2H6F
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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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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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2H6H
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1TN6
| Protein Farnesyltransferase Complexed with a Rap2a Peptide Substrate and a FPP Analog at 1.8A Resolution | Descriptor: | ACETIC ACID, Protein farnesyltransferase alpha subunit, Protein farnesyltransferase beta 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 (1.8 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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3E37
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2H6G
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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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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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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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1SA4
| human protein farnesyltransferase complexed with FPP and R115777 | Descriptor: | 6-[(S)-AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-4-(3-CHLOROPHENYL)-1-METHYLQUINOLIN-2(1H)-ONE, FARNESYL DIPHOSPHATE, Protein farnesyltransferase beta subunit, ... | 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 (2.1 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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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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2F0Y
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2H6I
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