Literature for peptidase T01.012: proteasome subunit beta5c

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

(Topics flags: A Assay, S Structure, T Target, P Specificity, K Knockout, V Review, M Mutation, I Inhibitor, L Localization. To select only the references relevant to a single topic, click the link above. See explanation.)

    2024
  1. Wang,S., Li,Z., Ma,S., Zhang,S., Guo,S., Ma,Z., Du,L. and Li,M.
    Discovery of novel 20S proteasome subunit beta5 PROTAC degraders as potential therapeutics for pharyngeal carcinoma and Bortezomib-resistant multiple myeloma
    Bioorg Chem153, 107801-107801. PubMed  Europe PubMed DOI  I
  2. 2023
  3. Douglas,C., Lomeli,N., Lepe,J., Di,K., Nandwana,N.K., Vu,T., Pham,J., Kenney,M.C., Das,B. and Bota,D.A.
    Discovery and Validation of Novel LonP1 and Proteasome Inhibitor in IDH1-R132H Malignant Astrocytoma Models
    bioRxiv PubMed  Europe PubMed DOI  I
  4. Muli,C.S. and Trader,D.J.
    20S proteasome hydrolysis of LLVY substrates to determine preferences for moieties in its primed substrate channel
    Bioorg Med Chem Lett85, 129233-129233. PubMed  Europe PubMed DOI
  5. 2022
  6. Fu,M., Liu,Y., Wang,G., Wang,P., Zhang,J., Chen,C., Zhao,M., Zhang,S., Jiao,J., Ouyang,X., Yu,Y., Wen,B., He,C., Wang,J., Zhou,D. and Xiong,X.
    A protein-protein interaction map reveals that the Coxiella burnetii effector CirB inhibits host proteasome activity
    PLoS Pathog18, e1010660-e1010660. PubMed  Europe PubMed DOI  K
  7. Han,L., Hao,Y., Wu,X. and Hu,D.
    PSMB5 Alleviates Ulcerative Colitis by Inhibiting ROS-Dependent NLRP3 Inflammasome-Mediated Pyroptosis
    Dis Markers2022, 2329904-2329904. PubMed  Europe PubMed DOI
  8. Kong,H.E., Lim,J., Linsalata,A., Kang,Y., Malik,I., Allen,E.G., Cao,Y., Shubeck,L., Johnston,R., Huang,Y., Gu,Y., Guo,X., Zwick,M.E., Qin,Z., Wingo,T.S., Juncos,J., Nelson,D.L., Epstein,M.P., Cutler,D.J., Todd,P.K., Sherman,S.L., Warren,S.T. and Jin,P.
    Identification of PSMB5 as a genetic modifier of fragile X-associated tremor/ataxia syndrome
    Proc Natl Acad Sci U S A119, e2118124119-e2118124119. PubMed  Europe PubMed DOI  K
  9. Yang,X., Liu,A., Yang,L., Wen,T., Wang,J., Shi,J., Zhou,H., Chen,Z., Lei,M. and Zhu,Y.
    Preclinical Pharmacokinetics, Tissue Distribution and in vitro Metabolism of FHND6091, a Novel Oral Proteasome Inhibitor
    Drug Des Devel Ther16, 3087-3107. PubMed  Europe PubMed DOI  I
  10. Yang,Y., Gao,Y., Huang,J., Yang,Z., Luo,H., Wang,F., Xu,J., Cui,Y., Ding,H., Lin,Z., Zhai,X., Qu,Y., Zhang,L., Liu,T., Ye,L., Niu,T. and Zheng,Y.
    ISG20L2 suppresses bortezomib antimyeloma activity by attenuating bortezomib binding to PSMB5
    JCI Insight7, PubMed  Europe PubMed DOI  I
  11. 2020
  12. Caputi,F.F., Di Cesare Mannelli,L., Rullo,L., Micheli,L., Stamatakos,S., Posa,L., Ghelardini,C., Romualdi,P. and Candeletti,S.
    The active second-generation proteasome inhibitor oprozomib reverts the oxaliplatin-induced neuropathy symptoms
    Biochem Pharmacol182, 114255-114255. PubMed  Europe PubMed DOI  I
  13. Corrigan,T.S., Lotti Diaz,L.M., Border,S.E., Ratigan,S.C., Kasper,K.Q., Sojka,D., Fajtova,P., Caffrey,C.R., Salvesen,G.S., McElroy,C.A., Hadad,C.M. and Dogan Ekici,O.
    Design, synthesis, and in vitro evaluation of aza-peptide aldehydes and ketones as novel and selective protease inhibitors
    J Enzyme Inhib Med Chem35, 1387-1402. PubMed  Europe PubMed DOI  I
  14. Koper-Lenkiewicz,O.M., Kaminska,J., Reszec,J., Dymicka-Piekarska,V., Ostrowska,H., Karpinska,M., Matowicka-Karna,J. and Tylicka,M.
    Elevated plasma 20S proteasome chymotrypsin-like activity is correlated with IL-8 levels and associated with an increased risk of death in glial brain tumor patients
    PLoS ONE15, e0238406-e0238406. PubMed  Europe PubMed DOI
  15. Sanchez,G., Chalmers,S., Ahumada,X., Montecinos,L., Olmedo,I., Eisner,V., Riveros,A., Kogan,M.J., Lavandero,S., Pedrozo,Z. and Donoso,P.
    Inhibition of chymotrypsin-like activity of the proteasome by ixazomib prevents mitochondrial dysfunction during myocardial ischemia
    PLoS ONE15, e0233591-e0233591. PubMed  Europe PubMed DOI  I
  16. Sun,Q., Zhou,T., Xi,D., Li,X., Lu,Z., Xu,F., Wang,C., Niu,Y. and Xu,P.
    Design and synthesis of tripeptidyl furylketones as selective inhibitors against the beta5 subunit of human 20S proteasome
    Eur J Med Chem192, 112160-112160. PubMed  Europe PubMed DOI  I
  17. 2019
  18. Besse,A., Besse,L., Kraus,M., Mendez-Lopez,M., Bader,J., Xin,B.T., de Bruin,G., Maurits,E., Overkleeft,H.S. and Driessen,C.
    Proteasome Inhibition in Multiple Myeloma: Head-to-Head Comparison of Currently Available Proteasome Inhibitors
    Cell Chem Biol26, 340-351. PubMed  Europe PubMed DOI  I
  19. Han,J.J., Yang,X., Wang,Q., Tang,L., Yu,F., Huang,X., Wang,Y., Liu,J.X. and Xie,Q.
    The beta5 subunit is essential for intact 26S proteasome assembly to specifically promote plant autotrophic growth under salt stress
    New Phytol221, 1359-1368. PubMed  Europe PubMed DOI
  20. Lei,M., Feng,H., Bai,E., Zhou,H., Wang,J., Qin,Y., Zhang,H., Wang,X., Liu,Z., Hai,O., Liu,J. and Zhu,Y.
    Discovery of a novel dipeptidyl boronic acid proteasome inhibitor for the treatment of multiple myeloma and triple-negative breast cancer
    Org Biomol Chem17, 683-691. PubMed  Europe PubMed DOI  I
  21. Li,D.D., Yague,E., Wang,L.Y., Dai,L.L., Yang,Z.B., Zhi,S., Zhang,N., Zhao,X.M. and Hu,Y.H.
    Novel copper complexes that inhibit the proteasome and trigger apoptosis in triple-negative breast cancer cells
    ACS Med Chem Lett10, 1328-1335. PubMed  Europe PubMed DOI  I
  22. Matsunaga,T., Tsuchimura,S., Azuma,N., Endo,S., Ichihara,K. and Ikari,A.
    Caffeic acid phenethyl ester potentiates gastric cancer cell sensitivity to doxorubicin and cisplatin by decreasing proteasome function
