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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1MZC
 | | Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a | | Descriptor: | 2-[3-(3-ETHYL-1-METHYL-2-OXO-AZEPAN-3-YL)-PHENOXY]-4-[1-AMINO-1-(1-METHYL-1H-IMIDIZOL-5-YL)-ETHYL]-BENZONITRILE, FARNESYL DIPHOSPHATE, Protein Farnesyltransferase alpha Subunit, ... | | Authors: | deSolms, S.J, Ciccarone, T.M, MacTough, S.C, Shaw, A.W, Buser, C.A, Ellis-Hutchings, M, Fernandes, C, Hamilton, K.A, Huber, H.E, Kohl, N.E, Lobell, R.B, Robinson, R.G, Tsou, N.N, Walsh, E.S, Graham, S.L, Beese, L.S, Taylor, J.S. | | Deposit date: | 2002-10-07 | | Release date: | 2003-07-08 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Dual Protein Farnesyltransferase-Geranylgeranyltransferase-I Inhibitors as Potential Cancer Chemotherapeutic Agents.
J.Med.Chem., 46, 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: | 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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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: | 2017-06-28 | | 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: | 2017-06-28 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure of mammalian protein geranylgeranyltransferase type-I
EMBO J., 22, 2003
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1N95
 | | Aryl Tetrahydrophyridine Inhbitors of Farnesyltranferase: Glycine, Phenylalanine and Histidine Derivatives | | Descriptor: | 1-[2-(4-CYANO-BENZYLAMINO)-3-(3-METHYL-3H-IMIDAZOL-4-YL)-PROPIONYL]-5-NAPHTHALEN-1-YL-1,2,3,6-TETRAHYDRO-PYRIDINE-4-CARBONITRILE, ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID, Protein farnesyltransferase alpha subunit, ... | | Authors: | Gwaltney II, S.L, O'Conner, S.J, Nelson, L.T, Sullivan, G.M, Imade, H, Wang, W, Hasvold, L, Li, Q, Cohen, J, Gu, W.Z. | | Deposit date: | 2002-11-22 | | Release date: | 2003-01-07 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
Bioorg.Med.Chem.Lett., 13, 2003
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1NI1
 | | Imidazole and cyanophenyl farnesyl transferase inhibitors | | Descriptor: | 2-CHLORO-5-(3-CHLORO-PHENYL)-6-[(4-CYANO-PHENYL)-(3-METHYL-3H-IMIDAZOL-4-YL)- METHOXYMETHYL]-NICOTINONITRILE, ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID, Protein farnesyltransferase alpha subunit, ... | | Authors: | Tong, Y, Lin, N.H, Wang, L, Hasvold, L, Wang, W, Leonard, N, Li, T, Li, Q, Cohen, J, Gu, W.Z, Zhang, H, Stoll, V, Bauch, J, Marsh, K, Rosenberg, S.H, Sham, H.L. | | Deposit date: | 2002-12-20 | | Release date: | 2004-04-06 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability.
Bioorg.Med.Chem.Lett., 13, 2003
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1NL4
 | | Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor | | Descriptor: | 4-[(3-CYANO-BENZYL)-(3-METHYL-3H-IMIDAZOL-4-YLMETHYL)-AMINO]-2-NAPHTHALEN-1-YL-BENZONITRILE, ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID, Protein farnesyltransferase alpha subunit, ... | | Authors: | Curtin, M.L, Florjancic, A.S, Cohen, J, Gu, W.-J, Frost, D.J, Muchmore, S.W, Sham, H.L. | | Deposit date: | 2003-01-06 | | Release date: | 2003-02-11 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Novel and Selective Imidazole-containing Biphenyl Inhibitors of Protein Farnesyltransferase
BIOORG.MED.CHEM.LETT., 13, 2003
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1N94
 | | Aryl Tetrahydropyridine Inhbitors of Farnesyltransferase: Glycine, Phenylalanine and Histidine Derivates | | Descriptor: | 2-{(5-{[BUTYL-(2-CYCLOHEXYL-ETHYL)-AMINO]-METHYL}-2'-METHYL-BIPHENYL-2-CARBONYL)-AMINO]-4-METHYLSULFANYL-BUTYRIC ACID, ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID, Protein farnesyltransferase alpha subunit, ... | | Authors: | Gwaltney II, S.L, O'Connor, S.J, Nelson, L.T, Sullivan, G.M, Imade, H, Wang, W, Hasvold, L, Li, Q, Cohen, J, Gu, W.Z. | | Deposit date: | 2002-11-22 | | Release date: | 2003-01-07 | | Last modified: | 2017-10-11 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
Bioorg.Med.Chem.Lett., 13, 2003
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1N9A
 | | Farnesyltransferase complex with tetrahydropyridine inhibitors | | Descriptor: | 1-{2-[3-(4-CYANO-BENZYL)-3H-IMIDAZOL-4-YL]-ACETYL}-5-NAPHTHALEN-1-YL-1,2,3,6-TETRAHYDRO-PYRIDINE-4-CARBONITRILE, ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID, Protein farnesyltransferase alpha subunit, ... | | Authors: | Gwaltney II, S.L, O'Conner, S.J, Nelson, L.T, Sullivan, G.M, Imade, H, Wang, W, Hasvold, L, Li, Q, Cohen, J, Gu, W.Z. | | Deposit date: | 2002-11-22 | | Release date: | 2003-01-07 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Bioorg.Med.Chem.Lett., 13, 2003
