1SA4
 
 | | human protein farnesyltransferase complexed with FPP and R115777 | | Descriptor: | 6-[(S)-AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-4-(3-CHLOROPHENYL)-1-METHYLQUINOLIN-2(1H)-ONE, FARNESYL DIPHOSPHATE, Protein farnesyltransferase beta subunit, ... | | Authors: | Reid, T.S, Beese, L.S. | | Deposit date: | 2004-02-06 | | Release date: | 2004-06-08 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Crystal Structures of the Anticancer Clinical Candidates R115777 (Tipifarnib) and BMS-214662 Complexed with Protein Farnesyltransferase Suggest a Mechanism of FTI Selectivity.
Biochemistry, 43, 2004
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2EYZ
 | | CT10-Regulated Kinase isoform II | | Descriptor: | v-crk sarcoma virus CT10 oncogene homolog isoform a | | Authors: | Kobashigawa, Y, Tanaka, S, Inagaki, F. | | Deposit date: | 2005-11-10 | | Release date: | 2006-11-10 | | Last modified: | 2024-05-29 | | Method: | SOLUTION NMR | | Cite: | Structural basis for the transforming activity of human cancer-related signaling adaptor protein CRK.
Nat.Struct.Mol.Biol., 14, 2007
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7RNI
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7RN5
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6TWO
 | | Binding domain of BoNT/A6 | | Descriptor: | Bont/A1, CHLORIDE ION | | Authors: | Davies, J.R, Britton, A, Acharya, K.R. | | Deposit date: | 2020-01-13 | | Release date: | 2020-07-22 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.35 Å) | | Cite: | High-resolution crystal structures of the botulinum neurotoxin binding domains from subtypes A5 and A6.
Febs Open Bio, 10, 2020
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6TWP
 | | Binding domain of BoNT/A5 | | Descriptor: | Botulinum neurotoxin A5, CHLORIDE ION | | Authors: | Davies, J.R, Acharya, K.R. | | Deposit date: | 2020-01-13 | | Release date: | 2020-07-22 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.15 Å) | | Cite: | High-resolution crystal structures of the botulinum neurotoxin binding domains from subtypes A5 and A6.
Febs Open Bio, 10, 2020
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2IQY
 | | Rat Phosphatidylethanolamine-Binding Protein | | Descriptor: | CALCIUM ION, CHLORIDE ION, Phosphatidylethanolamine-binding protein 1 | | Authors: | Kim, Y, Joachimiak, G, Heil, G.L, Koide, S, Joachimiak, A. | | Deposit date: | 2006-10-14 | | Release date: | 2007-09-25 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | Crystal Structure of Rat Phosphatidylethanolamine-Binding Protein
To be Published
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2IQX
 | | Rat Phosphatidylethanolamine-Binding Protein Containing the S153E Mutation in the Complex with o-Phosphorylethanolamine | | Descriptor: | PHOSPHORIC ACID MONO-(2-AMINO-ETHYL) ESTER, Phosphatidylethanolamine-binding protein 1 | | Authors: | Kim, Y, Joachimiak, G, Clark, M.C, Rosner, M, Joachimiak, A. | | Deposit date: | 2006-10-14 | | Release date: | 2007-09-25 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Rat Phosphatidylethanolamine-Binding Crystal structure of Protein Containing the S153E Mutation in the Complex with o-Phosphorylethanolamine
To be Published
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3KSQ
 | | Discovery of C-Imidazole Azaheptapyridine FPT Inhibitors | | Descriptor: | FARNESYL DIPHOSPHATE, Farnesyltransferase, CAAX box, ... | | Authors: | Zhu, H.Y, Cooper, A.B, Njoroge, G, Kirschmeier, P, Strickland, C, Hruza, A, Girijavallabhan, V.M. | | Deposit date: | 2009-11-23 | | Release date: | 2010-01-26 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Discovery of C-imidazole azaheptapyridine FPT inhibitors.
Bioorg.Med.Chem.Lett., 20, 2010
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3KSL
 | | Structure of FPT bound to DATFP-DH-GPP | | Descriptor: | (2S,6E)-8-{[(R)-hydroxy(phosphonooxy)phosphoryl]oxy}-2,6-dimethyloct-6-en-1-yl (2S)-3,3,3-trifluoro-2-hydrazinopropanoate, Farnesyltransferase, CAAX box, ... | | Authors: | Hovlid, M.L, Edelstein, R.L, Henry, O, Ochocki, J, DeGraw, A, Lenevich, S, Talbot, T, Young, V, Hruza, A.W, Lopez-Gallego, F, Labello, N.P, Strickland, C.L, Schmidt-Dannert, C, Distefano, M.D. | | Deposit date: | 2009-11-23 | | Release date: | 2009-12-22 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Synthesis, properties, and applications of diazotrifluropropanoyl-containing photoactive analogs of farnesyl diphosphate containing modified linkages for enhanced stability.