    Anticancer Drugs30, 251-259. PubMed  Europe PubMed DOI  I
  23. Munkacsy,E., Chocron,E.S., Quintanilla,L., Gendron,C.M., Pletcher,S.D. and Pickering,A.M.
    Neuronal-specific proteasome augmentation via Prosbeta5 overexpression extends lifespan and reduces age-related cognitive decline
    Aging Celle13005-e13005. PubMed  Europe PubMed DOI
  24. Wyllie,S., Brand,S., Thomas,M., De Rycker,M., Chung,C.W., Pena,I., Bingham,R.P., Bueren-Calabuig,J.A., Cantizani,J., Cebrian,D., Craggs,P.D., Ferguson,L., Goswami,P., Hobrath,J., Howe,J., Jeacock,L., Ko,E.J., Korczynska,J., MacLean,L., Manthri,S., Martinez,M.S., Mata-Cantero,L., Moniz,S., Nuhs,A., Osuna-Cabello,M., Pinto,E., Riley,J., Robinson,S., Rowland,P., Simeons,F.R.C., Shishikura,Y., Spinks,D., Stojanovski,L., Thomas,J., Thompson,S., Viayna Gaza,E., Wall,R.J., Zuccotto,F., Horn,D., Ferguson,M.A.J., Fairlamb,A.H., Fiandor,J.M., Martin,J., Gray,D.W., Miles,T.J., Gilbert,I.H., Read,K.D., Marco,M. and Wyatt,P.G.
    Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition
    Proc Natl Acad Sci U S A116, 9318-9323. PubMed  Europe PubMed DOI  S
  25. Yu,J., Xu,L., Hong,D., Zhang,X., Liu,J., Li,D., Li,J., Zhou,Y. and Liu,T.
    Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors
    Eur J Med Chem161, 543-558. PubMed  Europe PubMed DOI  I
  26. Yu,J., Liu,J., Li,D., Xu,L., Hong,D., Chang,S., Xu,L., Li,J., Liu,T. and Zhou,Y.
    Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors
    Eur J Med Chem164, 423-439. PubMed  Europe PubMed DOI  I
  27. Zapata-Carmona,H., Baron,L., Zuniga,L.M., Diaz,E.S., Kong,M., Drobnis,E.Z., Sutovsky,P. and Morales,P.
    The activation of the chymotrypsin-like activity of the proteasome is regulated by soluble adenyl cyclase / cAMP / protein kinase a pathway and required for human sperm capacitation
    Mol Hum Reprod25, 587-600. PubMed  Europe PubMed DOI
  28. 2018
  29. Arba,M., Nur-Hidayat,A., Ruslin, Yusuf,M., Sumarlin, Hertadi,R., Wahyudi,S.T., Surantaadmaja,S.I. and Tjahjono,D.H.
    Molecular modeling on porphyrin derivatives as beta5 subunit inhibitor of 20S proteasome
    Comput Biol Chem74, 230-238. PubMed  Europe PubMed DOI  I
  30. Groll,M., Nguyen,H., Vellalath,S. and Romo,D.
    (-)-Homosalinosporamide A and its mode of proteasome inhibition: an X-ray crystallographic study
    Mar Drugs16, PubMed  Europe PubMed DOI  S  I
  31. Inoue,M., Hitora,Y., Kato,H., Losung,F., Mangindaan,R.E.P. and Tsukamoto,S.
    New geranyl flavonoids from the leaves of Artocarpus communis
    J Nat Med72, 632-640. PubMed  Europe PubMed DOI  I
  32. Lei,M., Feng,H., Bai,E., Zhou,H., Wang,J., Shi,J., Wang,X., Hu,S., Liu,Z. and Zhu,Y.
    Design, synthesis, in vitro and in vivo evaluation, and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studies
    Bioorg Med Chem26, 3975-3981. PubMed  Europe PubMed DOI  I
  33. Liu,H., Wu,J., Ge,Y., Li,A., Li,J., Liu,Z., Xu,Y., Xu,Q. and Li,Y.
    Novel aromatic sulfonyl naphthalene-based boronates as 20S proteasome inhibitors
    Bioorg Med Chem26, 1050-1061. PubMed  Europe PubMed DOI  I
  34. Oerlemans,R., Berkers,C.R., Assaraf,Y.G., Scheffer,G.L., Peters,G.J., Verbrugge,S.E., Cloos,J., Slootstra,J., Meloen,R.H., Shoemaker,R.H., Dijkmans,B.A.C., Scheper,R.J., Ovaa,H. and Jansen,G.
    Proteasome inhibition and mechanism of resistance to a synthetic, library-based hexapeptide
    Invest New Drugs36, 797-809. PubMed  Europe PubMed DOI  I
  35. Pierce,M.R., Bakas,N.A., Pirrung,M.C. and Bachmann,A.S.
    Thiasyrbactins induce cell death via proteasome inhibition in multiple myeloma cells
    Anticancer Res38, 5607-5613. PubMed  Europe PubMed DOI  I
  36. Xie,S.C., Gillett,D.L., Spillman,N.J., Tsu,C., Luth,M.R., Ottilie,S., Duffy,S., Gould,A.E., Hales,P., Seager,B.A., Charron,C.L., Bruzzese,F., Yang,X., Zhao,X., Huang,S.C., Hutton,C.A., Burrows,J.N., Winzeler,E.A., Avery,V.M., Dick,L.R. and Tilley,L.
    Target validation and identification of novel boronate inhibitors of the Plasmodium falciparum proteasome
    J Med Chem61, 10053-10066. PubMed  Europe PubMed DOI  I
  37. 2017
  38. Hewings,D.S., Flygare,J.A., Wertz,I.E. and Bogyo,M.
    Activity-based probes for the multicatalytic proteasome
    FEBS J284, 1540-1554. PubMed  Europe PubMed DOI  V  L  I
  39. Jorda,R., Dusek,J., Reznickova,E., Pauk,K., Magar,P.P., Imramovsky,A. and Krystof,V.
    Synthesis and antiproteasomal activity of novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine
    Eur J Med Chem135, 142-158. PubMed  Europe PubMed DOI  I
  40. LaMonte,G.M., Almaliti,J., Bibo-Verdugo,B., Keller,L., Zou,B.Y., Yang,J., Antonova-Koch,Y., Orjuela-Sanchez,P., Boyle,C.A., Vigil,E., Wang,L., Goldgof,G.M., Gerwick,L., O'Donoghue,A.J., Winzeler,E.A., Gerwick,W.H. and Ottilie,S.
    Development of a potent inhibitor of the Plasmodium proteasome with reduced mammalian toxicity
    J Med Chem60, 6721-6732. PubMed  Europe PubMed DOI  I
  41. Misas-Villamil,J.C., van der Burgh,A.M., Grosse-Holz,F., Bach-Pages,M., Kovacs,J., Kaschani,F., Schilasky,S., Emon,A.E., Ruben,M., Kaiser,M., Overkleeft,H.S. and Van Der Hoorn,R.A.
    Subunit-selective proteasome activity profiling uncovers uncoupled proteasome subunit activities during bacterial infections
    Plant J90, 418-430. PubMed  Europe PubMed DOI
  42. Qin,J.M., Huang,R.Z., Yao,G.Y., Liao,Z.X., Pan,Y.M. and Wang,H.S.
    Terminal functionalized thiourea-containing dipeptides as multidrug-resistance reversers that target 20S proteasome and cell proliferation
    Eur J Med Chem126, 259-269. PubMed  Europe PubMed DOI  I
  43. Rolfe,M.
    The holy grail: solid tumor efficacy by proteasome inhibition
    Cell Chem Biol24, 125-126. PubMed  Europe PubMed DOI  T  I
  44. Weyburne,E.S., Wilkins,O.M., Sha,Z., Williams,D.A., Pletnev,A.A., de Bruin,G., Overkleeft,H.S., Goldberg,A.L., Cole,M.D. and Kisselev,A.F.
    Inhibition of the proteasome beta2 site sensitizes triple-negative breast cancer cells to beta5 inhibitors and suppresses Nrf1 activation
    Cell Chem Biol24, 218-230. PubMed  Europe PubMed DOI  T  I
  45. Zhuang,R., Gao,L., Lv,X., Xi,J., Sheng,L., Zhao,Y., He,R., Hu,X., Shao,Y., Pan,X., Liu,S., Huang,W., Zhou,Y., Li,J. and Zhang,J.
    Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors
    Eur J Med Chem126, 1056-1070. PubMed  Europe PubMed DOI  I
  46. 2016
  47. Bensinger,D., Neumann,T., Scholz,C., Voss,C., Knorr,S., Kuckelkorn,U., Hamacher,K., Kloetzel,P.M. and Schmidt,B.
    Elastase-like activity is dominant to chymotrypsin-like activity in 20S proteasome's beta5 catalytic subunit
    ACS Chem Biol11, 1800-1804. PubMed  Europe PubMed DOI  P  I
  48. de Bruin,G., Xin,B.T., Kraus,M., van der Stelt,M., van der Marel,G.A., Kisselev,A.F., Driessen,C., Florea,B.I. and Overkleeft,H.S.
    A set of activity-based probes to visualize human (immuno)proteasome activities
    Angew Chem Int Ed Engl55, 4199-4203. PubMed  Europe PubMed DOI  A  I
  49. Di Giovanni,C., Ettari,R., Sarno,S., Rotondo,A., Bitto,A., Squadrito,F., Altavilla,D., Schirmeister,T., Novellino,E., Grasso,S., Zappala,M. and Lavecchia,A.
    Identification of noncovalent proteasome inhibitors with high selectivity for chymotrypsin-like activity by a multistep structure-based virtual screening
    Eur J Med Chem121, 578-591. PubMed  Europe PubMed DOI  I
  50. Gruba,N., Wysocka,M., Brzezinska,M., Debowski,D., Sienczyk,M., Gorodkiewicz,E., Guszcz,T., Czaplewski,C., Rolka,K. and Lesner,A.
    Bladder cancer detection using a peptide substrate of the 20S proteasome
    FEBS J283, 2929-2948. PubMed  Europe PubMed DOI  A
  51. Huber,E.M., Heinemeyer,W., Li,X., Arendt,C.S., Hochstrasser,M. and Groll,M.
    A unified mechanism for proteolysis and autocatalytic activation in the 20S proteasome
    Nat Commun7, 10900-10900. PubMed  Europe PubMed DOI
  52. Huber,E.M., Heinemeyer,W., de Bruin,G., Overkleeft,H.S. and Groll,M.
    A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit beta5i
    EMBO J35, 2602-2613. PubMed  Europe PubMed DOI  S  I
  53. Li,X., Li,Y., Arendt,C.S. and Hochstrasser,M.
    Distinct elements in the proteasomal beta5 subunit propeptide required for autocatalytic processing and proteasome assembly
    J Biol Chem291, 1991-2003. PubMed  Europe PubMed DOI
  54. McDaniel,T.J., Lansdell,T.A., Dissanayake,A.A., Azevedo,L.M., Claes,J., Odom,A.L. and Tepe,J.J.
    Substituted quinolines as noncovalent proteasome inhibitors
    Bioorg Med Chem24, 2441-2450. PubMed  Europe PubMed DOI  I
  55. Rut,W. and Drag,M.
    Human 20S proteasome activity towards fluorogenic peptides of various chain lengths
    Biol Chem397, 921-926. PubMed  Europe PubMed DOI  P
  56. Sanchez,G., Berrios,D., Olmedo,I., Pezoa,J., Riquelme,J.A., Montecinos,L., Pedrozo,Z. and Donoso,P.
    Activation of chymotrypsin-like activity of the proteasome during ischemia induces myocardial dysfunction and death
    PLoS ONE11, e0161068-e0161068. PubMed  Europe PubMed DOI  I
  57. Shi,J., Lei,M., Wu,W., Feng,H., Wang,J., Chen,S., Zhu,Y., Hu,S., Liu,Z. and Jiang,C.
    Design, synthesis and docking studies of novel dipeptidyl boronic acid proteasome inhibitors constructed from alphaalpha- and alphabeta-amino acids
    Bioorg Med Chem Lett26, 1958-1962. PubMed  Europe PubMed DOI  I
  58. Singh,P.K., Fan,H., Jiang,X., Shi,L., Nathan,C.F. and Lin,G.
    Immunoproteasome beta5i-selective dipeptidomimetic inhibitors
    ChemMedChem11, 2127-2131. PubMed  Europe PubMed DOI  I
  59. Xin,B.T., de Bruin,G., Huber,E.M., Besse,A., Florea,B.I., Filippov,D.V., van der Marel,G.A., Kisselev,A.F., van der Stelt,M., Driessen,C., Groll,M. and Overkleeft,H.S.
    Structure-based design of beta5c selective inhibitors of human constitutive proteasomes
    J Med Chem59, 7177-7187. PubMed  Europe PubMed DOI
  60. Zhang,X., Adwal,A., Turner,A.G., Callen,D.F. and Abell,A.D.
    New peptidomimetic boronates for selective inhibition of the chymotrypsin-like activity of the 26S proteasome
    ACS Med Chem Lett7, 1039-1043. PubMed  Europe PubMed DOI  I
  61. 2015
  62. Beck,P., Lansdell,T.A., Hewlett,N.M., Tepe,J.J. and Groll,M.
    Indolo-phakellins as beta5-specific noncovalent proteasome inhibitors
    Angew Chem Int Ed Engl54, 2830-2833. PubMed  Europe PubMed DOI  I
  63. Chatterjee,S.
    Exploration to uncover a new enzyme reactive group for proteasome inhibition
    C R Chim18, 478-481. DOI  I
  64. Groll,M., Korotkov,V.S., Huber,E.M., de Meijere,A. and Ludwig,A.
    A minimal beta-lactone fragment for selective beta5c or beta5I proteasome inhibitors
    Angew Chem Int Ed Engl54, 7810-7814. PubMed  Europe PubMed DOI  I
  65. Harshbarger,W., Miller,C., Diedrich,C. and Sacchettini,J.
    Crystal structure of the human 20S proteasome in complex with carfilzomib
    Structure23, 418-424. PubMed  Europe PubMed DOI  S  I
  66. Huber,E.M., Heinemeyer,W. and Groll,M.
    Bortezomib-resistant mutant proteasomes: structural and biochemical evaluation with carfilzomib and ONX 0914
    Structure23, 407-417. PubMed  Europe PubMed DOI  S  I
  67. Huber,E.M., de Bruin,G., Heinemeyer,W., Paniagua Soriano,G., Overkleeft,H.S. and Groll,M.
    Systematic analyses of substrate preferences of 20S proteasomes using peptidic epoxyketone inhibitors
    J Am Chem Soc137, 7835-7842. PubMed  Europe PubMed DOI  P  S  I
  68. O'Brien,M.A., Moravec,R.A., Riss,T.L. and Bulleit,R.F.
    Homogeneous, bioluminescent proteasome assays
    Methods Mol Biol1219, 95-114. PubMed  Europe PubMed DOI  A
  69. Sedlacek,J. and Svecarova,M.
    Methods for determination of proteasome activity and their applications
    Chem Listy109, 198-203.  A
  70. Sun,Q., Xu,B., Niu,Y., Xu,F., Liang,L., Wang,C., Yu,J., Yan,G., Wang,W., Jin,H. and Xu,P.
    Synthesis, bioactivity, docking and molecular dynamics studies of furan-based peptides as 20S proteasome inhibitors
    ChemMedChem10, 498-510. PubMed  Europe PubMed DOI  I
  71. Wang,Z., Dove,P., Wang,X., Shamas-Din,A., Li,Z., Nachman,A., Oh,Y.J., Hurren,R., Ruschak,A., Climie,S., Press,B., Griffin,C., Undzys,E., Aman,A., Al-Awar,R., Kay,L.E., O'Neill,D., Trudel,S., Slassi,M. and Schimmer,A.D.
