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: | 2024-04-10 | | 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, 2024
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8T70
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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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7T0B
 | | Cryptococcus neoformans protein farnesyltransferase in complex with FPP and inhibitor 2g | | Descriptor: | (2R)-3-(cyclohexylamino)-2-hydroxypropane-1-sulfonic acid, (5S)-5-butyl-4-({1-[(4-fluorophenyl)methyl]-1H-imidazol-5-yl}methyl)-1-[3-(trifluoromethoxy)phenyl]piperazin-2-one, 1,2-ETHANEDIOL, ... | | Authors: | Wang, Y, Shi, Y, Beese, L.S. | | Deposit date: | 2021-11-29 | | Release date: | 2022-11-09 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.026 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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7T0E
 | | Cryptococcus neoformans protein farnesyltransferase in complex with FPP and inhibitor 2b | | Descriptor: | (2R)-3-(cyclohexylamino)-2-hydroxypropane-1-sulfonic acid, (5S)-4-({1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl}methyl)-5-butyl-1-(3-chlorophenyl)piperazin-2-one, 1,2-ETHANEDIOL, ... | | Authors: | Wang, Y, Shi, Y, Beese, L.S. | | Deposit date: | 2021-11-29 | | Release date: | 2022-11-09 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.223 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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7T09
 | | Cryptococcus neoformans protein farnesyltransferase in complex with FPP and inhibitor 2d | | Descriptor: | (2R)-3-(cyclohexylamino)-2-hydroxypropane-1-sulfonic acid, 1,2-ETHANEDIOL, 4-{[5-({(2S)-2-butyl-5-oxo-4-[3-(trifluoromethoxy)phenyl]piperazin-1-yl}methyl)-1H-imidazol-1-yl]methyl}benzonitrile, ... | | Authors: | Wang, Y, Shi, Y, Beese, L.S. | | Deposit date: | 2021-11-29 | | Release date: | 2022-11-09 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.984 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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7T0C
 | | Cryptococcus neoformans protein farnesyltransferase in complex with FPP and inhibitor 2e | | Descriptor: | (2R)-3-(cyclohexylamino)-2-hydroxypropane-1-sulfonic acid, (5S)-5-butyl-4-({1-[(4-chlorophenyl)methyl]-1H-imidazol-5-yl}methyl)-1-[3-(trifluoromethoxy)phenyl]piperazin-2-one, 1,2-ETHANEDIOL, ... | | Authors: | Wang, Y, Shi, Y, Beese, L.S. | | Deposit date: | 2021-11-29 | | Release date: | 2022-11-09 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.903 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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7T0D
 | | Cryptococcus neoformans protein farnesyltransferase in complex with FPP and inhibitor 2k | | Descriptor: | (2R)-3-(cyclohexylamino)-2-hydroxypropane-1-sulfonic acid, (5S)-4-({1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl}methyl)-5-propyl-1-[3-(trifluoromethoxy)phenyl]piperazin-2-one, 1,2-ETHANEDIOL, ... | | Authors: | Wang, Y, Shi, Y, Beese, L.S. | | Deposit date: | 2021-11-29 | | Release date: | 2022-11-09 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.906 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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7T08
 | | Cryptococcus neoformans protein farnesyltransferase in complex with FPP and inhibitor 2q | | Descriptor: | (2R)-3-(cyclohexylamino)-2-hydroxypropane-1-sulfonic acid, 1,2-ETHANEDIOL, 4-{[5-({(2S)-2-butyl-5-oxo-4-[3-(trifluoromethoxy)phenyl]piperazin-1-yl}methyl)-1H-imidazol-1-yl]methyl}-2-fluorobenzonitrile, ... | | Authors: | Wang, Y, Shi, Y, Beese, L.S. | | Deposit date: | 2021-11-29 | | Release date: | 2022-11-09 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.803 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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7T0A
 | | Cryptococcus neoformans protein farnesyltransferase co-crystallized with FPP and inhibitor 2f | | Descriptor: | (2R)-3-(cyclohexylamino)-2-hydroxypropane-1-sulfonic acid, (5S)-4-({1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl}methyl)-5-butyl-1-[3-(trifluoromethoxy)phenyl]piperazin-2-one, 1,2-ETHANEDIOL, ... | | Authors: | Wang, Y, Shi, Y, Beese, L.S. | | Deposit date: | 2021-11-29 | | Release date: | 2022-11-09 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.099 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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7RN5
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7RNI
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6VPT
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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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6J7F
 | | Complex of GGTaseIII, farnesyl-Ykt6 (C-terminal methylated), and GGPP | | Descriptor: | DIPHOSPHATE, FARNESYL, GERAN-8-YL GERAN, ... | | Authors: | Goto-Ito, S, Yamagata, A, Sato, Y, Fukai, S. | | Deposit date: | 2019-01-18 | | Release date: | 2020-01-22 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.883 Å) | | Cite: | Complex of GGTaseIII, farnesyl-Ykt6 (C-terminal methylated), and GGPP
To Be Published
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6J7X