Chem.Biol.Drug Des., 75, 2010
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3PZ4
 | | Crystal structure of FTase(ALPHA-subunit; BETA-subunit DELTA C10) in complex with BMS3 and lipid substrate FPP | | Descriptor: | (3R)-3-benzyl-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-carbonitrile, FARNESYL DIPHOSPHATE, Protein farnesyltransferase subunit beta, ... | | Authors: | Guo, Z, Bon, R.S, Stigter, E.A, Waldmann, H, Alexandrov, K, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2010-12-14 | | Release date: | 2011-05-11 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structure-Guided Development of Selective RabGGTase Inhibitors.
Angew.Chem.Int.Ed.Engl., 50, 2011
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4GTM
 | | FTase in complex with BMS analogue 11 | | Descriptor: | 4-({(3R)-7-cyano-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-3-yl}methyl)phenyl hexylcarbamate, DIMETHYL SULFOXIDE, FARNESYL DIPHOSPHATE, ... | | Authors: | Guo, Z, Stigter, E.A, Bon, R.S, Waldmann, H, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2012-08-28 | | Release date: | 2012-10-24 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Development of Selective, Potent RabGGTase Inhibitors
J.Med.Chem., 55, 2012
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4GTO
 | | FTase in complex with BMS analogue 14 | | Descriptor: | 4-({(3R)-7-cyano-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-3-yl}methyl)phenyl trifluoromethanesulfonate, DIMETHYL SULFOXIDE, FARNESYL DIPHOSPHATE, ... | | Authors: | Guo, Z, Stigter, E.A, Bon, R.S, Waldmann, H, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2012-08-29 | | Release date: | 2012-10-24 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Development of Selective, Potent RabGGTase Inhibitors
J.Med.Chem., 55, 2012
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4GTR
 | | FTase in complex with BMS analogue 13 | | Descriptor: | 4-({(3R)-7-cyano-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-3-yl}methyl)phenyl diethylcarbamate, DIMETHYL SULFOXIDE, FARNESYL DIPHOSPHATE, ... | | Authors: | Guo, Z, Stigter, E.A, Bon, R.S, Waldmann, H, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2012-08-29 | | Release date: | 2012-10-24 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Development of Selective, Potent RabGGTase Inhibitors
J.Med.Chem., 55, 2012
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4GTP
 | | FTase in complex with BMS analogue 16 | | Descriptor: | 5-{(3R)-3-(4-hydroxybenzyl)-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-7-yl}furan-2-carbaldehyde, DIMETHYL SULFOXIDE, FARNESYL DIPHOSPHATE, ... | | Authors: | Guo, Z, Stigter, E.A, Bon, R.S, Waldmann, H, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2012-08-29 | | Release date: | 2012-10-24 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | Development of Selective, Potent RabGGTase Inhibitors
J.Med.Chem., 55, 2012
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4GTQ
 | | FTase in complex with BMS analogue 12 | | Descriptor: | 4-({(3R)-7-cyano-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-3-yl}methyl)phenyl benzylcarbamate, FARNESYL DIPHOSPHATE, Protein farnesyltransferase subunit beta, ... | | Authors: | Guo, Z, Stigter, E.A, Bon, R.S, Waldmann, H, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2012-08-29 | | Release date: | 2012-10-24 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Development of Selective, Potent RabGGTase Inhibitors
J.Med.Chem., 55, 2012
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3E33
 | | Protein farnesyltransferase complexed with FPP and ethylenediamine scaffold inhibitor 7 | | Descriptor: | FARNESYL DIPHOSPHATE, N-benzyl-N-(2-{(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino}ethyl)-2-methylbenzenesulfonamide, Protein farnesyltransferase subunit beta, ... | | Authors: | Hast, M.A, Beese, L.S. | | Deposit date: | 2008-08-06 | | Release date: | 2009-03-10 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase.