    FV-162 is a novel, orally bioavailable, irreversible proteasome inhibitor with improved pharmacokinetics displaying preclinical efficacy with continuous daily dosing
    Cell Death Dis6, e1815-e1815. PubMed  Europe PubMed DOI  I
  72. Xu,K., Wang,K., Yang,Y., Yan,D.A., Huang,L., Chen,C.H. and Xiao,Z.
    Discovery of novel non-covalent inhibitors selective to the beta5-subunit of the human 20S proteasome
    Eur J Med Chem98, 61-68. PubMed  Europe PubMed DOI  I
  73. 2014
  74. Arciniega,M., Beck,P., Lange,O.F., Groll,M. and Huber,R.
    Differential global structural changes in the core particle of yeast and mouse proteasome induced by ligand binding
    Proc Natl Acad Sci U S A111, 9479-9484. PubMed  Europe PubMed DOI
  75. Dal Vechio,F.H., Cerqueira,F., Augusto,O., Lopes,R. and Demasi,M.
    Peptides that activate the 20S proteasome by gate opening increased oxidized protein removal and reduced protein aggregation
    Free Radic Biol Med67, 304-313. PubMed  Europe PubMed DOI
  76. Debowski,D., Pikula,M., Lubos,M., Langa,P., Trzonkowski,P., Lesner,A., Legowska,A. and Rolka,K.
    Inhibition of human and yeast 20S proteasome by analogues of trypsin inhibitor SFTI-1
    PLoS ONE9, e89465-e89465. PubMed  Europe PubMed DOI
  77. Keita,M., Kaffy,J., Troufflard,C., Morvan,E., Crousse,B. and Ongeri,S.
    (19)F NMR monitoring of the eukaryotic 20S proteasome chymotrypsin-like activity: an investigative tool for studying allosteric regulation
    Org Biomol Chem12, 4576-4581. PubMed  Europe PubMed DOI  A
  78. Kondakova,I.V., Spirina,L.V., Koval,V.D., Shashova,E.E., Choinzonov,E.L., Ivanova,E.V., Kolomiets,L.A., Chernyshova,A.L., Slonimskaya,E.M., Usynin,E.A. and Afanas'ev,S.G.
    Chymotrypsin-like activity and subunit composition of proteasomes in human cancers
    Mol Biol48, 384-389. DOI
  79. Latif,M., Jung,M.E., Lee,K. and Choi,G.
    Synthesis and biological evaluation of tetrapeptide ketones as reversible 20S proteasome inhibitors
    Bull Korean Chem Soc35, 3571-3575. DOI  I
  80. Loizidou,E.Z. and Zeinalipour-Yazdi,C.D.
    Computational inhibition studies of the human proteasome by argyrin-based analogues with subunit specificity
    Chem Biol Drug Des84, 99-107. PubMed  Europe PubMed DOI  I
  81. Metcalf,R., Scott,L.M., Daniel,K.G. and Dou,Q.P.
    Proteasome inhibitor patents (2010 - present)
    Expert Opin Ther Pat24, 369-382. PubMed  Europe PubMed DOI  V  I
  82. Scarbaci,K., Troiano,V., Micale,N., Ettari,R., Tamborini,L., Di Giovanni,C., Cerchia,C., Grasso,S., Novellino,E., Schirmeister,T., Lavecchia,A. and Zappala,M.
    Identification of a new series of amides as non-covalent proteasome inhibitors
    Eur J Med Chem76, 1-9. PubMed  Europe PubMed DOI  I
  83. Troiano,V., Scarbaci,K., Ettari,R., Micale,N., Cerchia,C., Pinto,A., Schirmeister,T., Novellino,E., Grasso,S., Lavecchia,A. and Zappala,M.
    Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors
    Eur J Med Chem83, 1-14. PubMed  Europe PubMed DOI  I
  84. Yamakuma,M., Kato,H., Matsuo,K., El-Desoky,A.H., Kawabata,T., Losung,F., Mangindaan,R.E.P., de Voogd,N.J., Yokosawa,H. and Tsukamoto,S.
    1-Hydroxyethylhalenaquinone: a new proteasome inhibitor from the marine sponge Xestospongia sp
    Heterocycles89, 2605-2610. DOI  I
  85. Yucel,G., Van Arnam,J., Means,P.C., Huntzicker,E., Altindag,B., Lara,M.F., Yuan,J., Kuo,C. and Oro,A.E.
    Partial proteasome inhibitors induce hair follicle growth by stabilizing beta-catenin
    Stem Cells32, 85-92. PubMed  Europe PubMed DOI  I
  86. Zhang,L., Shi,W., Cao,W., Liang,X., Hu,Y., Chen,M. and Shi,G.
    Tetrandrine inhibits proteasomal chymotrypsin-like activity and induces apoptosis in human PC-3 Cells
    Lect Notes Electr Eng250 LNEE, 723-731. DOI  I
  87. 2013
  88. Bordessa,A., Keita,M., Marechal,X., Formicola,L., Lagarde,N., Rodrigo,J., Bernadat,G., Bauvais,C., Soulier,J.L., Dufau,L., Milcent,T., Crousse,B., Reboud-Ravaux,M. and Ongeri,S.
    alpha- and beta-hydrazino acid-based pseudopeptides inhibit the chymotrypsin-like activity of the eukaryotic 20S proteasome
    Eur J Med Chem70, 505-524. PubMed  Europe PubMed DOI  I
  89. D'Souza,A.J., Desai,S.D., Rudner,X.L., Kelly,M.N., Ruan,S. and Shellito,J.E.
    Suppression of the macrophage proteasome by ethanol impairs MHC class I antigen processing and presentation
    PLoS ONE8, e56890-e56890. PubMed  Europe PubMed DOI  I
  90. Felth,J., Lesiak-Mieczkowska,K., D'Arcy,P., Haglund,C., Gullbo,J., Larsson,R., Linder,S., Bohlin,L., Fryknas,M. and Rickardson,L.
    Gambogic acid is cytotoxic to cancer cells through inhibition of the ubiquitin-proteasome system
    Invest New Drugs31, 587-598. PubMed  Europe PubMed DOI  I
  91. Gotze,S., Bose,A., Abele,D., Sokolova,I.M. and Saborowski,R.
    Pitfalls in invertebrate proteasome assays
    J Exp Biol216, 1351-1354. PubMed  Europe PubMed DOI  A  I
  92. Kawamura,S., Unno,Y., List,A., Mizuno,A., Tanaka,M., Sasaki,T., Arisawa,M., Asai,A., Groll,M. and Shuto,S.
    Potent proteasome inhibitors derived from the unnatural cis-cyclopropane isomer of belactosin A: synthesis, biological activity, and mode of action
    J Med Chem56, 3689-3700. PubMed  Europe PubMed DOI  S  I
  93. Li,X., Liu,S., Huang,H., Liu,N., Zhao,C., Liao,S., Yang,C., Liu,Y., Zhao,C., Li,S., Lu,X., Liu,C., Guan,L., Zhao,K., Shi,X., Song,W., Zhou,P., Dong,X., Guo,H., Wen,G., Zhang,C., Jiang,L., Ma,N., Li,B., Wang,S., Tan,H., Wang,X., Dou,Q.P. and Liu,J.
    Gambogic acid is a tissue-specific proteasome inhibitor invitro and invivo
    Cell Rep3, 211-222. PubMed  Europe PubMed DOI  I
  94. Marechal,X., Genin,E., Qin,L., Sperandio,O., Montes,M., Basse,N., Richy,N., Miteva,M.A., Reboud-Ravaux,M., Vidal,J. and Villoutreix,B.O.
    1,2,4-Oxadiazoles identified by virtual screening and their non-covalent inhibition of the human 20S proteasome
    Curr Med Chem20, 2351-2362. PubMed  Europe PubMed DOI  I
  95. Micale,N., Ettari,R., Lavecchia,A., Di Giovanni,C., Scarbaci,K., Troiano,V., Grasso,S., Novellino,E., Schirmeister,T. and Zappala,M.
