5ML3
 
 | | The crystal structure of PDE6D in complex to Deltasonamide1 | | Descriptor: | Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta, ~{N}1-[(4-chlorophenyl)methyl]-~{N}1-cyclopentyl-~{N}4-[[2-(methylamino)pyrimidin-4-yl]methyl]-~{N}4-(piperidin-4-ylmethyl)benzene-1,4-disulfonamide | | Authors: | Fansa, E.K, Martin-Gago, P, Waldmann, H, Wittinghofer, A. | | Deposit date: | 2016-12-06 | | Release date: | 2017-02-01 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | A PDE6 delta-KRas Inhibitor Chemotype with up to Seven H-Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2.
Angew. Chem. Int. Ed. Engl., 56, 2017
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7Q9Q
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4JV8
 | | The crystal structure of PDE6D in complex with rac-S1 | | Descriptor: | (6R)-6-(pyridin-2-yl)-5,6-dihydrobenzimidazo[1,2-c]quinazoline, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | | Authors: | Gunther, Z, Papke, B, Ismail, S, Vartak, N, Chandra, A, Hoffmann, M, Hahn, S, Triola, G, Wittinghofer, A, Bastiaens, P, Waldmann, H. | | Deposit date: | 2013-03-25 | | Release date: | 2013-05-22 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.45 Å) | | Cite: | Small molecule inhibition of the KRAS PDEd interaction impairs oncogenic KRAS signalling
Nature, 497, 2013
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7PAD
 | | The crystal structure of DW-0254 in complex with PDE6D | | Descriptor: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, GLYCEROL, NICKEL (II) ION, ... | | Authors: | Beaumont, E, Williams, D. | | Deposit date: | 2021-07-29 | | Release date: | 2022-06-08 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.49 Å) | | Cite: | Validation of a small molecule inhibitor of PDE6D-RAS interaction with favorable anti-leukemic effects.
Blood Cancer J, 12, 2022
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5ML2
 | | The crystal structure of PDE6D in complex with inhibitor-3 | | Descriptor: | Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta, ~{N}1-[(4-chlorophenyl)methyl]-~{N}1-cyclopentyl-~{N}4-(phenylmethyl)benzene-1,4-disulfonamide | | Authors: | Fansa, E.K, Martin-Gago, P, Waldmann, H, Wittinghofer, A. | | Deposit date: | 2016-12-06 | | Release date: | 2017-02-01 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | A PDE6 delta-KRas Inhibitor Chemotype with up to Seven H-Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2.
Angew. Chem. Int. Ed. Engl., 56, 2017
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3T5G
 | | Structure of fully modified farnesylated Rheb in complex with PDE6D | | Descriptor: | FARNESYL, GTP-binding protein Rheb, GUANOSINE-5'-DIPHOSPHATE, ... | | Authors: | Ismail, S.A, Chen, Y.-X, Wittinghofer, A. | | Deposit date: | 2011-07-27 | | Release date: | 2011-10-26 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Arl2-GTP and Arl3-GTP regulate a GDI-like transport system for farnesylated cargo.
Nat.Chem.Biol., 7, 2011
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4JVB
 | | Crystal structure of PDE6D in complex with the inhibitor rac-2 | | Descriptor: | 1-benzyl-2-(4-{[(2R)-2-(2-phenyl-1H-benzimidazol-1-yl)pent-4-en-1-yl]oxy}phenyl)-1H-benzimidazole, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | | Authors: | Gunther, Z, Papke, B, Ismail, S, Vartak, N, Chandra, A, Hoffmann, M, Hahn, S, Triola, G, Wittinghofer, A, Bastiaens, P, Waldmann, H. | | Deposit date: | 2013-03-25 | | Release date: | 2013-05-22 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Small molecule inhibition of the KRAS PDEd interaction impairs oncogenic KRAS signalling
Nature, 497, 2013
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1KSH
 | | Complex of Arl2 and PDE delta, Crystal Form 2 (native) | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, PHOSPHATE ION, ... | | Authors: | Hanzal-Bayer, M, Renault, L, Roversi, P, Wittinghofer, A, Hillig, R.C. | | Deposit date: | 2002-01-13 | | Release date: | 2002-05-08 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | The complex of Arl2-GTP and PDE delta: from structure to function.