 | | Complex of GGTaseIII, farnesyl-Ykt6, and GGPP | | Descriptor: | FORMIC ACID, GERANYLGERANYL DIPHOSPHATE, Geranylgeranyl transferase type-2 subunit beta, ... | | Authors: | Goto-Ito, S, Yamagata, A, Sato, Y, Fukai, S. | | Deposit date: | 2019-01-18 | | Release date: | 2020-01-22 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | Complex of GGTaseIII, farnesyl-Ykt6 (C-terminal methylated), and GGPP
To Be Published
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6J6X
 | | Crystal structure of apo GGTaseIII | | Descriptor: | (4S)-2-METHYL-2,4-PENTANEDIOL, Geranylgeranyl transferase type-2 subunit beta, MAGNESIUM ION, ... | | Authors: | Goto-Ito, S, Yamagata, A, Sato, Y, Fukai, S. | | Deposit date: | 2019-01-16 | | Release date: | 2020-01-22 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.962 Å) | | Cite: | Crystal structure of apo GGTaseIII
To Be Published
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6J74
 | | Complex of GGTaseIII and full-length Ykt6 | | Descriptor: | Geranylgeranyl transferase type-2 subunit beta, PHOSPHATE ION, Protein prenyltransferase alpha subunit repeat-containing protein 1, ... | | Authors: | Goto-Ito, S, Yamagata, A, Sato, Y, Fukai, S. | | Deposit date: | 2019-01-16 | | Release date: | 2020-01-22 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (3.212 Å) | | Cite: | Complex of GGTaseIII and full-length Ykt6
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: | 2019-12-25 | | 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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4MBG
 | | Crystal structure of Aspergillus fumigatus protein farnesyltransferase binary complex with farnesyldiphosphate | | Descriptor: | 1,2-ETHANEDIOL, CaaX farnesyltransferase alpha subunit Ram2, CaaX farnesyltransferase beta subunit Ram1, ... | | Authors: | Mabanglo, M.F, Hast, M.A, Beese, L.S. | | Deposit date: | 2013-08-19 | | Release date: | 2014-01-01 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.74 Å) | | Cite: | Crystal structures of the fungal pathogen Aspergillus fumigatus protein farnesyltransferase complexed with substrates and inhibitors reveal features for antifungal drug design.
Protein Sci., 23, 2014
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4LNG
 | | Aspergillus fumigatus protein farnesyltransferase complex with farnesyldiphosphate and tipifarnib | | Descriptor: | 1,2-ETHANEDIOL, 6-[(S)-AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-4-(3-CHLOROPHENYL)-1-METHYLQUINOLIN-2(1H)-ONE, CaaX farnesyltransferase alpha subunit Ram2, ... | | Authors: | Mabanglo, M.F, Hast, M.A, Beese, L.S. | | Deposit date: | 2013-07-11 | | Release date: | 2014-01-01 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (1.905 Å) | | Cite: | Crystal structures of the fungal pathogen Aspergillus fumigatus protein farnesyltransferase complexed with substrates and inhibitors reveal features for antifungal drug design.
Protein Sci., 23, 2014
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4LNB
 | | Aspergillus fumigatus protein farnesyltransferase ternary complex with farnesyldiphosphate and ethylenediamine scaffold inhibitor 5 | | Descriptor: | 1,2-ETHANEDIOL, CaaX farnesyltransferase alpha subunit Ram2, CaaX farnesyltransferase beta subunit Ram1, ... | | Authors: | Mabanglo, M.F, Hast, M.A, Beese, L.S. | | Deposit date: | 2013-07-11 | | Release date: | 2014-01-01 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (1.752 Å) | | Cite: | Crystal structures of the fungal pathogen Aspergillus fumigatus protein farnesyltransferase complexed with substrates and inhibitors reveal features for antifungal drug design.
Protein Sci., 23, 2014
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4L9P
 | | Crystal structure of Aspergillus fumigatus protein farnesyltransferase complexed with the FII analog, FPT-II, and the KCVVM peptide | | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, CaaX farnesyltransferase alpha subunit Ram2, ... | | Authors: | Mabanglo, M.F, Hast, M.A, Beese, L.S. | | Deposit date: | 2013-06-18 | | Release date: | 2014-01-01 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.45 Å) | | Cite: | Crystal structures of the fungal pathogen Aspergillus fumigatus protein farnesyltransferase complexed with substrates and inhibitors reveal features for antifungal drug design.
Protein Sci., 23, 2014
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4GTS
 | | Engineered RabGGTase in complex with BMS analogue 16 | | Descriptor: | 5-{(3R)-3-(4-hydroxybenzyl)-4-[(4-methoxyphenyl)sulfonyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-7-yl}furan-2-carbaldehyde, CALCIUM ION, Geranylgeranyl transferase type-2 subunit alpha, ... | | Authors: | Guo, Z, Stigter, E.A, Bon, R.S, Waldmann, H, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2012-08-29 | | Release date: | 2012-10-24 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Development of Selective, Potent RabGGTase Inhibitors
J.Med.Chem., 55, 2012
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4GTV
 | | Engineered RabGGTase in complex with BMS analogue 13 | | Descriptor: | 4-({(3R)-7-cyano-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 diethylcarbamate, CALCIUM ION, Geranylgeranyl transferase type-2 subunit alpha, ... | | Authors: | Guo, Z, Stigter, E.A, Bon, R.S, Waldmann, H, Blankenfeldt, W, Goody, R.S. | | Deposit date: | 2012-08-29 | | Release date: | 2012-10-24 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Development of Selective, Potent RabGGTase Inhibitors
J.Med.Chem., 55, 2012
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