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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
3DSU
| Crystal structure of RabGGTase(DELTA LRR; DELTA IG)in complex with farnesyl pyrophosphate | Descriptor: | CALCIUM ION, FARNESYL DIPHOSPHATE, 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 (1.9 Å) | Cite: | Structures of RabGGTase-substrate/product complexes provide insights into the evolution of protein prenylation Embo J., 27, 2008
|
|
3DSV
| Crystal structure of RabGGTase(DELTA LRR; DELTA IG)in complex with mono-prenylated peptide Ser-Cys-Ser-Cys(GG) 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 (2.1 Å) | Cite: | Structures of RabGGTase-substrate/product complexes provide insights into the evolution of protein prenylation Embo J., 27, 2008
|
|
3DST
| Crystal structure of RabGGTase(DELTA LRR; DELTA IG)in complex with geranylgeranyl pyrophosphate | Descriptor: | CALCIUM ION, GERANYLGERANYL DIPHOSPHATE, 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 (1.9 Å) | Cite: | Structures of RabGGTase-substrate/product complexes provide insights into the evolution of protein prenylation Embo J., 27, 2008
|
|
3DSX
| Crystal structure of RabGGTase(DELTA LRR; DELTA IG)in complex with di-prenylated peptide Ser-Cys(GG)-Ser-Cys(GG) 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 (2.1 Å) | Cite: | Structures of RabGGTase-substrate/product complexes provide insights into the evolution of protein prenylation Embo J., 27, 2008
|
|
3DPY
| |
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
|
|
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
|
|
3E37
| |
3HXD
| Engineered RabGGTase in complex with a peptidomimetic inhibitor (compound 9) | Descriptor: | CALCIUM ION, Geranylgeranyl transferase type-2 subunit alpha, Geranylgeranyl transferase type-2 subunit beta, ... | Authors: | Guo, Z, Alexandrov, K, Waldmann, H, Goody, R.S, Blankenfeldt, W. | Deposit date: | 2009-06-20 | Release date: | 2009-09-08 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Design, synthesis, and characterization of Peptide-based rab geranylgeranyl transferase inhibitors J.Med.Chem., 52, 2009
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|