4QW7
 
 | | yCP beta5-M45T 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 (2.7 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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4QV4
 | | yCP beta5-M45T 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 (2.7 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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4QZ2
 | | yCP beta5-M45I 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 (2.7 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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3GPJ
 | | Crystal structure of the yeast 20S proteasome in complex with syringolin B | | 分子名称: | N-{[(1S)-2-methyl-1-{[(5S,8S)-5-(1-methylethyl)-2,7-dioxo-1,6-diazacyclododec-3-en-8-yl]carbamoyl}propyl]carbamoyl}-L-valine, Proteasome component C1, Proteasome component C11, ... | | 著者 | Groll, M, Huber, R, Kaiser, M. | | 登録日 | 2009-03-23 | | 公開日 | 2009-06-02 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Synthetic and structural studies on syringolin A and B reveal critical determinants of selectivity and potency of proteasome inhibition
Proc.Natl.Acad.Sci.USA, 106, 2009
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3OKJ
 | | Alpha-keto-aldehyde binding mechanism reveals a novel lead structure motif for proteasome inhibition | | 分子名称: | N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S,3S)-3-hydroxy-1-(4-hydroxyphenyl)-4-oxobutan-2-yl]-L-leucinamide, Proteasome component C1, Proteasome component C11, ... | | 著者 | Groll, M, Poynor, M, Gallastegui, P, Stein, M, Schmidt, B, Kloetzel, P.M, Huber, R. | | 登録日 | 2010-08-25 | | 公開日 | 2011-06-08 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Elucidation of the alpha-keto-aldehyde binding mechanism: a lead structure motif for proteasome inhibition
Angew.Chem.Int.Ed.Engl., 50, 2011
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4YA7
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8CVR
 | | Human 20S proteasome with MG-132 | | 分子名称: | N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide, Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, ... | | 著者 | Zhao, J. | | 登録日 | 2022-05-18 | | 公開日 | 2022-11-02 | | 最終更新日 | 2024-06-12 | | 実験手法 | ELECTRON MICROSCOPY (2.7 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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4Y74
 | | Yeast 20S proteasome in complex with Ac-LAL-ep | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-LAL-ep, CHLORIDE ION, ... | | 著者 | Groll, M, Huber, E.M. | | 登録日 | 2015-02-13 | | 公開日 | 2015-06-17 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.7 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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4X6Z
 | | Yeast 20S proteasome in complex with PR-VI modulator | | 分子名称: | (4S)-2-METHYL-2,4-PENTANEDIOL, GLYCEROL, MAGNESIUM ION, ... | | 著者 | Rostankowski, R, Witkowska, J, Borek, D, Otwinowski, Z, Jankowska, E. | | 登録日 | 2014-12-09 | | 公開日 | 2015-12-23 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Crystal structures revealed the common place of binding of low-molecular
mass activators with the 20S proteasome
To Be Published
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3SDK
 | | Structure of yeast 20S open-gate proteasome with Compound 34 | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, MAGNESIUM ION, N-[(2S)-3-(3-tert-butyl-1,2,4-oxadiazol-5-yl)-1-({(2S)-1-[(4-methylbenzyl)amino]-1-oxo-4-phenylbutan-2-yl}amino)-1-oxopropan-2-yl]-5-methyl-1,2-oxazole-3-carboxamide, ... | | 著者 | Sintchak, M.D. | | 登録日 | 2011-06-09 | | 公開日 | 2012-06-13 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome.
Bioorg.Med.Chem.Lett., 20, 2010
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5L5V
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5CZ6
 | | Yeast 20S proteasome beta5-T1A mutant in complex with Syringolin A, propeptide expressed in trans | | 分子名称: | (2S)-2-[[(2S)-1-[[(5S,8S,9E)-2,7-dioxo-5-propan-2-yl-1,6-diazacyclododeca-3,9-dien-8-yl]amino]-3-methyl-1-oxo-butan-2-yl]carbamoylamino]-3-methyl-butanoic acid, CHLORIDE ION, MAGNESIUM ION, ... | | 著者 | Huber, E.M, Groll, M. | | 登録日 | 2015-07-31 | | 公開日 | 2016-03-23 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | A unified mechanism for proteolysis and autocatalytic activation in the 20S proteasome.
Nat Commun, 7, 2016
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6HV3
 | | Yeast 20S proteasome with human beta2i (1-53) | | 分子名称: | CHLORIDE ION, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | 著者 | Huber, E.M, Groll, M. | | 登録日 | 2018-10-10 | | 公開日 | 2019-01-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.7 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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6HW6
 | | Yeast 20S proteasome in complex with 20 | | 分子名称: | MAGNESIUM ION, Probable proteasome subunit alpha type-7, Proteasome subunit alpha type-1, ... | | 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 (2.7 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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5L64
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5L60
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5L69
 | | Yeast 20S proteasome with mouse beta5i (1-138) and mouse beta6 (97-111; 118-133) in complex with epoxyketone inhibitor 16 | | 分子名称: | (2~{S})-3-(1~{H}-indol-3-yl)-~{N}-[(2~{S},3~{S},4~{R})-4-methyl-3,5-bis(oxidanyl)-1-phenyl-pentan-2-yl]-2-[[(2~{R})-2-(2-morpholin-4-ylethanoylamino)propanoyl]amino]propanamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CHLORIDE ION, ... | | 著者 | Groll, M, Huber, E.M. | | 登録日 | 2016-05-28 | | 公開日 | 2016-11-09 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit beta 5i.
EMBO J., 35, 2016
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4NO8
 | | yCP in complex with Z-Leu-Leu-Leu-ketoamide | | 分子名称: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S,3S)-2-hydroxy-5-methyl-1-oxo-1-(phenylamino)hexan-3-yl]-L-leucinamide, Probable proteasome subunit alpha type-7, ... | | 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 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.7 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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4INR
 | | Yeast 20S proteasome in complex with the vinyl sulfone LU102 | | 分子名称: | N3Phe-Leu-Leu-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 (2.7 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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5L63
 | | Yeast 20S proteasome with human beta5c (1-138) and human beta6 (97-111; 118-133) in complex with epoxyketone inhibitor 17 | | 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 | Groll, M, Huber, E.M. | | 登録日 | 2016-05-28 | | 公開日 | 2016-11-09 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit beta 5i.
EMBO J., 35, 2016
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4Y8O
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4Y6Z
 | | Yeast 20S proteasome in complex with Ac-PAL-ep | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Ac-PAL-ep, CHLORIDE ION, ... | | 著者 | Groll, M, Huber, E.M. | | 登録日 | 2015-02-13 | | 公開日 | 2015-06-17 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.7 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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4Y8T
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4YA2
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5L5Z
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