6HTP
 
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6HUC
 | | Yeast 20S proteasome with human beta2c (S171G) 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 | 2018-10-05 | | 公開日 | 2019-01-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (3 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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6HV4
 | | Yeast 20S proteasome with human beta2i (1-53) in complex with ONX 0914 | | 分子名称: | (2~{S})-3-(4-methoxyphenyl)-~{N}-[(2~{S},3~{R})-4-methyl-3,4-bis(oxidanyl)-1-phenyl-pentan-2-yl]-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 | 2018-10-10 | | 公開日 | 2019-01-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (3 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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8T08
 | | Preholo-Proteasome from Pre1-1 Pre4-1 Double Mutant | | 分子名称: | Proteasome assembly chaperone 2, Proteasome chaperone 1, Proteasome maturation factor UMP1, ... | | 著者 | Walsh Jr, R.M, Rawson, S, Schnell, H, Velez, B, Hanna, J. | | 登録日 | 2023-05-31 | | 公開日 | 2023-09-06 | | 最終更新日 | 2023-10-25 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structure of the preholoproteasome reveals late steps in proteasome core particle biogenesis.
Nat.Struct.Mol.Biol., 30, 2023
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6ZP8
 | | Yeast 20S proteasome in complex with glidobactin-like natural product HB335 | | 分子名称: | (2~{S},3~{R})-~{N}-[(5~{S},8~{S},10~{S})-5-methyl-10-oxidanyl-2,7-bis(oxidanylidene)-1,6-diazacyclododec-8-yl]-3-oxidanyl-2-(3-phenylpropanoylamino)butanamide, CHLORIDE ION, MAGNESIUM ION, ... | | 著者 | Zhao, L, Le Chapelain, C, Brachmann, A.O, Kaiser, M, Groll, M, Bode, H.B. | | 登録日 | 2020-07-08 | | 公開日 | 2021-05-19 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Activation, Structure, Biosynthesis and Bioactivity of Glidobactin-like Proteasome Inhibitors from Photorhabdus laumondii.
Chembiochem, 22, 2021
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4NO6
 | | yCP in complex with Z-Leu-Leu-Leu-vinylsulfone | | 分子名称: | MAGNESIUM ION, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(3S)-5-methyl-1-(methylsulfonyl)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 (3 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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6XMJ
 | | Human 20S proteasome bound to an engineered 11S (PA26) activator | | 分子名称: | Proteasome activator protein PA26, Proteasome subunit alpha type-1, Proteasome subunit alpha type-2, ... | | 著者 | de la Pena, A.H, Opoku-Nsiah, K.A, Williams, S.K, Chopra, N, Sali, A, Gestwicki, J.E, Lander, G.C. | | 登録日 | 2020-06-30 | | 公開日 | 2020-07-22 | | 最終更新日 | 2024-05-15 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | The Y Phi motif defines the structure-activity relationships of human 20S proteasome activators.
Nat Commun, 13, 2022
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6HV5
 | | Yeast 20S proteasome with human beta2i (1-53) 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 | 2018-10-10 | | 公開日 | 2019-01-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (3 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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4Z1L
 | | Yeast 20S proteasome in complex with belactosin C derivative 3 | | 分子名称: | (2S,3S)-2-{(1R)-2-[(3,5-dimethoxybenzyl)amino]-1-hydroxy-2-oxoethyl}-3-methylpentanoic acid, CHLORIDE ION, MAGNESIUM ION, ... | | 著者 | Huber, E.M, Groll, M. | | 登録日 | 2015-03-27 | | 公開日 | 2015-05-27 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | A Minimal beta-Lactone Fragment for Selective beta 5c or beta 5i Proteasome Inhibitors.
Angew.Chem.Int.Ed.Engl., 54, 2015
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6REY
 | | Human 20S-PA200 Proteasome Complex | | 分子名称: | INOSITOL HEXAKISPHOSPHATE, Proteasome activator complex subunit 4, Proteasome subunit alpha type-1, ... | | 著者 | Toste Rego, A, da Fonseca, P.C.A. | | 登録日 | 2019-04-12 | | 公開日 | 2019-09-04 | | 最終更新日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Characterization of Fully Recombinant Human 20S and 20S-PA200 Proteasome Complexes.
Mol.Cell, 76, 2019
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1JD2
 | | Crystal Structure of the yeast 20S Proteasome:TMC-95A complex: A non-covalent Proteasome Inhibitor | | 分子名称: | MAGNESIUM ION, PROTEASOME COMPONENT C1, PROTEASOME COMPONENT C11, ... | | 著者 | Groll, M, Koguchi, Y, Huber, R, Kohno, J. | | 登録日 | 2001-06-12 | | 公開日 | 2002-02-13 | | 最終更新日 | 2017-10-04 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Crystal structure of the 20 S proteasome:TMC-95A complex: a non-covalent proteasome inhibitor.