EMBO J., 21, 2002
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7Q9S
 | | Crystal structure of PDE6D KRas peptide complex with Compound-1 | | Descriptor: | 1,2-ETHANEDIOL, 2-methyl-3-(1~{H}-pyrazol-5-yl)imidazo[1,2-a]pyridine, DIMETHYL SULFOXIDE, ... | | Authors: | Yelland, T, Ismail, S. | | Deposit date: | 2021-11-14 | | Release date: | 2022-01-19 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Stabilization of the RAS:PDE6D Complex Is a Novel Strategy to Inhibit RAS Signaling.
J.Med.Chem., 65, 2022
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7PAE
 | | The crystal structure of Deltarasin in complex with PDE6D | | Descriptor: | ACETIC ACID, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta, deltarasin | | Authors: | Beaumont, E, Williams, D. | | Deposit date: | 2021-07-29 | | Release date: | 2022-06-08 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Validation of a small molecule inhibitor of PDE6D-RAS interaction with favorable anti-leukemic effects.
Blood Cancer J, 12, 2022
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5F2U
 | | Structure of Fully modified farnesylated INPP5E Peptide in complex with PDE6D | | Descriptor: | FARNESYL, Phosphatidylinositol 4,5-bisphosphate 5-phosphatase, s-farnesyl-l-cysteine methyl ester, ... | | Authors: | Fansa, E.K, Isamil, S, Wittinghofer, A. | | Deposit date: | 2015-12-02 | | Release date: | 2016-04-13 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | PDE6delta-mediated sorting of INPP5E into the cilium is determined by cargo-carrier affinity.
Nat Commun, 7, 2016
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4JV6
 | | The crystal structure of PDE6D in complex to inhibitor-1 | | Descriptor: | 1-benzyl-2-phenyl-1H-benzimidazole, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | | Authors: | Gunther, Z, Papke, B, Ismail, S, Vartak, N, Chandra, A, Hoffmann, M, Hahn, S, Triola, G, Wittinghofer, A, Bastiaens, P, Waldmann, H. | | Deposit date: | 2013-03-25 | | Release date: | 2013-05-22 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.87 Å) | | Cite: | Small molecule inhibition of the KRAS PDEd interaction impairs oncogenic KRAS signalling
Nature, 497, 2013
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5ML6
 | | The crystal structure of PDE6D in complex to inhibitor-8 | | Descriptor: | 2-azanyl-4-[[[4-[(4-chlorophenyl)methyl-cyclopentyl-sulfamoyl]phenyl]sulfonyl-(piperidin-4-ylmethyl)amino]methyl]benzoic acid, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | | Authors: | Fansa, E.K, Martin-gago, P, Waldmann, H, Wittinghofer, A. | | Deposit date: | 2016-12-06 | | Release date: | 2017-02-01 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.87 Å) | | Cite: | A PDE6 delta-KRas Inhibitor Chemotype with up to Seven H-Bonds and Picomolar Affinity that Prevents Efficient Inhibitor Release by Arl2.
Angew. Chem. Int. Ed. Engl., 56, 2017
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5TAR
 | | Crystal structure of farnesylated and methylated kras4b in complex with PDE-delta (crystal form II - with ordered hypervariable region) | | Descriptor: | 1,2-ETHANEDIOL, FARNESYL, GTPase KRas, ... | | Authors: | Dharmaiah, S, Tran, T.H, Simanshu, D.K. | | Deposit date: | 2016-09-10 | | Release date: | 2016-11-02 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structural basis of recognition of farnesylated and methylated KRAS4b by PDE delta.
Proc.Natl.Acad.Sci.USA, 113, 2016
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4JHP
 | | The crystal structure of the RPGR RCC1-like domain in complex with PDE6D | | Descriptor: | Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta, X-linked retinitis pigmentosa GTPase regulator | | Authors: | Waetzlich, D, Vetter, I, Wittinghofer, A, Ismail, S. | | Deposit date: | 2013-03-05 | | Release date: | 2013-04-17 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | The interplay between RPGR, PDE-delta and Arl2/3 regulate the ciliary targeting of farnesylated cargo.