    Development of peptidomimetic boronates as proteasome inhibitors
    Eur J Med Chem64, 23-34. PubMed  Europe PubMed DOI  I
  96. Min,L., Xu,H., Wang,J., Qu,L., Jiang,B., Zeng,Y., Meng,L., Jin,H. and Shou,C.
    N-alpha-acetyltransferase 10 protein is a negative regulator of 28S proteasome through interaction with PA28beta
    FEBS Lett587, 1630-1637. PubMed  Europe PubMed DOI
  97. Neilsen,P.M., Pehere,A.D., Pishas,K.I., Callen,D.F. and Abell,A.D.
    New 26S proteasome inhibitors with high selectivity for chymotrypsin-like activity and p53-dependent cytotoxicity
    ACS Chem Biol8, 353-359. PubMed  Europe PubMed DOI  I
  98. Ozcan,S., Kazi,A., Marsilio,F., Fang,B., Guida,W.C., Koomen,J., Lawrence,H.R. and Sebti,S.M.
    Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors
    J Med Chem56, 3783-3805. PubMed  Europe PubMed DOI  I
  99. 2012
  100. Dang,Z., Jung,K., Qian,K., Lee,K.H., Huang,L. and Chen,C.H.
    Synthesis of lithocholic acid derivatives as proteasome regulators
    ACS Med Chem Lett3, 925-930. PubMed  Europe PubMed DOI  I
  101. de Jong,A., Schuurman,K.G., Rodenko,B., Ovaa,H. and Berkers,C.R.
    Fluorescence-based proteasome activity profiling
    Methods Mol Biol803, 183-204. PubMed  Europe PubMed DOI  A
  102. Dunn,D., Iqbal,M., Husten,J., Ator,M.A. and Chatterjee,S.
    Serendipity in discovery of proteasome inhibitors
    Bioorg Med Chem Lett22, 3503-3505. PubMed  Europe PubMed DOI  I
  103. Franke,N.E., Niewerth,D., Assaraf,Y.G., van Meerloo,J., Vojtekova,K., van Zantwijk,C.H., Zweegman,S., Chan,E.T., Kirk,C.J., Geerke,D.P., Schimmer,A.D., Kaspers,G.J., Jansen,G. and Cloos,J.
    Impaired bortezomib binding to mutant beta5 subunit of the proteasome is the underlying basis for bortezomib resistance in leukemia cells
    Leukemia26, 757-768. PubMed  Europe PubMed DOI  M  I
  104. Grawert,M.A. and Groll,M.
    Eukaryotic 20S proteasome
    [ISSN:978-0-12-407742-3]3, 3684-3691. DOI
  105. Joeris,T., Schmidt,N., Ermert,D., Krienke,P., Visekruna,A., Kuckelkorn,U., Kaufmann,S.H. and Steinhoff,U.
    The proteasome system in infection: impact of beta5 and LMP7 on composition, maturation and quantity of active proteasome complexes
    PLoS ONE7, e39827-e39827. PubMed  Europe PubMed DOI
  106. Ma,Y.H., Xu,B., Cui,J.R., Yang,Z.J., Zhang,L.R. and Zhang,L.H.
    [Design, synthesis and biological assay of novel tripeptidic tetrazoles as inhibitors of 20S proteasome]
    Yao Xue Xue Bao47, 472-478. PubMed  Europe PubMed  I
  107. Pereira,A.R., Kale,A.J., Fenley,A.T., Byrum,T., Debonsi,H.M., Gilson,M.K., Valeriote,F.A., Moore,B.S. and Gerwick,W.H.
    The carmaphycins: new proteasome inhibitors exhibiting an alpha,beta-epoxyketone warhead from a marine cyanobacterium
    Chembiochem13, 810-817. PubMed  Europe PubMed DOI  I
  108. van der Linden,W.A., Willems,L.I., Shabaneh,T.B., Li,N., Ruben,M., Florea,B.I., van der Marel,G.A., Kaiser,M., Kisselev,A.F. and Overkleeft,H.S.
    Discovery of a potent and highly beta1 specific proteasome inhibitor from a focused library of urea-containing peptide vinyl sulfones and peptide epoxyketones
    Org Biomol Chem10, 181-194. PubMed  Europe PubMed DOI  I
  109. Verani,C.N.
    Metal complexes as inhibitors of the 26S proteasome in tumor cells
    J Inorg Biochem106, 59-67. PubMed  Europe PubMed DOI  I
  110. Verbrugge,S.E., Assaraf,Y.G., Dijkmans,B.A., Scheffer,G.L., Al,M., den Uyl,D., Oerlemans,R., Chan,E.T., Kirk,C.J., Peters,G.J., van der Heijden,J.W., de Gruijl,T.D., Scheper,R.J. and Jansen,G.
    Inactivating PSMB5 mutations and P-glycoprotein (multidrug resistance-associated protein/ATP-binding cassette B1) mediate resistance to proteasome inhibitors: ex vivo efficacy of (immuno)proteasome inhibitors in mononuclear blood cells from patients with rheumatoid arthritis
    J Pharmacol Exp Ther341, 174-182. PubMed  Europe PubMed DOI  I
  111. 2011
  112. Ettari,R., Bonaccorso,C., Micale,N., Heindl,C., Schirmeister,T., Calabro,M.L., Grasso,S. and Zappala,M.
    Development of novel peptidomimetics containing a vinyl sulfone moiety as proteasome inhibitors
    ChemMedChem6, 1228-1237. PubMed  Europe PubMed DOI  I
  113. Keyomarsi,K., Efuet,E.T. and Bui,T.N.
    Semi-high throughput method of measuring proteasome inhibition in vitro and in cultured cells
    Cell Biol Toxicol27, 123-131. PubMed  Europe PubMed DOI  A
  114. Liu,J., Zhang,H., Xiao,Z., Wang,F., Wang,X. and Wang,Y.
    Combined 3D-QSAR, molecular docking and molecular dynamics study on derivatives of peptide epoxyketone and tyropeptin-boronic acid as inhibitors against the beta5 subunit of human 20S proteasome
    Int J Mol Sci12, 1807-1835. PubMed  Europe PubMed DOI  I
  115. Qian,K., Kim,S.Y., Hung,H.Y., Huang,L., Chen,C.H. and Lee,K.H.
    New betulinic acid derivatives as potent proteasome inhibitors
    Bioorg Med Chem Lett21, 5944-5947. PubMed  Europe PubMed DOI  I
  116. Sacco,A., Aujay,M., Morgan,B., Azab,A.K., Maiso,P., Liu,Y., Zhang,Y., Azab,F., Ngo,H.T., Issa,G.C., Quang,P., Roccaro,A.M. and Ghobrial,I.M.
    Carfilzomib-dependent selective inhibition of the chymotrypsin-like activity of the proteasome leads to antitumor activity in Waldenstrom's macroglobulinemia
    Clin Cancer Res17, 1753-1764. PubMed  Europe PubMed DOI  I
  117. 2010
  118. Blackburn,C., Gigstad,K.M., Hales,P., Garcia,K., Jones,M., Bruzzese,F.J., Barrett,C., Liu,J.X., Soucy,T.A., Sappal,D.S., Bump,N., Olhava,E.J., Fleming,P., Dick,L.R., Tsu,C., Sintchak,M.D. and Blank,J.L.
    Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit
    Biochem J430, 461-476. PubMed  Europe PubMed DOI  S  I
  119. Blackburn,C., Barrett,C., Blank,J.L., Bruzzese,F.J., Bump,N., Dick,L.R., Fleming,P., Garcia,K., Hales,P., Hu,Z., Jones,M., Liu,J.X., Sappal,D.S., Sintchak,M.D., Tsu,C. and Gigstad,K.M.
    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 Lett20, 6581-6586. PubMed  Europe PubMed DOI  I
  120. Geurink,P.P., Florea,B.I., van der Marel,G.A., Kessler,B.M. and Overkleeft,H.S.
    Probing the proteasome cavity in three steps: bio-orthogonal photo-reactive suicide substrates
    Chem Commun (Camb)46, 9052-9054. PubMed  Europe PubMed DOI
  121. Geurink,P.P., Liu,N., Spaans,M.P., Downey,S.L., van den Nieuwendijk,A.M., van der Marel,G.A., Kisselev,A.F., Florea,B.I. and Overkleeft,H.S.
