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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3DPY
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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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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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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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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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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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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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1SA5
 | | Rat protein farnesyltransferase complexed with FPP and BMS-214662 | | Descriptor: | 3-BENZYL-1-(1H-IMIDAZOL-4-YLMETHYL)-4-(THIEN-2-YLSULFONYL)-2,3,4,5-TETRAHYDRO-1H-1,4-BENZODIAZEPINE-7-CARBONITRILE, ACETIC ACID, FARNESYL DIPHOSPHATE, ... | | 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 (2.6 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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8E9E
 | | Rat protein farnesyltransferase in complex with FPP and inhibitor 2f | | Descriptor: | (5S)-4-({1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl}methyl)-5-butyl-1-[3-(trifluoromethoxy)phenyl]piperazin-2-one, 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ... | | Authors: | Wang, Y, Shi, Y, Beese, L.S. | | Deposit date: | 2022-08-26 | | Release date: | 2022-10-26 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.844 Å) | | Cite: | Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyltransferase.
J.Med.Chem., 65, 2022
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1KZP
 | | PROTEIN FARNESYLTRANSFERASE COMPLEXED WITH A FARNESYLATED K-RAS4B PEPTIDE PRODUCT | | Descriptor: | ACETIC ACID, FARNESYL, Farnesylated K-Ras4B peptide product, ... | | Authors: | Long, S.B, Casey, P.J, Beese, L.S. | | Deposit date: | 2002-02-07 | | Release date: | 2002-10-16 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Reaction path of protein farnesyltransferase at atomic resolution
Nature, 419, 2002
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1KZO
 | | PROTEIN FARNESYLTRANSFERASE COMPLEXED WITH FARNESYLATED K-RAS4B PEPTIDE PRODUCT AND FARNESYL DIPHOSPHATE SUBSTRATE BOUND SIMULTANEOUSLY | | Descriptor: | ACETIC ACID, FARNESYL, FARNESYL DIPHOSPHATE, ... | | Authors: | Long, S.B, Casey, P.J, Beese, L.S. | | Deposit date: | 2002-02-07 | | Release date: | 2002-10-16 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | The Reaction Path of Protein Farnesyltransferase at Atomic Resolution
Nature, 419, 2002
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1S64
 | | Rat protein geranylgeranyltransferase type-I complexed with L-778,123 and a sulfate anion | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]METHYL}-1H-IMIDAZOL-1-YL)METHYL]BENZONITRILE, CHLORIDE ION, ... | | Authors: | Reid, T.S, Long, S.B, Beese, L.S. | | Deposit date: | 2004-01-22 | | Release date: | 2004-07-27 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Crystallographic Analysis Reveals that Anticancer Clinical Candidate L-778,123 Inhibits Protein Farnesyltransferase and Geranylgeranyltransferase-I by Different Binding Modes.
Biochemistry, 43, 2004
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1O1R
 | | Structure of FPT bound to GGPP | | Descriptor: | GERANYLGERANYL DIPHOSPHATE, Protein farnesyltransferase alpha subunit, Protein farnesyltransferase beta subunit, ... | | Authors: | Turek-Etienne, T.C, Strickland, C.L, Distefano, M.D. | | Deposit date: | 2003-01-14 | | Release date: | 2003-05-06 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Biochemical and Structural Studies with Prenyl Diphosphate Analogues Provide Insights
into Isoprenoid Recognition by Protein Farnesyl Transferase
Biochemistry, 42, 2003
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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: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structure of mammalian protein geranylgeranyltransferase type-I
EMBO J., 22, 2003
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1N4P
 | | Protein Geranylgeranyltransferase type-I Complexed with Geranylgeranyl Diphosphate | | Descriptor: | CHLORIDE ION, Fusion protein consisting of transforming protein p21b and Ras related protein Rap-2b, GERAN-8-YL GERAN, ... | | 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: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.65 Å) | | Cite: | Structure of mammalian protein geranylgeranyltransferase type-I
EMBO J., 22, 2003
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1N4Q
