1FPP
 
 | | PROTEIN FARNESYLTRANSFERASE COMPLEX WITH FARNESYL DIPHOSPHATE | | Descriptor: | FARNESYL DIPHOSPHATE, PHOSPHATE ION, PROTEIN FARNESYLTRANSFERASE, ... | | Authors: | Dunten, P, Kammlott, U, Crowther, R, Weber, D, Palermo, R, Birktoft, J. | | Deposit date: | 1998-07-10 | | Release date: | 1999-06-08 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | Protein farnesyltransferase: structure and implications for substrate binding.
Biochemistry, 37, 1998
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1FT2
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1FT1
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1H37
 | | Structures of Human Oxidosqualene Cyclase Inhibitors Bound to an Homologous Enzyme | | Descriptor: | (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, SQUALENE--HOPENE CYCLASE, {4-[((1S,2S)-2-{[ALLYL(CYCLOPROPYL)AMINO]METHYL}CYCLOPROPYL)METHOXY]PHENYL}(4-BROMOPHENYL)METHANONE | | Authors: | Lenhart, A, Reinert, D.J, Weihofen, W.A, Aebi, J.D, Dehmlow, H, Morand, O.H, Schulz, G.E. | | Deposit date: | 2002-08-24 | | Release date: | 2003-08-21 | | Last modified: | 2024-05-08 | | 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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1H36
 | | Structures of Human Oxidosqualene Cyclase Inhibitors Bound to an Homologous Enzyme | | Descriptor: | (4-BROMOPHENYL)[4-({(2E)-4-[CYCLOPROPYL(METHYL)AMINO]BUT-2-ENYL}OXY)PHENYL]METHANONE, (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, 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: | 2002-08-24 | | Release date: | 2003-08-21 | | Last modified: | 2024-05-08 | | 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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1H35
 | | Structures of Human Oxidosqualene Cyclase Inhibitors Bound to an Homologous Enzyme | | Descriptor: | (4'-{[ALLYL(METHYL)AMINO]METHYL}-1,1'-BIPHENYL-4-YL)(4-BROMOPHENYL)METHANONE, (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, 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: | 2002-08-24 | | Release date: | 2003-08-21 | | Last modified: | 2024-05-08 | | 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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1H3B
 | | Squalene-Hopene Cyclase | | Descriptor: | (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, N-{6-[4-(6-BROMO-1,2-BENZISOTHIAZOL-3-YL)PHENOXY]HEXYL}-N-METHYL-2-PROPEN-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: | 2002-08-25 | | Release date: | 2003-08-21 | | Last modified: | 2024-05-08 | | 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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1H3A
 | | Structures of Human Oxidosqualene Cyclase Inhibitors Bound to an Homologous Enzyme | | Descriptor: | (2E)-N-ALLYL-4-{[3-(4-BROMOPHENYL)-5-FLUORO-1-METHYL-1H-INDAZOL-6-YL]OXY}-N-METHYL-2-BUTEN-1-AMINE, (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, 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: | 2002-08-24 | | Release date: | 2003-08-21 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.85 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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1H39
 | | Structures of Human Oxidosqualene Cyclase Inhibitors Bound to an Homologous Enzyme | | Descriptor: | (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, ALLYL-{6-[3-(4-BROMO-PHENYL)-1-METHYL-1H-INDAZOL-6-YL]OXY}HEXYL)-N-METHYLAMINE, 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: | 2002-08-24 | | Release date: | 2003-08-21 | | Last modified: | 2024-05-08 | | 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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1GSZ
 | | Crystal Structure of a Squalene Cyclase in Complex with the Potential Anticholesteremic Drug Ro48-8071 | | Descriptor: | (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, SQUALENE--HOPENE CYCLASE, [4-({6-[ALLYL(METHYL)AMINO]HEXYL}OXY)-2-FLUOROPHENYL](4-BROMOPHENYL)METHANONE | | Authors: | Lenhart, A, Weihofen, W.A, Pleschke, A.E.W, Schulz, G.E. | | Deposit date: | 2002-01-09 | | Release date: | 2003-01-16 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Crystal Structure of a Squalene Cyclase in Complex with the Potential Anticholesteremic Drug Ro48-8071
Chem.Biol., 9, 2002
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1H3C
 | | Structures of Human Oxidosqualene Cyclase Inhibitors Bound to an Homologous Enzyme | | Descriptor: | (HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE, N-(6-{[3-(4-BROMOPHENYL)-1,2-BENZISOTHIAZOL-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: | 2002-08-25 | | Release date: | 2003-08-21 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.9 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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3E37
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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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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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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: | 2024-05-08 | | 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: | 2024-05-08 | | 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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3DSW
 | | Crystal structure of RabGGTase(DELTA LRR; DELTA IG)in complex with mono-prenylated peptide Ser-Cys(GG)-Ser-Cys derivated from Rab7 | | Descriptor: | CALCIUM ION, GERAN-8-YL GERAN, Geranylgeranyl transferase type-2 subunit alpha, ... | | Authors: | Guo, Z, Yu, S, Goody, R.S, Alexandrov, K, Blankenfeldt, W. | | Deposit date: | 2008-07-14 | | Release date: | 2008-09-09 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Structures of RabGGTase-substrate/product complexes provide insights into the evolution of protein prenylation
Embo J., 27, 2008
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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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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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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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