6HVU
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7NAO
| Human PA28-20S proteasome complex | 分子名称: | Proteasome activator complex subunit 1, Proteasome activator complex subunit 2, Proteasome subunit alpha type-1, ... | 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 (2.9 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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4QW0
| yCP beta5-A49T-A50V-double 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 (2.9 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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4QV8
| yCP beta5-C52F 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 (2.9 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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4QZ6
| yCP beta5-A49T-A50V double 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 (2.9 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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6HW5
| Yeast 20S proteasome in complex with 18 | 分子名称: | (2~{S})-~{N}-[2-[[(2~{S})-1-[4-(aminomethyl)phenyl]-4-methylsulfonyl-butan-2-yl]amino]-2-oxidanylidene-ethyl]-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 (2.9 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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4QWJ
| yCP beta5-A49T-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 (2.9 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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4QWR
| yCP beta5-C52F 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 | 2014-07-17 | 公開日 | 2015-02-04 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.9 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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4QVN
| yCP beta5-M45V 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 (2.9 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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4QW1
| yCP beta5-A50V 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 (2.9 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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4QWX
| yCP 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 | 2014-07-17 | 公開日 | 2015-02-04 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.9 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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4QZZ
| yCP 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 (2.9 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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5FGI
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4Y69
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4INT
| Yeast 20S proteasome in complex with the vinyl sulfone LU122 | 分子名称: | HMB-Val-Ser-Phe(4-NH2CH2)-methyl vinyl sulfone, bound form, Proteasome component C1, ... | 著者 | Geurink, P.P, van der Linden, W.A, Mirabella, A.C, Gallastegui, N, de Bruin, G, Blom, A.E.M, Voges, M.J, Mock, E.D, Florea, B.I, van der Marel, G.A, Driessen, C, van der Stelt, M, Groll, M, Overkleeft, H.S, Kisselev, A.F. | 登録日 | 2013-01-06 | 公開日 | 2013-01-30 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | Incorporation of Non-natural Amino Acids Improves Cell Permeability and Potency of Specific Inhibitors of Proteasome Trypsin-like Sites. J.Med.Chem., 56, 2013
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4YA4
| Yeast 20S proteasome beta2-H114D mutant | 分子名称: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | 著者 | Huber, E.M, Groll, M. | 登録日 | 2015-02-17 | 公開日 | 2015-06-17 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors. J.Am.Chem.Soc., 137, 2015
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4Y8U
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4YA1
| Yeast 20S proteasome beta2-H116N mutant | 分子名称: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | 著者 | Huber, E.M, Groll, M. | 登録日 | 2015-02-17 | 公開日 | 2015-06-17 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors. J.Am.Chem.Soc., 137, 2015
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5JHR
| Yeast 20S proteasome in complex with the peptidic epoxyketone inhibitor 27 | 分子名称: | (2S)-2-azido-N-[(2S)-3-(biphenyl-4-yl)-1-{[(2S)-1-{[(2S,3S,4R)-3,5-dihydroxy-4-methylpentan-2-yl]amino}-1-oxo-3-phenylpropan-2-yl]amino}-1-oxopropan-2-yl]-3-phenylpropanamide (non-preferred name), 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | 著者 | Huber, E.M, Groll, M. | 登録日 | 2016-04-21 | 公開日 | 2016-08-03 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | Structure-Based Design of beta 5c Selective Inhibitors of Human Constitutive Proteasomes. J.Med.Chem., 59, 2016
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6GOP
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5CGG
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5D0V
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5CZ9
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4JSU
| Yeast 20S proteasome in complex with the dimerized linear mimetic of TMC-95A - yCP:3a | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Probable proteasome subunit alpha type-7, Proteasome subunit alpha type-1, ... | 著者 | Desvergne, A, Genin, E, Marechal, X, Gallastegui, N, Dufau, L, Richy, N, Groll, M, Vidal, J, Reboud-Ravaux, M. | 登録日 | 2013-03-22 | 公開日 | 2013-05-01 | 最終更新日 | 2023-11-15 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome J.Med.Chem., 56, 2013
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4NO9
| yCP in complex with Z-Leu-Leu-Leu-epoxyketone | 分子名称: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2R,3S,4S)-1,3-dihydroxy-2,6-dimethylheptan-4-yl]-L-leucinamide, N-[(benzyloxy)carbonyl]-L-leucyl-N-{(1R,2S)-1-hydroxy-4-methyl-1-[(2R)-2-methyloxiran-2-yl]pentan-2-yl}-L-leucinamide, ... | 著者 | Stein, M.L, Cui, H, Beck, P, Dubiella, C, Voss, C, Krueger, A, Schmidt, B, Groll, M. | 登録日 | 2013-11-19 | 公開日 | 2014-02-12 | 最終更新日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | Systematic Comparison of Peptidic Proteasome Inhibitors Highlights the alpha-Ketoamide Electrophile as an Auspicious Reversible Lead Motif. Angew.Chem.Int.Ed.Engl., 53, 2014
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