Embo Rep., 14, 2013
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7QF9
 | | Crystal structure of PDE6D bound to HRas peptide | | Descriptor: | 1,2-ETHANEDIOL, FARNESYL, HRas peptide, ... | | Authors: | Yelland, T, Ismail, I. | | Deposit date: | 2021-12-05 | | Release date: | 2022-02-09 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Stabilization of the RAS:PDE6D Complex Is a Novel Strategy to Inhibit RAS Signaling.
J.Med.Chem., 65, 2022
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5X72
 | | The crystal Structure PDE delta in complex with (rac)-p9 | | Descriptor: | (2R)-2-(2-fluorophenyl)-3-phenyl-1,2-dihydroquinazolin-4-one, (2S)-2-(2-fluorophenyl)-3-phenyl-1,2-dihydroquinazolin-4-one, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | | Authors: | Jiang, Y, Zhuang, C, Chen, L, Wang, R, Wang, F, Sheng, C. | | Deposit date: | 2017-02-23 | | Release date: | 2017-10-04 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Structural Biology-Inspired Discovery of Novel KRAS-PDE delta Inhibitors
J. Med. Chem., 60, 2017
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5YAV
 | | Fragment-based Drug Discovery of inhibitors to block PDEdelta-RAS protein-protein interaction | | Descriptor: | 1-phenyl-5-propan-2-ylsulfanyl-1,2,3,4-tetrazole, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | | Authors: | Bing, X, Yanlian, L, Danyan, C. | | Deposit date: | 2017-09-01 | | Release date: | 2018-09-05 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (1.989 Å) | | Cite: | Fragment-based Drug Discovery of inhibitors to block PDEdelta-RAS protein-protein interaction
To Be Published
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5TB5
 | | Crystal structure of full-length farnesylated and methylated KRAS4b in complex with PDE-delta (crystal form I - with partially disordered hypervariable region) | | Descriptor: | 1,2-ETHANEDIOL, FARNESYL, GTPase KRas, ... | | Authors: | Dharmaiah, S, Tran, T.H, Simanshu, D.K. | | Deposit date: | 2016-09-11 | | Release date: | 2016-11-02 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structural basis of recognition of farnesylated and methylated KRAS4b by PDE delta.
Proc.Natl.Acad.Sci.USA, 113, 2016
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5YAW
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7PAC
 | | The crystal structure of PDE6D in the apo state | | Descriptor: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, NICKEL (II) ION, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | | Authors: | Beaumont, E, Williams, D. | | Deposit date: | 2021-07-29 | | Release date: | 2022-06-08 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Validation of a small molecule inhibitor of PDE6D-RAS interaction with favorable anti-leukemic effects.
Blood Cancer J, 12, 2022
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5E8F
 | | Structure of Fully modified geranylgeranylated PDE6C Peptide in complex with PDE6D | | Descriptor: | Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha', GERAN-8-YL GERAN, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | | Authors: | Fansa, E.K, O'Reilly, N.J, Ismail, S.A, Wittinghofer, A. | | Deposit date: | 2015-10-14 | | Release date: | 2015-11-18 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | The N- and C-terminal ends of RPGR can bind to PDE6 delta.
Embo Rep., 16, 2015
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3T5I
 | | Structure of Fully modified farnesylated Rheb Peptide in complex with PDE6D | | Descriptor: | C-terminal Farnesylated Rheb peptide CSQQGKSS(CMT), FARNESYL, Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | | Authors: | Ismail, S.A, Chen, Y.-X, Wittinghofer, A. | | Deposit date: | 2011-07-27 | | Release date: | 2011-11-02 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Arl2-GTP and Arl3-GTP regulate a GDI-like transport system for farnesylated cargo.
Nat.Chem.Biol., 7, 2011
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5NAL
 | | The crystal structure of inhibitor-15 covalently bound to PDE6D | | Descriptor: | Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta, ~{N}4-[(4-chlorophenyl)methyl]-~{N}1-(cyclohexylmethyl)-~{N}4-cyclopentyl-~{N}1-[(~{Z})-4-[(~{E})-methyliminomethyl]-5-oxidanyl-hex-4-enyl]benzene-1,4-disulfonamide | | Authors: | Fansa, E.K, Martin-Gago, P, Waldmann, H, Wittinghofer, A. | | Deposit date: | 2017-02-28 | | Release date: | 2017-05-10 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Covalent Protein Labeling at Glutamic Acids.
Cell Chem Biol, 24, 2017
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7Q9U
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