    Incorporation of fluorinated phenylalanine generates highly specific inhibitor of proteasome's chymotrypsin-like sites
    J Med Chem53, 2319-2323. PubMed  Europe PubMed DOI  I
  122. Lawrence,H.R., Kazi,A., Luo,Y., Kendig,R., Ge,Y., Jain,S., Daniel,K., Santiago,D., Guida,W.C. and Sebti,S.M.
    Synthesis and biological evaluation of naphthoquinone analogs as a novel class of proteasome inhibitors
    Bioorg Med Chem18, 5576-5592. PubMed  Europe PubMed DOI  I
  123. Liggett,A., Crawford,L.J., Walker,B., Morris,T.C. and Irvine,A.E.
    Methods for measuring proteasome activity: current limitations and future developments
    Leuk Res34, 1403-1409. PubMed  Europe PubMed DOI  A
  124. Roccaro,A.M., Sacco,A., Aujay,M., Ngo,H.T., Azab,A.K., Azab,F., Quang,P., Maiso,P., Runnels,J., Anderson,K.C., Demo,S. and Ghobrial,I.M.
    Selective inhibition of chymotrypsin-like activity of the immunoproteasome and constitutive proteasome in Waldenstrom macroglobulinemia
    Blood115, 4051-4060. PubMed  Europe PubMed DOI  I
  125. Screen,M., Britton,M., Downey,S.L., Verdoes,M., Voges,M.J., Blom,A.E., Geurink,P.P., Risseeuw,M.D., Florea,B.I., van der Linden,W.A., Pletnev,A.A., Overkleeft,H.S. and Kisselev,A.F.
    Nature of pharmacophore influences active site specificity of proteasome inhibitors
    J Biol Chem285, 40125-40134. PubMed  Europe PubMed DOI  I
  126. Shi,G., Sun,Q., Yang,H., Dou,Q.P., Deng,Q., Wang,H. and Zhong,G.
    Molecular modeling for the interaction between proteasome beta 5 subunit and organotin compounds
    Sci China Chem53, 2387-2393. DOI  I
  127. Tsukamoto,S., Yamanokuchi,R., Yoshitomi,M., Sato,K., Ikeda,T., Rotinsulu,H., Mangindaan,R.E., de Voogd,N.J., Van Soest,R.W. and Yokosawa,H.
    Aaptamine, an alkaloid from the sponge Aaptos suberitoides, functions as a proteasome inhibitor
    Bioorg Med Chem Lett20, 3341-3343. PubMed  Europe PubMed DOI  I
  128. Urru,S.A., Veglianese,P., De Luigi,A., Fumagalli,E., Erba,E., Gonella Diaza,R., Carra,A., Davoli,E., Borsello,T., Forloni,G., Pengo,N., Monzani,E., Cascio,P., Cenci,S., Sitia,R. and Salmona,M.
    A new fluorogenic peptide determines proteasome activity in single cells
    J Med Chem53, 7452-7460. PubMed  Europe PubMed DOI  A  L
  129. Wakata,A., Lee,H.M., Rommel,P., Toutchkine,A., Schmidt,M. and Lawrence,D.S.
    Simultaneous fluorescent monitoring of proteasomal subunit catalysis
    J Am Chem Soc132, 1578-1582. PubMed  Europe PubMed DOI  A
  130. Wu,Y.X. and Fang,X.
    Apigenin, chrysin, and luteolin selectively inhibit chymotrypsin-like and trypsin-like proteasome catalytic activities in tumor cells
    Planta Med76, 128-132. PubMed  Europe PubMed DOI  I
  131. 2009
  132. Britton,M., Lucas,M.M., Downey,S.L., Screen,M., Pletnev,A.A., Verdoes,M., Tokhunts,R.A., Amir,O., Goddard,A.L., Pelphrey,P.M., Wright,D.L., Overkleeft,H.S. and Kisselev,A.F.
    Selective inhibitor of proteasome's caspase-like sites sensitizes cells to specific inhibition of chymotrypsin-like sites
    Chem Biol16, 1278-1289. PubMed  Europe PubMed DOI  I
  133. Kazi,A., Lawrence,H., Guida,W.C., McLaughlin,M.L., Springett,G.M., Berndt,N., Yip,R.M. and Sebti,S.M.
    Discovery of a novel proteasome inhibitor selective for cancer cells over non-transformed cells
    Cell Cycle8, 1940-1951. PubMed  Europe PubMed  I
  134. Moravec,R.A., O'Brien,M.A., Daily,W.J., Scurria,M.A., Bernad,L. and Riss,T.L.
    Cell-based bioluminescent assays for all three proteasome activities in a homogeneous format
    Anal Biochem387, 294-302. PubMed  Europe PubMed DOI  A
  135. Parlati,F., Lee,S.J., Aujay,M., Suzuki,E., Levitsky,K., Lorens,J.B., Micklem,D.R., Ruurs,P., Sylvain,C., Lu,Y., Shenk,K.D. and Bennett,M.K.
    Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome
    Blood114, 3439-3447. PubMed  Europe PubMed DOI  I
  136. Zhou,H.J., Aujay,M.A., Bennett,M.K., Dajee,M., Demo,S.D., Fang,Y., Ho,M.N., Jiang,J., Kirk,C.J., Laidig,G.J., Lewis,E.R., Lu,Y., Muchamuel,T., Parlati,F., Ring,E., Shenk,K.D., Shields,J., Shwonek,P.J., Stanton,T., Sun,C.M., Sylvain,C., Woo,T.M. and Yang,J.
    Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047)
    J Med Chem52, 3028-3038. PubMed  Europe PubMed DOI  I
  137. 2008
  138. Fuchs,D., Berges,C., Opelz,G., Daniel,V. and Naujokat,C.
    Increased expression and altered subunit composition of proteasomes induced by continuous proteasome inhibition establish apoptosis resistance and hyperproliferation of Burkitt lymphoma cells
    J Cell Biochem103, 270-283. PubMed  Europe PubMed DOI  I
  139. Leban,J., Blisse,M., Krauss,B., Rath,S., Baumgartner,R. and Seifert,M.H.
    Proteasome inhibition by peptide-semicarbazones
    Bioorg Med Chem16, 4579-4588. PubMed  Europe PubMed DOI  I
  140. Lu,S., Yang,J., Song,X., Gong,S., Zhou,H., Guo,L., Song,N., Bao,X., Chen,P. and Wang,J.
    Point mutation of the proteasome beta5 subunit gene is an important mechanism of bortezomib resistance in bortezomib-selected variants of jurkat T cell lymphoblastic lymphoma/leukemia line
    J Pharmacol Exp Ther326, 423-431. PubMed  Europe PubMed DOI  M  I
  141. Oerlemans,R., Franke,N.E., Assaraf,Y.G., Cloos,J., van Zantwijk,I., Berkers,C.R., Scheffer,G.L., Debipersad,K., Vojtekova,K., Lemos,C., van der Heijden,J.W., Ylstra,B., Peters,G.J., Kaspers,G.L., Dijkmans,B.A., Scheper,R.J. and Jansen,G.
