7MXX
 
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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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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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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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3EYZ
 | | Cocrystal structure of Bacillus fragment DNA polymerase I with duplex DNA (open form) | | Descriptor: | 5'-D(*DAP*DTP*DGP*DCP*DGP*DAP*DGP*DTP*DCP*DAP*DGP*DGP*DA)-3', 5'-D(*DCP*DCP*DTP*DGP*DAP*DCP*DTP*DCP*DGP*DC)-3', DNA polymerase I, ... | | Authors: | Warren, J.J, Wu, E.Y, Golosov, A.A, Karplus, M, Beese, L.S. | | Deposit date: | 2008-10-22 | | Release date: | 2009-11-10 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | The Mechanism of the Translocation Step in DNA Replication by DNA Polymerase I: A Computer Simulation Analysis.
Structure, 18, 2010
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3EZ5
 | | Cocrystal structure of Bacillus fragment DNA polymerase I with duplex DNA , dCTP, and zinc (closed form). | | Descriptor: | 2',3'-DIDEOXYADENOSINE-5'-TRIPHOSPHATE, 5'-D(*DAP*DTP*DTP*DCP*DGP*DAP*DGP*DTP*DCP*DAP*DGP*DG)-3', 5'-D(*DCP*DCP*DTP*DGP*DAP*DCP*DTP*DCP*DG)-3', ... | | Authors: | Warren, J.J, Wu, E.Y, Golosov, A.A, Karplus, M, Beese, L.S. | | Deposit date: | 2008-10-22 | | Release date: | 2009-11-10 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | The Mechanism of the Translocation Step in DNA Replication by DNA Polymerase I: A Computer Simulation Analysis.
Structure, 18, 2010
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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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3DPY
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3DRA
 | | Candida albicans protein geranylgeranyltransferase-I complexed with GGPP | | Descriptor: | 2-[3-(2-HYDROXY-1,1-DIHYDROXYMETHYL-ETHYLAMINO)-PROPYLAMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, GERANYLGERANYL DIPHOSPHATE, Geranylgeranyltransferase type I beta subunit, ... | | Authors: | Hast, M.A, Beese, L.S. | | Deposit date: | 2008-07-10 | | Release date: | 2008-09-30 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structure of protein geranylgeranyltransferase-I from the human pathogen Candida albicans complexed with a lipid substrate.
J.Biol.Chem., 283, 2008
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1QHT
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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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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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3TAR
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3TAP
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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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2H6F
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2H6G
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2HHQ
 | | O6-methyl-guanine:T pair in the polymerase-10 basepair position | | Descriptor: | 5'-D(*CP*AP*TP*(6OG)P*CP*GP*AP*GP*TP*CP*AP*GP*G)-3', 5'-D(*GP*CP*CP*TP*GP*AP*CP*TP*CP*GP*TP*AP*TP*GP*A)-3', DNA polymerase I, ... | | Authors: | Warren, J.J, Forsberg, L.J, Beese, L.S. | | Deposit date: | 2006-06-28 | | Release date: | 2006-12-12 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | The structural basis for the mutagenicity of O6-methyl-guanine lesions.
Proc.Natl.Acad.Sci.Usa, 103, 2006
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2HHU
 | | C:O6-methyl-guanine in the polymerase postinsertion site (-1 basepair position) | | Descriptor: | 2'-DEOXYCYTIDINE-5'-TRIPHOSPHATE, 5'-D(*GP*CP*GP*AP*TP*CP*AP*GP*CP*CP*C)-3', 5'-D(*GP*TP*AP*CP*(6OG)P*GP*GP*CP*TP*GP*AP*TP*CP*GP*CP*A)-3', ... | | Authors: | Warren, J.J, Forsberg, L.J, Beese, L.S. | | Deposit date: | 2006-06-28 | | Release date: | 2006-12-12 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | The structural basis for the mutagenicity of O6-methyl-guanine lesions.
Proc.Natl.Acad.Sci.Usa, 103, 2006
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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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2IEJ
 | | Human Protein Farnesyltransferase Complexed with Inhibitor Compound STN-48 And FPP Analog at 1.8A Resolution | | Descriptor: | ACETATE ION, METHYL N-{(3S)-1-[(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-6-PHENYL-1,2,3,4-TETRAHYDROQUINOLIN-3-YL}-N-[(1-METHYL-1H-IMIDAZOL-4-YL)SULFONYL]GLYCINATE, Protein farnesyltransferase subunit beta, ... | | Authors: | Hast, M.A, Beese, L.S. | | Deposit date: | 2006-09-19 | | Release date: | 2007-01-23 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Resistance mutations at the lipid substrate binding site of Plasmodium falciparum protein farnesyltransferase.
Mol.Biochem.Parasitol., 152, 2007
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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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2HHT
 | | C:O6-methyl-guanine pair in the polymerase-2 basepair position | | Descriptor: | 5'-D(*GP*CP*GP*AP*TP*CP*AP*GP*CP*TP*CP*G)-3', 5'-D(*GP*TP*AP*CP*(6OG)P*AP*GP*CP*TP*GP*AP*TP*CP*GP*CP*A)-3', DNA polymerase I, ... | | Authors: | Warren, J.J, Forsberg, L.J, Beese, L.S. | | Deposit date: | 2006-06-28 | | Release date: | 2006-12-12 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | The structural basis for the mutagenicity of O6-methyl-guanine lesions.
Proc.Natl.Acad.Sci.Usa, 103, 2006
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2HHW
 | | ddTTP:O6-methyl-guanine pair in the polymerase active site, in the closed conformation | | Descriptor: | 2',3'-DIDEOXY-THYMIDINE-5'-TRIPHOSPHATE, 5'-D(*CP*AP*TP*(6OG)P*CP*GP*AP*GP*TP*CP*AP*GP*G)-3', 5'-D(*CP*CP*TP*GP*AP*CP*TP*CP*(DDG))-3', ... | | Authors: | Warren, J.J, Forsberg, L.J, Beese, L.S. | | Deposit date: | 2006-06-28 | | Release date: | 2006-12-12 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.88 Å) | | Cite: | The structural basis for the mutagenicity of O6-methyl-guanine lesions.
Proc.Natl.Acad.Sci.Usa, 103, 2006
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