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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1D8E
 | | Zinc-depleted FTase complexed with K-RAS4B peptide substrate and FPP analog. | | Descriptor: | ACETATE ION, FARNESYLTRANSFERASE (ALPHA SUBUNIT), FARNESYLTRANSFERASE (BETA SUBUNIT), ... | | Authors: | Long, S.B, Casey, P.J, Beese, L.S. | | Deposit date: | 1999-10-22 | | Release date: | 2000-03-20 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (3 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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1DCE
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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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1FT1
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1FT2
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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: | 2019-05-08 | | 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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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: | 2018-06-13 | | 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: | 2018-06-13 | | 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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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: | 2018-06-13 | | 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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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: | 2018-06-13 | | 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: | 2018-06-13 | | 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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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: | 2018-06-13 | | 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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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: | 2018-06-13 | | 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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1JCQ
 | | CRYSTAL STRUCTURE OF HUMAN PROTEIN FARNESYLTRANSFERASE COMPLEXED WITH FARNESYL DIPHOSPHATE AND THE PEPTIDOMIMETIC INHIBITOR L-739,750 | | Descriptor: | 2(S)-{2(S)-[2(R)-AMINO-3-MERCAPTO]PROPYLAMINO-3(S)-METHYL}PENTYLOXY-3-PHENYLPROPIONYLMETHIONINE SULFONE, ACETIC ACID, FARNESYL DIPHOSPHATE, ... | | Authors: | Long, S.B, Casey, P.J, Beese, L.S. | | Deposit date: | 2001-06-11 | | Release date: | 2001-11-02 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | The crystal structure of human protein farnesyltransferase reveals the basis for inhibition by CaaX tetrapeptides and their mimetics.
Proc.Natl.Acad.Sci.USA, 98, 2001
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1JCR
 | | CRYSTAL STRUCTURE OF RAT PROTEIN FARNESYLTRANSFERASE COMPLEXED WITH THE NON-SUBSTRATE TETRAPEPTIDE INHIBITOR CVFM AND FARNESYL DIPHOSPHATE SUBSTRATE | | Descriptor: | ACETIC ACID, FARNESYL DIPHOSPHATE, PROTEIN FARNESYLTRANSFERASE, ... | | Authors: | Long, S.B, Casey, P.J, Beese, L.S. | | Deposit date: | 2001-06-11 | | Release date: | 2001-11-02 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | The crystal structure of human protein farnesyltransferase reveals the basis for inhibition by CaaX tetrapeptides and their mimetics.
Proc.Natl.Acad.Sci.USA, 98, 2001
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1JCS
 | | CRYSTAL STRUCTURE OF RAT PROTEIN FARNESYLTRANSFERASE COMPLEXED WITH THE PEPTIDE SUBSTRATE TKCVFM AND AN ANALOG OF FARNESYL DIPHOSPHATE | | Descriptor: | ACETIC ACID, PROTEIN FARNESYLTRANSFERASE, ALPHA SUBUNIT, ... | | Authors: | Long, S.B, Casey, P.J, Beese, L.S. | | Deposit date: | 2001-06-11 | | Release date: | 2001-11-02 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | The crystal structure of human protein farnesyltransferase reveals the basis for inhibition by CaaX tetrapeptides and their mimetics.
Proc.Natl.Acad.Sci.USA, 98, 2001
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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: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | The Reaction Path of Protein Farnesyltransferase at Atomic Resolution
Nature, 419, 2002
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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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1LD7
 | | Co-crystal structure of Human Farnesyltransferase with farnesyldiphosphate and inhibitor compound 66 | | Descriptor: | (20S)-19,20,22,23-TETRAHYDRO-19-OXO-5H,21H-18,20-ETHANO-12,14-ETHENO-6,10-METHENOBENZ[D]IMIDAZO[4,3-L][1,6,9,13]OXATRIA ZACYCLONOADECOSINE-9-CARBONITRILE, FARNESYL DIPHOSPHATE, ZINC ION, ... | | Authors: | Taylor, J.S, Terry, K.L, Beese, L.S. | | Deposit date: | 2002-04-08 | | Release date: | 2002-06-19 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
J.Med.Chem., 45, 2002
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1LD8
 | | Co-crystal structure of Human Farnesyltransferase with farnesyldiphosphate and inhibitor compound 49 | | Descriptor: | (20S)-19,20,21,22-TETRAHYDRO-19-OXO-5H-18,20-ETHANO-12,14-ETHENO-6,10-METHENO-18H-BENZ[D]IMIDAZO[4,3-K][1,6,9,12]OXATRI AZA-CYCLOOCTADECOSINE-9-CARBONITRILE, ACETIC ACID, FARNESYL DIPHOSPHATE, ... | | Authors: | Taylor, J.S, Terry, K.L, Beese, L.S. | | Deposit date: | 2002-04-08 | | Release date: | 2002-06-19 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | 3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
J.Med.Chem., 45, 2002
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1LTX
 | | Structure of Rab Escort Protein-1 in complex with Rab geranylgeranyl transferase and isoprenoid | | Descriptor: | AAAA, CHLORIDE ION, FARNESYL, ... | | Authors: | Pylypenko, O, Rak, A, Reents, R, Niculae, A, Thoma, N.H, Waldmann, H, Schlichting, I, Goody, R.S, Alexandrov, K. | | Deposit date: | 2002-05-21 | | Release date: | 2003-05-21 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Structure of Rab Escort Protein-1 in Complex with Rab Geranylgeranyltransferase
Mol.Cell, 11, 2003
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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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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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