1W6K
 
 | | Structure of human OSC in complex with Lanosterol | | Descriptor: | LANOSTEROL, LANOSTEROL SYNTHASE, octyl beta-D-glucopyranoside | | Authors: | Thoma, R, Schulz-Gasch, T, D'Arcy, B, Benz, J, Aebi, J, Dehmlow, H, Hennig, M, Ruf, A. | | Deposit date: | 2004-08-19 | | Release date: | 2004-10-29 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Insight Into Steroid Scaffold Formation from the Structure of Human Oxidosqualene Cyclase
Nature, 432, 2004
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1W6J
 | | Structure of human OSC in complex with Ro 48-8071 | | Descriptor: | LANOSTEROL SYNTHASE, TETRADECANE, [4-({6-[ALLYL(METHYL)AMINO]HEXYL}OXY)-2-FLUOROPHENYL](4-BROMOPHENYL)METHANONE, ... | | Authors: | Thoma, R, Schulz-Gasch, T, D'Arcy, B, Benz, J, Aebi, J, Dehmlow, H, Hennig, M, Ruf, A. | | Deposit date: | 2004-08-18 | | Release date: | 2004-10-29 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Insight Into Steroid Scaffold Formation from the Structure of Human Oxidosqualene Cyclase
Nature, 432, 2004
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6O60
 | | Crystal structure of GGTase3-FBXL2-SKP1 complex | | Descriptor: | F-box/LRR-repeat protein 2, Geranylgeranyl transferase type-2 subunit beta, Protein prenyltransferase alpha subunit repeat-containing protein 1, ... | | Authors: | Wang, H, Zheng, N. | | Deposit date: | 2019-03-04 | | Release date: | 2019-06-26 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.503 Å) | | Cite: | GGTase3 is a newly identified geranylgeranyltransferase targeting a ubiquitin ligase.
Nat.Struct.Mol.Biol., 26, 2019
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6VPT
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3SQC
 | | SQUALENE-HOPENE CYCLASE | | Descriptor: | SQUALENE--HOPENE CYCLASE | | Authors: | Wendt, K.U, Schulz, G.E. | | Deposit date: | 1998-09-04 | | Release date: | 1999-05-18 | | Last modified: | 2024-05-22 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | The structure of the membrane protein squalene-hopene cyclase at 2.0 A resolution.
J.Mol.Biol., 286, 1999
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2BED
 | | Structure of FPT bound to inhibitor SCH207736 | | Descriptor: | (11S)-8-CHLORO-11-[1-(METHYLSULFONYL)PIPERIDIN-4-YL]-6-PIPERAZIN-1-YL-11H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDINE, FARNESYL DIPHOSPHATE, Protein farnesyltransferase beta subunit, ... | | Authors: | Strickland, C. | | Deposit date: | 2005-10-24 | | Release date: | 2006-08-08 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Enhanced FTase activity achieved via piperazine interaction with catalytic zinc.
Bioorg.Med.Chem.Lett., 16, 2006
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8RDX
 | | PGGtase I in complex with probe BAY-6092 | | Descriptor: | (5~{R})-5-(2-methoxyphenyl)-9-[(2~{R})-3,3,3-tris(fluoranyl)-2-methoxy-2-phenyl-propanoyl]-3,9-diazaspiro[5.5]undecan-2-one, CHLORIDE ION, DIPHOSPHATE, ... | | Authors: | Steuber, H. | | Deposit date: | 2023-12-08 | | Release date: | 2024-02-14 | | Last modified: | 2024-07-31 | | Method: | X-RAY DIFFRACTION (3.67 Å) | | Cite: | Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling.
Cell Chem Biol, 31, 2024
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8E9E
 | | Rat protein farnesyltransferase in complex with FPP and inhibitor 2f | | Descriptor: | (5S)-4-({1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl}methyl)-5-butyl-1-[3-(trifluoromethoxy)phenyl]piperazin-2-one, 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ... | | Authors: | Wang, Y, Shi, Y, Beese, L.S. | | Deposit date: | 2022-08-26 | | Release date: | 2022-10-26 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.844 Å) | | Cite: | Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyltransferase.