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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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1O6R
 | | Structures of human oxidosqualene cyclase inhibitors bound to an homologous enzyme | | Descriptor: | (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, ALLYL-{6-[3-(4-BROMO-PHENYL)-BENZOFURAN-6-YLOXY]-HEXYL-}-METHYL-AMIN, SQUALENE--HOPENE CYCLASE | | Authors: | Lenhart, A, Reinert, D.J, Weihofen, W.A, Aebi, J.D, Dehmlow, H, Morand, O.H, Schulz, G.E. | | Deposit date: | 2002-10-13 | | Release date: | 2003-10-17 | | Last modified: | 2018-06-20 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Binding Structures and Potencies of Oxidosqualene Cyclase Inhibitors with the Homologous Squalene-Hopene Cyclase
J.Med.Chem., 46, 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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1O6Q
 | | Structures of human oxidosqualene cyclase inhibitors bound to an homologous enzyme | | Descriptor: | (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, ALLYL-{4-[3-(4-BROMO-PHENYL)-BENZOFURAN-6-YLOXY]-BUT-2-ENYL}-METHYL-AMINE, SQUALENE--HOPENE CYCLASE | | Authors: | Lenhart, A, Reinert, D.J, Weihofen, W.A, Aebi, J.D, Dehmlow, H, Morand, O.H, Schulz, G.E. | | Deposit date: | 2002-10-13 | | Release date: | 2003-10-17 | | Last modified: | 2018-06-20 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Binding Structures and Potencies of Oxidosqualene Cyclase Inhibitors with the Homologous Squalene-Hopene Cyclase
J.Med.Chem., 46, 2003
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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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1O6H
 | | Squalene-Hopene Cyclase | | Descriptor: | (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, N-(6-{[1-(4-BROMOPHENYL)ISOQUINOLIN-6-YL]OXY}HEXYL)-N-METHYLPROP-2-EN-1-AMINE, SQUALENE--HOPENE CYCLASE | | Authors: | Lenhart, A, Reinert, D.J, Weihofen, W.A, Aebi, J.D, Dehmlow, H, Morand, O.H, Schulz, G.E. | | Deposit date: | 2002-10-03 | | Release date: | 2003-10-02 | | Last modified: | 2018-06-20 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Binding Structures and Potencies of Oxidosqualene Cyclase Inhibitors with the Homologous Squalene-Hopene Cyclase
J.Med.Chem., 46, 2003
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1O79
 | | Structures of human oxidosqualene cyclase inhibitors bound to an homologous enzyme | | Descriptor: | (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, METHYL-[4-(4-PIPERIDINE-1-YLMETHYL-PHENYL)-CYCLOHEXYL]-CARBAMINIC ACID-(4-CHLOROPHENYL)-ESTER, SQUALENE--HOPENE CYCLASE | | Authors: | Lenhart, A, Reinert, D.J, Weihofen, W.A, Aebi, J.D, Dehmlow, H, Morand, O.H, Schulz, G.E. | | Deposit date: | 2002-10-27 | | Release date: | 2003-10-23 | | Last modified: | 2018-06-20 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Binding Structures and Potencies of Oxidosqualene Cyclase Inhibitors with the Homologous Squalene-Hopene Cyclase
J.Med.Chem., 46, 2003
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1QBQ
 | | STRUCTURE OF RAT FARNESYL PROTEIN TRANSFERASE COMPLEXED WITH A CVIM PEPTIDE AND ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID. | | Descriptor: | ACETATE ION, ACETYL-CYS-VAL-ILE-SELENOMET-COOH PEPTIDE, ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID, ... | | Authors: | Strickland, C.L, Windsor, W.T, Syto, R, Wang, L, Bond, R, Wu, Z, Schwartz, J, Le, H.V, Beese, L.S, Weber, P.C. | | Deposit date: | 1999-04-27 | | Release date: | 1999-06-18 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Crystal structure of farnesyl protein transferase complexed with a CaaX peptide and farnesyl diphosphate analogue
Biochemistry, 37, 1998
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1S63
 | | Human protein farnesyltransferase complexed with L-778,123 and FPP | | Descriptor: | 4-[(5-{[4-(3-CHLOROPHENYL)-3-OXOPIPERAZIN-1-YL]METHYL}-1H-IMIDAZOL-1-YL)METHYL]BENZONITRILE, FARNESYL DIPHOSPHATE, Protein farnesyltransferase beta subunit, ... | | Authors: | Long, S.B, Casey, P.J, Beese, L.S. | | Deposit date: | 2004-01-22 | | Release date: | 2004-07-27 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.9 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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