J.Mol.Biol., 311, 2001
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6HUQ
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3E47
 | | Crystal Structure of the Yeast 20S Proteasome in Complex with Homobelactosin C | | 分子名称: | Proteasome component C1, Proteasome component C11, Proteasome component C5, ... | | 著者 | Groll, M, Larionov, O.V, de Meijere, A. | | 登録日 | 2008-08-10 | | 公開日 | 2008-09-02 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Inhibitor-binding mode of homobelactosin C to proteasomes: new insights into class I MHC ligand generation
Proc.Natl.Acad.Sci.Usa, 103, 2006
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7W37
 | | Structure of USP14-bound human 26S proteasome in state EA1_UBL | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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4QBY
 | | yCP in complex with BOC-ALA-ALA-ALA-CHO | | 分子名称: | BOC-ALA-ALA-ALA-CHO, MAGNESIUM ION, Probable proteasome subunit alpha type-7, ... | | 著者 | Arciniega, M, Beck, P, Lange, O, Groll, M, Huber, R. | | 登録日 | 2014-05-09 | | 公開日 | 2014-06-18 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Differential global structural changes in the core particle of yeast and mouse proteasome induced by ligand binding.
Proc.Natl.Acad.Sci.USA, 111, 2014
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4FZG
 | | 20S yeast proteasome in complex with glidobactin | | 分子名称: | Glidobactin, Proteasome component C1, Proteasome component C11, ... | | 著者 | Stein, M, Beck, P, Kaiser, M, Dudler, R, Becker, C.F.W, Groll, M. | | 登録日 | 2012-07-06 | | 公開日 | 2012-10-24 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | One-shot NMR analysis of microbial secretions identifies highly potent proteasome inhibitor.
Proc.Natl.Acad.Sci.USA, 109, 2012
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4QZ4
 | | yCP beta5-A49S 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 (3 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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4V7O
 | | Proteasome Activator Complex | | 分子名称: | Proteasome activator BLM10, Proteasome component C1, Proteasome component C11, ... | | 著者 | Hill, C.P, Whitby, F.G. | | 登録日 | 2009-12-22 | | 公開日 | 2014-07-09 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (3.005 Å) | | 主引用文献 | Structure of a Blm10 complex reveals common mechanisms for proteasome binding and gate opening.
Mol.Cell, 37, 2010
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8RHJ
 | | Yeast 20S proteasome in complex with a macrocyclic oxindole epoxyketone (compound 5) | | 分子名称: | CHLORIDE ION, MAGNESIUM ION, Macrocyclic oxindole epoxyketone, ... | | 著者 | Goetz, M.G, Godwin, K, Price, R, Dorn, R, Merrill-Steskal, G, Hansen, H, Klemmer, W, Produturi, G, Rocha, M, Palmer, M, Molacek, L, Strater, Z, Groll, M. | | 登録日 | 2023-12-15 | | 公開日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (3.05 Å) | | 主引用文献 | Macrocyclic Oxindole Peptide Epoxyketones-A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome.
Acs Med.Chem.Lett., 15, 2024
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7W38
 | | Structure of USP14-bound human 26S proteasome in state EA2.0_UBL | | 分子名称: | 26S protease regulatory subunit 4, 26S protease regulatory subunit 6A, 26S protease regulatory subunit 6B, ... | | 著者 | Zhang, S, Zou, S, Yin, D, Wu, Z, Mao, Y. | | 登録日 | 2021-11-25 | | 公開日 | 2022-05-04 | | 最終更新日 | 2022-06-01 | | 実験手法 | ELECTRON MICROSCOPY (3.1 Å) | | 主引用文献 | USP14-regulated allostery of the human proteasome by time-resolved cryo-EM.
Nature, 605, 2022
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4QV0
 | | yCP beta5-A49T-A50V-double 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 (3.1 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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8CVS
 | | Human PA200-20S proteasome with MG-132 | | 分子名称: | INOSITOL HEXAKISPHOSPHATE, N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide, Proteasome activator complex subunit 4, ... | | 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 (3.1 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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6HVS
 | | Yeast 20S proteasome with human beta2i (1-53) 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 (3.1 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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4INU
 | | Yeast 20S proteasome in complex with the vinyl sulfone LU112 | | 分子名称: | N3Phe-Phe(4-NH2CH2)-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 (3.1 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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6HUV
 | | Yeast 20S proteasome with human beta2c (S171G) 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 | 2018-10-09 | | 公開日 | 2019-01-30 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (3.1 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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