J.Med.Chem., 65, 2022
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8T70
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8PAK
 | | Crystal Structure of a Squalene-Hopene Cyclase from Cystobacter fuscus | | Descriptor: | (4S)-2-METHYL-2,4-PENTANEDIOL, 1,2-ETHANEDIOL, 1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE, ... | | Authors: | Worthy, H.L, Mitchell, D.E, Isupov, M.N, Littlechild, J.A. | | Deposit date: | 2023-06-08 | | Release date: | 2024-06-26 | | Method: | X-RAY DIFFRACTION (1.42 Å) | | Cite: | Structure of Mesophilic Squalene-Hopene Cyclases from Cystobacter fuscus and Archangium gephyra
To Be Published
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5BP8
 | | ent-Copalyl diphosphate synthase from Streptomyces platensis | | Descriptor: | 1,2-ETHANEDIOL, Ent-copalyl diphosphate synthase, SULFATE ION | | Authors: | Osipiuk, J, Hatzos-Skintges, C, Endres, M, Babnigg, G, Rudolf, J.D, Ma, M, Chang, C.-Y, Shen, B, Joachimiak, A, Enzyme Discovery for Natural Product Biosynthesis (NatPro), Midwest Center for Structural Genomics (MCSG) | | Deposit date: | 2015-05-27 | | Release date: | 2015-06-10 | | Last modified: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structure of the ent-Copalyl Diphosphate Synthase PtmT2 from Streptomyces platensis CB00739, a Bacterial Type II Diterpene Synthase.
J.Am.Chem.Soc., 138, 2016
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3KSL
 | | Structure of FPT bound to DATFP-DH-GPP | | Descriptor: | (2S,6E)-8-{[(R)-hydroxy(phosphonooxy)phosphoryl]oxy}-2,6-dimethyloct-6-en-1-yl (2S)-3,3,3-trifluoro-2-hydrazinopropanoate, Farnesyltransferase, CAAX box, ... | | Authors: | Hovlid, M.L, Edelstein, R.L, Henry, O, Ochocki, J, DeGraw, A, Lenevich, S, Talbot, T, Young, V, Hruza, A.W, Lopez-Gallego, F, Labello, N.P, Strickland, C.L, Schmidt-Dannert, C, Distefano, M.D. | | Deposit date: | 2009-11-23 | | Release date: | 2009-12-22 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Synthesis, properties, and applications of diazotrifluropropanoyl-containing photoactive analogs of farnesyl diphosphate containing modified linkages for enhanced stability.
Chem.Biol.Drug Des., 75, 2010
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2ZIS
 | | Crystal Structure of rat protein farnesyltransferase complexed with a bezoruran inhibitor and FPP | | Descriptor: | 3-{2-[(S)-(4-cyanophenyl)(hydroxy)(1-methyl-1H-imidazol-5-yl)methyl]-5-nitro-1-benzofuran-7-yl}benzonitrile, ACETIC ACID, FARNESYL DIPHOSPHATE, ... | | Authors: | Fukami, T.A, Sogabe, S, Nagata, Y, Kondoh, O, Ishii, N. | | Deposit date: | 2008-02-22 | | Release date: | 2009-02-24 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors
Bioorg.Med.Chem.Lett., 19, 2009
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2SQC
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2ZIR
 | | Crystal Structure of rat protein farnesyltransferase complexed with a benzofuran inhibitor and FPP | | Descriptor: | 2-[(S)-(4-chlorophenyl)(hydroxy)(1-methyl-1H-imidazol-5-yl)methyl]-N-morpholin-4-yl-7-phenyl-1-benzofuran-5-carboxamide, FARNESYL DIPHOSPHATE, GLYCEROL, ... | | Authors: | Fukami, T.A, Sogabe, S, Nagata, Y, Kondoh, O, Ishii, N. | | Deposit date: | 2008-02-22 | | Release date: | 2009-02-24 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors
Bioorg.Med.Chem.Lett., 19, 2009
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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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2R2L
 | | Structure of Farnesyl Protein Transferase bound to PB-93 | | Descriptor: | FARNESYL DIPHOSPHATE, Farnesyltransferase subunit alpha, Farnesyltransferase subunit beta, ... | | Authors: | Strickland, C.O, Voorhis, W. | | Deposit date: | 2007-08-27 | | Release date: | 2008-03-11 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.23 Å) | | Cite: | Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase.