Chem.Biol., 16, 2009
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3E32
 | | Protein farnesyltransferase complexed with FPP and ethylenediamine scaffold inhibitor 2 | | Descriptor: | FARNESYL DIPHOSPHATE, N-benzyl-N-(2-{(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino}ethyl)-1-methyl-1H-imidazole-4-sulfonamide, Protein farnesyltransferase subunit beta, ... | | Authors: | Hast, M.A, Beese, L.S. | | Deposit date: | 2008-08-06 | | Release date: | 2009-03-10 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase.
Chem.Biol., 16, 2009
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3E34
 | | Protein farnesyltransferase complexed with FPP and ethylenediamine-scaffold inhibitor 10 | | Descriptor: | 3-{2'-[{[1-(tert-butoxycarbonyl)piperidin-4-yl]methyl}(2-{(4-cyanophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino}ethyl)sulfamoyl]biphenyl-3-yl}propanoic acid, FARNESYL DIPHOSPHATE, Protein farnesyltransferase subunit beta, ... | | Authors: | Hast, M.A, Beese, L.S. | | Deposit date: | 2008-08-06 | | Release date: | 2009-03-10 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase.
Chem.Biol., 16, 2009
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3EUV
 | | Crystal structure of FTase(ALPHA-subunit; BETA-subunit DELTA C10, W102T, Y154T) in complex with BiotinGPP | | Descriptor: | (2E,6E)-3,7-dimethyl-8-({5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl}amino)octa-2,6-dien-1-yl trihydrogen diphosphate, Protein farnesyltransferase subunit beta, Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha, ... | | Authors: | Guo, Z, Nguyen, U.T.T, Delon, C, Bon, R.S, Blankenfeldt, W, Goody, R.S, Waldmann, H, Wolters, D, Alexandrov, K. | | Deposit date: | 2008-10-11 | | Release date: | 2009-07-07 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | Analysis of the eukaryotic prenylome by isoprenoid affinity tagging
Nat.Chem.Biol., 5, 2009
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3DPY
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3E30
 | | Protein farnesyltransferase complexed with FPP and ethylene diamine inhibitor 4 | | Descriptor: | FARNESYL DIPHOSPHATE, Protein farnesyltransferase subunit beta, Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha, ... | | Authors: | Hast, M.A, Beese, L.S. | | Deposit date: | 2008-08-06 | | Release date: | 2009-03-10 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase.
Chem.Biol., 16, 2009
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3EU5
 | | Crystal structure of FTase(ALPHA-subunit; BETA-subunit DELTA C10) in complex with BiotinGPP | | Descriptor: | (2E,6E)-3,7-dimethyl-8-({5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl}amino)octa-2,6-dien-1-yl trihydrogen diphosphate, Protein farnesyltransferase subunit beta, Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha, ... | | Authors: | Guo, Z, Nguyen, U.T.T, Delon, C, Bon, R.S, Blankenfeldt, W, Goody, R.S, Waldmann, H, Wolters, D, Alexandrov, K. | | Deposit date: | 2008-10-09 | | Release date: | 2009-07-07 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Analysis of the eukaryotic prenylome by isoprenoid affinity tagging
Nat.Chem.Biol., 5, 2009
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1D8D
 | | CO-CRYSTAL STRUCTURE OF RAT PROTEIN FARNESYLTRANSFERASE COMPLEXED WITH A K-RAS4B PEPTIDE SUBSTRATE AND FPP ANALOG AT 2.0A RESOLUTION | | Descriptor: | ACETATE ION, K-RAS4B PEPTIDE SUBSTRATE, ZINC ION, ... | | Authors: | Long, S.B, Casey, P.J, Beese, L.S. | | Deposit date: | 1999-10-22 | | Release date: | 2000-02-09 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | The basis for K-Ras4B binding specificity to protein farnesyltransferase revealed by 2 A resolution ternary complex structures.
Structure Fold.Des., 8, 2000
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1N4R
 | | Protein Geranylgeranyltransferase type-I Complexed with a Geranylgeranylated KKKSKTKCVIL Peptide Product | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, Fusion protein consisting of transforming protein p21b and Ras related protein Rap-2b, ... | | Authors: | Taylor, J.S, Reid, T.S, Casey, P.J, Beese, L.S. | | Deposit date: | 2002-11-01 | | Release date: | 2003-11-18 | | Last modified: | 2017-06-28 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structure of mammalian protein geranylgeranyltransferase type-I
EMBO J., 22, 2003
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