE, MAGNESIUM ION, ... | | Authors: | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | | Deposit date: | 2004-10-06 | | Release date: | 2004-12-14 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.83 Å) | | Cite: | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases.
STRUCTURE, 12, 2004
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