    Molecular basis of bortezomib resistance: proteasome subunit beta5 (PSMB5) gene mutation and overexpression of PSMB5 protein
    Blood112, 2489-2499. PubMed  Europe PubMed DOI  M  I
  142. Uttenweiler-Joseph,S., Claverol,S., Sylvius,L., Bousquet-Dubouch,M.P., Burlet-Schiltz,O. and Monsarrat,B.
    Toward a full characterization of the human 20S proteasome subunits and their isoforms by a combination of proteomic approaches
    Methods Mol Biol484, 111-130. PubMed  Europe PubMed DOI
  143. 2007
  144. Huang,L., Ho,P. and Chen,C.H.
    Activation and inhibition of the proteasome by betulinic acid and its derivatives
    FEBS Lett581, 4955-4959. PubMed  Europe PubMed DOI  I
  145. Imbach,P., Lang,M., Garcia-Echeverria,C., Guagnano,V., Noorani,M., Roesel,J., Bitsch,F., Rihs,G. and Furet,P.
    Novel beta-lactam derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome
    Bioorg Med Chem Lett17, 358-362. PubMed  Europe PubMed DOI  I
  146. Miller,C.P., Ban,K., Dujka,M.E., McConkey,D.J., Munsell,M., Palladino,M. and Chandra,J.
    NPI-0052, a novel proteasome inhibitor, induces caspase-8 and ROS-dependent apoptosis alone and in combination with HDAC inhibitors in leukemia cells
    Blood110, 267-277. PubMed  Europe PubMed DOI  I
  147. Naujokat,C., Berges,C., Hoh,A., Wieczorek,H., Fuchs,D., Ovens,J., Miltz,M., Sadeghi,M., Opelz,G. and Daniel,V.
    Proteasomal chymotrypsin-like peptidase activity is required for essential functions of human monocyte-derived dendritic cells
    Immunology120, 120-132. PubMed  Europe PubMed DOI
  148. Pang,H., Chen,D., Cui,Q.C. and Dou,Q.P.
    Sodium diethyldithiocarbamate, an AIDS progression inhibitor and a copper-binding compound, has proteasome-inhibitory and apoptosis-inducing activities in cancer cells
    Int J Mol Med19, 809-816. PubMed  Europe PubMed  I
  149. 2006
  150. [YEAR:15-6-2006]Crawford,L.J., Walker,B., Ovaa,H., Chauhan,D., Anderson,K.C., Morris,T.C. and Irvine,A.E.
    Comparative selectivity and specificity of the proteasome inhibitors BzLLLCOCHO, PS-341, and MG-132
    Cancer Res66, 6379-6386. PubMed  Europe PubMed DOI  I
  151. [YEAR:2-2-2006]Kisselev,A.F., Callard,A. and Goldberg,A.L.
    Importance of the different proteolytic sites of the proteasome and the efficacy of inhibitors varies with the protein substrate
    J Biol Chem281, 8582-8590. PubMed  Europe PubMed DOI
  152. [YEAR:18-5-2006]Rydzewski,R.M., Burrill,L., Mendonca,R., Palmer,J.T., Rice,M., Tahilramani,R., Bass,K.E., Leung,L., Gjerstad,E., Janc,J.W. and Pan,L.
    Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors
    J Med Chem49, 2953-2968. PubMed  Europe PubMed DOI  I
  153. 2005
  154. Bos,D.H.
    Natural selection during functional divergence to LMP7 and proteasome subunit X (PSMB5) following gene duplication
    J Mol Evol60, 221-228. PubMed  Europe PubMed DOI
  155. [YEAR:9-6-2005]Braun,H.A., Umbreen,S., Groll,M., Kuckelkorn,U., Mlynarczuk,I., Wigand,M.E., Drung,I., Kloetzel,P.M. and Schmidt,B.
    Tripeptide mimetics inhibit the 20 S proteasome by covalent bonding to the active threonines
    J Biol Chem280, 28394-28401. PubMed  Europe PubMed DOI  I
  156. [YEAR:20-1-2005]Chondrogianni,N., Tzavelas,C., Pemberton,A.J., Nezis,I.P., Rivett,A.J. and Gonos,E.S.
    Overexpression of proteasome beta5 assembled subunit increases the amount of proteasome and confers ameliorated response to oxidative stress and higher survival rates
    J Biol Chem280, 11840-11850. PubMed  Europe PubMed DOI
  157. Daniel,K.G., Chen,D., Orlu,S., Cui,Q.C., Miller,F.R. and Dou,Q.P.
    Clioquinol and pyrrolidine dithiocarbamate complex with copper to form proteasome inhibitors and apoptosis inducers in human breast cancer cells
    Breast Cancer Res7, R897-R908. PubMed  Europe PubMed DOI  I
  158. Gaczynska,M. and Osmulski,P.A.
    Small-molecule inhibitors of proteasome activity
    Methods Mol Biol301, 3-22. PubMed  Europe PubMed DOI  I
  159. Kisselev,A.F. and Goldberg,A.L.
    Monitoring activity and inhibition of 26S proteasomes with fluorogenic peptide substrates
    Methods Enzymol398, 364-378. PubMed  Europe PubMed DOI
  160. Momose,I., Umezawa,Y., Hirosawa,S., Iijima,M., Iinuma,H. and Ikeda,D.
    Synthesis and activity of tyropeptin A derivatives as potent and selective inhibitors of mammalian 20S proteasome
    Biosci Biotechnol Biochem69, 1733-1742. PubMed  Europe PubMed DOI  I
  161. [YEAR:1-4-2005]Momose,I., Umezawa,Y., Hirosawa,S., Iinuma,H. and Ikeda,D.
    Structure-based design of derivatives of tyropeptin A as the potent and selective inhibitors of mammalian 20S proteasome
    Bioorg Med Chem Lett15, 1867-1871. PubMed  Europe PubMed DOI  I
  162. 2004
  163. Daniel,K.G., Gupta,P., Harbach,R.H., Guida,W.C. and Dou,Q.P.
    Organic copper complexes as a new class of proteasome inhibitors and apoptosis inducers in human cancer cells
    Biochem Pharmacol67, 1139-1151. PubMed  Europe PubMed DOI  I
  164. [YEAR:29-11-2004]Groll,M. and Huber,R.
    Inhibitors of the eukaryotic 20S proteasome core particle: a structural approach
    Biochim Biophys Acta1695, 33-44. PubMed  Europe PubMed DOI  V  I
  165. Seemuller,E., Dolenc,I. and Lupas,A.
    Eukaryotic 20S proteasome
    [ISSN:0-12-079610-4]2, 2068-2077.  V
  166. 2003
  167. [YEAR:18-4-2003]Holtz,K.M., Rice,A.M. and Sartorelli,A.C.
    Lithium chloride inactivates the 20S proteasome from WEHI-3B D+ leukemia cells
    Biochem Biophys Res Commun303, 1058-1064. PubMed  Europe PubMed DOI
  168. Kretz-Remy,C. and Arrigo,A.P.
    Modulation of the chymotrypsin-like activity of the 20S proteasome by intracellular redox status: effects of glutathione peroxidase-1 overexpression and antioxidant drugs
    Biol Chem384, 589-595. PubMed  Europe PubMed DOI
  169. 2002
  170. [YEAR:1-12-2002]Cardozo,C. and Michaud,C.
    Proteasome-mediated degradation of tau proteins occurs independently of the chymotrypsin-like activity by a nonprocessive pathway
    Arch Biochem Biophys408, 103-110. PubMed  Europe PubMed DOI
  171. [YEAR:20-5-2002]Furet,P., Imbach,P., Fuerst,P., Lang,M., Noorani,M., Zimmermann,J. and Garcia-Echeverria,C.
    Structure-based optimisation of 2-aminobenzylstatine derivatives: potent and selective inhibitors of the chymotrypsin-Like activity of the human 20S proteasome
    Bioorg Med Chem Lett12, 1331-1334. PubMed  Europe PubMed DOI  I
  172. Unno,M., Mizushima,T., Morimoto,Y., Tomisugi,Y., Tanaka,K., Yasuoka,N. and Tsukihara,T.
    The structure of the mammalian 20S proteasome at 2.75 A resolution
    Structure10, 609-618. PubMed  Europe PubMed DOI  S
  173. 2001
  174. [YEAR:21-5-2001]Furet,P., Imbach,P., Furst,P., Lang,M., Noorani,M., Zimmermann,J. and Garcia-Echeverria,C.
    Modeling of the binding mode of a non-covalent inhibitor of the 20S proteasome. Application to structure-based analogue design
    Bioorg Med Chem Lett11, 1321-1324. PubMed  Europe PubMed DOI  I
  175. [YEAR:21-5-2001]Garcia-Echevarria,C., Imbach,P., France,D., Furst,P., Lang,M., Noorani,M., Scholz,D., Zimmermann,J. and Furet,P.