Antimicrob.Agents Chemother., 51, 2007
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3KSQ
 | | Discovery of C-Imidazole Azaheptapyridine FPT Inhibitors | | Descriptor: | FARNESYL DIPHOSPHATE, Farnesyltransferase, CAAX box, ... | | Authors: | Zhu, H.Y, Cooper, A.B, Njoroge, G, Kirschmeier, P, Strickland, C, Hruza, A, Girijavallabhan, V.M. | | Deposit date: | 2009-11-23 | | Release date: | 2010-01-26 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Discovery of C-imidazole azaheptapyridine FPT inhibitors.
Bioorg.Med.Chem.Lett., 20, 2010
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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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1X81
 | | Farnesyl transferase structure of Jansen compound | | Descriptor: | 6-[(S)-AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-4-(3-CHLOROPHENYL)-1-METHYLQUINOLIN-2(1H)-ONE, Protein farnesyltransferase beta subunit, Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit, ... | | Authors: | Li, Q, Claiborne, A, Li, T, Hasvold, L, Stoll, V.S, Muchmore, S, Jakob, C.G, Gu, W, Cohen, J, Hutchins, C, Frost, D, Rosenberg, S.H, Sham, H.L. | | Deposit date: | 2004-08-16 | | Release date: | 2004-12-21 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.
Bioorg.Med.Chem.Lett., 14, 2004
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3PZ4
 | | Crystal structure of FTase(ALPHA-subunit; BETA-subunit DELTA C10) in complex with BMS3 and lipid substrate FPP | | Descriptor: | (3R)-3-benzyl-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-carbonitrile, FARNESYL DIPHOSPHATE, Protein farnesyltransferase subunit beta, ... | | Authors: | Guo, Z, Bon, R.S, Stigter, E.A, Waldmann, H, Alexandrov, K, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2010-12-14 | | Release date: | 2011-05-11 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structure-Guided Development of Selective RabGGTase Inhibitors.
Angew.Chem.Int.Ed.Engl., 50, 2011
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3PZ3
 | | Crystal structure of RabGGTase(DELTA LRR; DELTA IG) in Complex with BMS-analogue 14 | | Descriptor: | 4-({(3R)-7-(5-formylfuran-2-yl)-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-3-yl}methyl)phenyl benzylcarbamate, CALCIUM ION, Geranylgeranyl transferase type-2 subunit alpha, ... | | Authors: | Guo, Z, Bon, R.S, Stigter, E.A, Waldmann, H, Alexandrov, K, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2010-12-14 | | Release date: | 2011-05-11 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structure-Guided Development of Selective RabGGTase Inhibitors.
Angew.Chem.Int.Ed.Engl., 50, 2011
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3PZ2
 | | Crystal structure of RabGGTase(DELTA LRR; DELTA IG) in Complex with BMS3 and lipid substrate GGPP | | Descriptor: | (3R)-3-benzyl-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-carbonitrile, CALCIUM ION, GERANYLGERANYL DIPHOSPHATE, ... | | Authors: | Guo, Z, Bon, R.S, Stigter, E.A, Waldmann, H, Alexandrov, K, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2010-12-14 | | Release date: | 2011-05-11 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | Structure-Guided Development of Selective RabGGTase Inhibitors.
Angew.Chem.Int.Ed.Engl., 50, 2011
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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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3PZ1
 | | Crystal structure of RabGGTase(DELTA LRR; DELTA IG) in Complex with BMS3 | | Descriptor: | (3R)-3-benzyl-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-carbonitrile, CALCIUM ION, DIMETHYL SULFOXIDE, ... | | Authors: | Guo, Z, Bon, R.S, Stigter, E.A, Waldmann, H, Alexandrov, K, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2010-12-14 | | Release date: | 2011-05-11 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Structure-Guided Development of Selective RabGGTase Inhibitors.
Angew.Chem.Int.Ed.Engl., 50, 2011
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