5AHJ
 
 | | Yeast 20S proteasome in complex with Macyranone A | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 20S PROTEASOME, CHLORIDE ION, ... | | 著者 | Etzbach, L, Plaza, A, Dubiella, C, Groll, M, Kaiser, M, Mueller, R. | | 登録日 | 2015-02-06 | | 公開日 | 2015-02-18 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Macyranones: Structure, Biosynthesis, and Binding Mode of an Unprecedented Epoxyketone that Targets the 20S Proteasome.
J.Am.Chem.Soc., 137, 2015
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4QVL
 | | yCP in complex with bortezomib | | 分子名称: | CHLORIDE ION, MAGNESIUM ION, N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-15 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QZ7
 | | yCP beta5-A50V mutant in complex with the epoxyketone inhibitor ONX 0914 | | 分子名称: | 1,2,4-trideoxy-4-methyl-2-{[N-(morpholin-4-ylacetyl)-L-alanyl-O-methyl-L-tyrosyl]amino}-1-phenyl-D-xylitol, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-27 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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3DY4
 | | Crystal structure of yeast 20S proteasome in complex with spirolactacystin | | 分子名称: | Omuralide, open form, Proteasome component C1, ... | | 著者 | Groll, M, Balskus, E, Jacobsen, E. | | 登録日 | 2008-07-25 | | 公開日 | 2008-11-04 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structural analysis of spiro beta-lactone proteasome inhibitors.
J.Am.Chem.Soc., 130, 2008
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4HRD
 | | Crystal structure of yeast 20S proteasome in complex with the natural product carmaphycin A | | 分子名称: | N-[(2S)-1-({(2S)-1-{[(2R,3S,4S)-1,3-dihydroxy-2,6-dimethylheptan-4-yl]amino}-4-[(R)-methylsulfinyl]-1-oxobutan-2-yl}amino)-3-methyl-1-oxobutan-2-yl]hexanamide, Proteasome component C1, Proteasome component C11, ... | | 著者 | Trivella, D.B.B, Stein, M, Groll, M. | | 登録日 | 2012-10-27 | | 公開日 | 2014-01-29 | | 最終更新日 | 2014-07-02 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Enzyme inhibition by hydroamination: design and mechanism of a hybrid carmaphycin-syringolin enone proteasome inhibitor.
Chem.Biol., 21, 2014
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5BXN
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6HVX
 | | Yeast 20S proteasome in complex with 4 | | 分子名称: | (2~{S})-~{N}-[(2~{S})-1-[[(2~{S})-1-[4-(aminomethyl)phenyl]-4-methylsulfonyl-butan-2-yl]amino]-1-oxidanylidene-propan-2-yl]-2-[[(2~{S})-2-azido-3-phenyl-propanoyl]amino]-4-methyl-pentanamide, CHLORIDE ION, MAGNESIUM ION, ... | | 著者 | Huber, E.M, Groll, M. | | 登録日 | 2018-10-11 | | 公開日 | 2019-01-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structure-Based Design of Inhibitors Selective for Human Proteasome beta 2c or beta 2i Subunits.
J.Med.Chem., 62, 2019
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4QWK
 | | yCP beta5-A49T-A50V-double mutant in complex with carfilzomib | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-16 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4HRC
 | | Crystal structure of yeast 20S proteasome in complex with epoxyketone carmaphycin analogue 3 | | 分子名称: | N-hexanoyl-L-valyl-N~1~-[(2R,3S,4S)-1,3-dihydroxy-2,6-dimethylheptan-4-yl]-N~5~,N~5~-dimethyl-L-glutamamide, Proteasome component C1, Proteasome component C11, ... | | 著者 | Trivella, D.B.B, Stein, M, Groll, M. | | 登録日 | 2012-10-27 | | 公開日 | 2014-01-29 | | 最終更新日 | 2014-07-02 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Enzyme inhibition by hydroamination: design and mechanism of a hybrid carmaphycin-syringolin enone proteasome inhibitor.
Chem.Biol., 21, 2014
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8U6Y
 | | Preholo-Proteasome from Beta 3 D205 deletion | | 分子名称: | Proteasome assembly chaperone 2, Proteasome chaperone 1, Proteasome maturation factor UMP1, ... | | 著者 | Walsh Jr, R.M, Rawson, S, Velez, B, Blickling, M, Razi, A, Hanna, J. | | 登録日 | 2023-09-14 | | 公開日 | 2024-04-17 | | 最終更新日 | 2024-04-24 | | 実験手法 | ELECTRON MICROSCOPY (2.8 Å) | | 主引用文献 | Mechanism of autocatalytic activation during proteasome assembly.
Nat.Struct.Mol.Biol., 2024
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5FGD
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6HWA
 | | Yeast 20S proteasome in complex with 43 | | 分子名称: | (2~{S})-~{N}-[(2~{S},3~{R})-1-[(4~{a}~{S},8~{a}~{S})-1,2,3,4,4~{a},5,6,7,8,8~{a}-decahydronaphthalen-2-yl]-4-methyl-3,4-bis(oxidanyl)pentan-2-yl]-3-(4-methoxyphenyl)-2-[[(2~{S})-2-(2-morpholin-4-ylethanoylamino)propanoyl]amino]propanamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | | 著者 | Huber, E.M, Groll, M. | | 登録日 | 2018-10-11 | | 公開日 | 2019-01-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structure-Based Design of Inhibitors Selective for Human Proteasome beta 2c or beta 2i Subunits.