    A new structural class of selective and non-covalent inhibitors of the chymotrypsin-like activity of the 20S proteasome
    Bioorg Med Chem Lett11, 1317-1319. PubMed  Europe PubMed DOI  I
  176. Kessler,B.M., Tortorella,D., Altun,M., Kisselev,A.F., Fiebiger,E., Hekking,B.G., Ploegh,H.L. and Overkleeft,H.S.
    Extended peptide-based inhibitors efficiently target the proteasome and reveal overlapping specificities of the catalytic beta-subunits
    Chem Biol8, 913-929. PubMed  Europe PubMed DOI  I
  177. [YEAR:13-3-2001]Nazif,T. and Bogyo,M.
    Global analysis of proteasomal substrate specificity using positional-scanning libraries of covalent inhibitors
    Proc Natl Acad Sci U S A98, 2967-2972. PubMed  Europe PubMed DOI  I
  178. [YEAR:6-11-2001]Oberdorf,J., Carlson,E.J. and Skach,W.R.
    Redundancy of mammalian proteasome beta subunit function during endoplasmic reticulum associated degradation
    Biochemistry40, 13397-13405. PubMed  Europe PubMed DOI
  179. 2000
  180. [YEAR:19-5-2000]Kisselev,A.F., Songyang,Z. and Goldberg,A.L.
    Why does threonine, and not serine, function as the active site nucleophile in proteasomes?
    J Biol Chem275, 14831-14837. PubMed  Europe PubMed DOI  I
  181. Koguchi,Y., Kohno,J., Nishio,M., Takahashi,K., Okuda,T., Ohnuki,T. and Komatsubara,S.
    TMC-95A, B, C, and D, novel proteasome inhibitors produced by Apiospora montagnei Sacc. TC 1093. Taxonomy, production, isolation, and biological activities
    J Antibiot (Tokyo)53, 105-109. PubMed  Europe PubMed  I
  182. [YEAR:21-7-2000]Schmidtke,G., Emch,S., Groettrup,M. and Holzhutter,H.G.
    Evidence for the existence of a non-catalytic modifier site of peptide hydrolysis by the 20 S proteasome
    J Biol Chem275, 22056-22063. PubMed  Europe PubMed DOI  I
  183. 1999
  184. [YEAR:1-7-1999]Arendt,C.S. and Hochstrasser,M.
    Eukaryotic 20S proteasome catalytic subunit propeptides prevent active site inactivation by N-terminal acetylation and promote particle assembly
    EMBO J18, 3575-3585. PubMed  Europe PubMed DOI
  185. Elofsson,M., Splittgerber,U., Myung,J., Mohan,R. and Crews,C.M.
    Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide alpha',beta'-epoxyketones
    Chem Biol6, 811-822. PubMed  Europe PubMed DOI  I
  186. [YEAR:27-8-1999]Jager,S., Groll,M., Huber,R., Wolf,D.H. and Heinemeyer,W.
    Proteasome beta-type subunits: Unequal roles of propeptides in core particle maturation and a hierarchy of active site function
    J Mol Biol291, 997-1013. PubMed  Europe PubMed DOI
  187. [YEAR:1-9-1999]Murray,B.W., Sultmann,H. and Klein,J.
    Analysis of a 26-kb region linked to the Mhc in zebrafish: Genomic organization of the proteasome component beta/transporter associated with antigen processing-2 gene cluster and identification of five new proteasome beta subunit genes
    J Immunol163, 2657-2666. PubMed  Europe PubMed
  188. 1998
  189. [YEAR:2-10-1998]Dick,T.P., Nussbaum,A.K., Deeg,M., Heinemeyer,W., Groll,M., Schirle,M., Keilholz,W., Stevanovic,S., Wolf,D.H., Huber,R., Rammensee,H.G. and Schild,H.
    Contribution of proteasomal beta-subunits to the cleavage of peptide substrates analyzed with yeast mutants
    J Biol Chem273, 25637-25646. PubMed  Europe PubMed DOI
  190. [YEAR:17-2-1998]Lynas,J.F., Harriott,P., Healy,A., McKervey,M.A. and Walker,B.
    Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl alpha-keto aldehydes (glyoxals)
    Bioorg Med Chem Lett8, 373-378. PubMed  Europe PubMed DOI  I
  191. [YEAR:26-5-1998]McCormack,T.A., Cruikshank,A.A., Grenier,L., Melandri,F.D., Nunes,S.L., Plamondon,L., Stein,R.L. and Dick,L.R.
    Kinetic studies of the branched chain amino acid preferring peptidase activity of the 20S proteasome: development of a continuous assay and inhibition by tripeptide aldehydes and clasto-lactacystin beta-lactone
    Biochemistry37, 7792-7800. PubMed  Europe PubMed DOI  A  I
  192. [YEAR:13-10-1998]Nussbaum,A.K., Dick,T.P., Keilholz,W., Schirle,M., Stevanovic,S., Dietz,K., Heinemeyer,W., Groll,M., Wolf,D.H., Huber,R., Rammensee,H.G. and Schild,H.
    Cleavage motifs of the yeast 20S proteasome beta subunits deduced from digests of enolase 1
    Proc Natl Acad Sci U S A95, 12504-12509. PubMed  Europe PubMed
  193. Yamada,S., Sato,K., Yamada,J., Yasutomi,M., Tokumoto,T. and Ishikawa,K.
    Activation of the 20S proteasome of Xenopus oocytes by SDS: evidence for the substrate-induced conformational change characteristic of trypsin-like peptidase
    Zoolog Sci15, 353-357. PubMed  Europe PubMed DOI
  194. 1997
  195. Eleuteri,A.M., Kohanski,R.A., Cardozo,C. and Orlowski,M.
    Bovine spleen multicatalytic proteinase complex (proteasome). Replacement of X, Y, and Z subunits by LMP7, LMP2, and MECL1 and changes in properties and specificity
    J Biol Chem272, 11824-11831. PubMed  Europe PubMed DOI
  196. [YEAR:3-4-1997]Groll,M., Ditzel,L., Lowe,J., Stock,D., Bochtler,M., Bartunik,H.D. and Huber,R.
    Structure of 20S proteasome from yeast at 2.4 A resolution
    Nature386, 463-471. PubMed  Europe PubMed DOI  S
  197. 1996
  198. [YEAR:20-9-1996]Chen,P. and Hochstrasser,M.
    Autocatalytic subunit processing couples active site formation in the 20S proteasome to completion of assembly
    Cell86, 961-972. PubMed  Europe PubMed DOI
  199. Coux,O., Tanaka,K. and Goldberg,A.L.
    Structure and functions of the 20S and 26S proteasomes
    Annu Rev Biochem65, 801-847. PubMed  Europe PubMed DOI
  200. Tsubuki,S., Saito,Y., Tomioka,M., Ito,H. and Kawashima,S.
    Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine
    J Biochem119, 572-576. PubMed  Europe PubMed  I
  201. 1994
  202. Khan,M.T., Wang,K., Auland,M.E., Kable,E.P. and Roufogalis,B.D.
    Membrane-bound high molecular mass proteinases from human erythrocytes
    Biochim Biophys Acta1209, 215-221. PubMed  Europe PubMed  I
  203. 1993
  204. [YEAR:5-3-1993]Heinemeyer,W., Gruhler,A., Mohrle,V., Mahe,Y. and Wolf,D.H.
    PRE2, highly homologous to the human major histocompatibility complex-linked RING10 gene, codes for a yeast proteasome subunit necessary for chrymotryptic activity and degradation of ubiquitinated proteins
    J Biol Chem268, 5115-5120. PubMed  Europe PubMed
  205. 1992
  206. Djaballah,H., Harness,J.A., Savory,P.J. and Rivett,A.J.
    Use of serine-protease inhibitors as probes for the different proteolytic activities of the rat liver multicatalytic proteinase complex
    Eur J Biochem209, 629-634. PubMed  Europe PubMed DOI
  207. 1989
  208. Orlowski,M. and Michaud,C.
    Pituitary multicatalytic proteinase complex. Specificity of components and aspects of proteolytic activity
    Biochemistry28, 9270-9278. PubMed  Europe PubMed DOI  I