 | | Protein Geranylgeranyltransferase type-I Complexed with a GGPP Analog and a KKKSKTKCVIL Peptide | | Descriptor: | 2-[METHYL-(5-GERANYL-4-METHYL-PENT-3-ENYL)-AMINO]-ETHYL-DIPHOSPHATE, 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: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Structure of mammalian protein geranylgeranyltransferase type-I
EMBO J., 22, 2003
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1N4S
 | | Protein Geranylgeranyltransferase type-I Complexed with GGPP and a Geranylgeranylated KKKSKTKCVIL Peptide Product | | Descriptor: | CHLORIDE ION, Fusion protein consisting of transforming protein p21b and Ras related protein Rap-2b, GERAN-8-YL GERAN, ... | | 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: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure of mammalian protein geranylgeranyltransferase type-I
EMBO J., 22, 2003
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1O1T
 | | Structure of FPT bound to the CVIM-FPP product | | Descriptor: | MAGNESIUM ION, N-ACETYL-S-[(2E,6E)-3,7,11-TRIMETHYLDODECA-2,6,10-TRIENYL]-L-CYSTEINYL-D-VALYL-L-ISOLEUCYL-L-METHIONINE, Protein farnesyltransferase alpha subunit, ... | | Authors: | Turek-Etienne, T.C, Strickland, C.L, Distefano, M.D. | | Deposit date: | 2003-01-14 | | Release date: | 2003-05-06 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Biochemical and Structural Studies with Prenyl Diphosphate Analogues Provide Insights into
Isoprenoid Recognition by Protein Farnesyl Transferase
Biochemistry, 42, 2003
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1O5M
 | | Structure of FPT bound to the inhibitor SCH66336 | | Descriptor: | 4-{2-[4-(3,10-DIBROMO-8-CHLORO-6,11-DIHYDRO-5H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDIN-11-YL)PIPERIDIN-1-YL]-2-OXOETHYL}PIPERIDINE-1-CARBOXAMIDE, FARNESYL DIPHOSPHATE, Protein farnesyltransferase alpha subunit, ... | | Authors: | Strickland, C.L, Weber, P.C, Ganguly, A.K. | | Deposit date: | 2003-09-26 | | Release date: | 2003-10-21 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Tricyclic Farnesyl Protein Transferase Inhibitors: Crystallographic and Calorimetric Studies of Structure-Activity Relationships
J.Med.Chem., 42, 1999
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1O1S
 | | Structure of FPT bound to isoprenoid analog 3b | | Descriptor: | (2E,6E)-8-[(3-BENZOYLBENZYL)OXY]-3,7-DIMETHYLOCTA-2,6-DIENYL TRIHYDROGEN DIPHOSPHATE, Protein farnesyltransferase alpha subunit, Protein farnesyltransferase beta subunit, ... | | Authors: | Turek-Etienne, T.C, Strickland, C.L, Distefano, M.D. | | Deposit date: | 2003-01-14 | | Release date: | 2003-05-06 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Biochemical and Structural Studies with Prenyl Diphosphate Analogues Provide Insights into
Isoprenoid Recognition by Protein Farnesyl Transferase
Biochemistry, 42, 2003
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1TN7
 | | Protein Farnesyltransferase Complexed with a TC21 Peptide Substrate and a FPP Analog at 2.3A Resolution | | Descriptor: | ACETIC ACID, Fusion protein, Protein farnesyltransferase alpha subunit, ... | | Authors: | Reid, T.S, Terry, K.L, Casey, P.J, Beese, L.S. | | Deposit date: | 2004-06-11 | | Release date: | 2004-11-02 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Crystallographic analysis of CaaX prenyltransferases complexed with substrates defines rules of protein substrate selectivity.
J.Mol.Biol., 343, 2004
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1TNU
 | | Rat Protein Geranylgeranyltransferase Type-I Complexed with a GGPP analog and a GCINCCKVL Peptide Derived from RhoB | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 2-[METHYL-(5-GERANYL-4-METHYL-PENT-3-ENYL)-AMINO]-ETHYL-DIPHOSPHATE, CHLORIDE ION, ... | | Authors: | Reid, T.S, Terry, K.L, Casey, P.J, Beese, L.S. | | Deposit date: | 2004-06-11 | | Release date: | 2004-11-02 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Crystallographic analysis of CaaX prenyltransferases complexed with substrates defines rules of protein substrate selectivity.
J.Mol.Biol., 343, 2004
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1TNB
 | | Rat Protein Geranylgeranyltransferase Type-I Complexed with a GGPP analog and a substrate KKSKTKCVIF Peptide Derived from TC21 | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 2-[METHYL-(5-GERANYL-4-METHYL-PENT-3-ENYL)-AMINO]-ETHYL-DIPHOSPHATE, CHLORIDE ION, ... | | Authors: | Reid, T.S, Terry, K.L, Casey, P.J, Beese, L.S. | | Deposit date: | 2004-06-11 | | Release date: | 2004-11-02 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.85 Å) | | Cite: | Crystallographic analysis of CaaX prenyltransferases complexed with substrates defines rules of protein substrate selectivity.
J.Mol.Biol., 343, 2004
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