J.Med.Chem., 62, 2019
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5FGH
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7NAN
 | | Human 20S proteasome core particle | | 分子名称: | Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, Proteasome subunit alpha type-3, ... | | 著者 | Zhao, J, Makhija, S, Huang, B, Cheng, Y. | | 登録日 | 2021-06-22 | | 公開日 | 2022-11-02 | | 最終更新日 | 2024-06-05 | | 実験手法 | ELECTRON MICROSCOPY (2.8 Å) | | 主引用文献 | Structural insights into the human PA28-20S proteasome enabled by efficient tagging and purification of endogenous proteins.
Proc.Natl.Acad.Sci.USA, 119, 2022
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4QZ5
 | | yCP beta5-A49T-mutant in complex with ONX 0914 | | 分子名称: | 1,2,4-trideoxy-4-methyl-2-{[N-(morpholin-4-ylacetyl)-L-alanyl-O-methyl-L-tyrosyl]amino}-1-phenyl-D-xylitol, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-27 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QW4
 | | yCP in complex with carfilzomib | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, MAGNESIUM ION, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-16 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QVV
 | | yCP beta5-A49V mutant in complex with bortezomib | | 分子名称: | CHLORIDE ION, MAGNESIUM ION, N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-16 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QVM
 | | yCP beta5-M45A mutant in complex with bortezomib | | 分子名称: | CHLORIDE ION, MAGNESIUM ION, N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-15 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4GK7
 | | yeast 20S proteasome in complex with the Syringolin-Glidobactin chimera | | 分子名称: | Proteasome component C1, Proteasome component C11, Proteasome component C5, ... | | 著者 | Groll, M, Stein, M.L, Bachmann, A. | | 登録日 | 2012-08-10 | | 公開日 | 2012-08-29 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Activity enhancement of the synthetic syrbactin proteasome inhibitor hybrid and biological evaluation in tumor cells.
Biochemistry, 51, 2012
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6HW8
 | | Yeast 20S proteasome in complex with 39 | | 分子名称: | (2~{S})-~{N}-[(3~{S},4~{R})-1-cyclohexyl-5-methyl-4,5-bis(oxidanyl)hexan-3-yl]-3-(4-methoxyphenyl)-2-[[(2~{S})-2-(2-morpholin-4-ylethanoylamino)propanoyl]amino]propanamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | | 著者 | Huber, E.M, Groll, M. | | 登録日 | 2018-10-11 | | 公開日 | 2019-01-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structure-Based Design of Inhibitors Selective for Human Proteasome beta 2c or beta 2i Subunits.
J.Med.Chem., 62, 2019
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4R00
 | | yCP beta5-C52F mutant in complex with Omuralide | | 分子名称: | CHLORIDE ION, MAGNESIUM ION, Omuralide, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-29 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QV6
 | | yCP beta5-A49V mutant | | 分子名称: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-14 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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4QXJ
 | | yCP beta5-M45A mutant in complex with the epoxyketone inhibitor ONX 0914 | | 分子名称: | 1,2,4-trideoxy-4-methyl-2-{[N-(morpholin-4-ylacetyl)-L-alanyl-O-methyl-L-tyrosyl]amino}-1-phenyl-D-xylitol, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | | 著者 | Huber, E.M, Heinemeyer, W, Groll, M. | | 登録日 | 2014-07-21 | | 公開日 | 2015-02-04 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914.
Structure, 23, 2015
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3SHJ
 | | Proteasome in complex with hydroxyurea derivative HU10 | | 分子名称: | 1-hydroxy-1-[(2R)-4-{3-[(3S,5S,7S)-tricyclo[3.3.1.1~3,7~]dec-1-yloxy]phenyl}but-3-yn-2-yl]urea, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Proteasome component C1, ... | | 著者 | Gallastegui, N, Beck, P, Arciniega, M, Hillebrand, S, Huber, R, Groll, M. | | 登録日 | 2011-06-16 | | 公開日 | 2011-12-07 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Hydroxyureas as noncovalent proteasome inhibitors.
Angew.Chem.Int.Ed.Engl., 51, 2012
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4J70
 | | Yeast 20S proteasome in complex with the belactosin derivative 3e | | 分子名称: | Proteasome component C1, Proteasome component C11, Proteasome component C5, ... | | 著者 | Kawamura, S, Unno, Y, List, A, Tanaka, M, Sasaki, T, Arisawa, M, Asai, A, Groll, M, Shuto, S. | | 登録日 | 2013-02-12 | | 公開日 | 2013-04-17 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Potent Proteasome Inhibitors Derived from the Unnatural cis-Cyclopropane Isomer of Belactosin A: Synthesis, Biological Activity, and Mode of Action.
J.Med.Chem., 56, 2013
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