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Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit.

Figure 1
<div class='caption-title'>Synthesis of compound 1</div>
<div class='caption-title'>Synthesis of compound IV</div>
Blackburn C, Gigstad KM, Hales P, Garcia K, Jones M, Bruzzese FJ, Barrett C, Liu JX, Soucy TA, Sappal DS, Bump N, Olhava EJ, Fleming P, Dick LR, Tsu C, Sintchak MD, Blank JL
OpenAccess logo Biochem J 430 461-76 (2010)
Related entries: 3mg4, 3mg6, 3mg7, 3mg8

Cited: 84 times
EuropePMC logo PMID: 20632995

Abstract

The mammalian 26S proteasome is a 2500 kDa multi-catalytic complex involved in intracellular protein degradation. We describe the synthesis and properties of a novel series of non-covalent di-peptide inhibitors of the proteasome based [corrected] on a capped tri-peptide that was first identified by high-throughput screening of a library of approx. 350000 compounds for inhibitors of the ubiquitin-proteasome system in cells. We show that these compounds are entirely selective for the beta5 (chymotrypsin-like) site over the beta1 (caspase-like) and beta2 (trypsin-like) sites of the 20S core particle of the proteasome, and over a panel of less closely related proteases. Compound optimization, guided by X-ray crystallography of the liganded 20S core particle, confirmed their non-covalent binding mode and provided a structural basis for their enhanced in vitro and cellular potencies. We demonstrate that such compounds show low nanomolar IC50 values for the human 20S beta5 site in vitro, and that pharmacological inhibition of this site in cells is sufficient to potently inhibit the degradation of a tetra-ubiquitin-luciferase reporter, activation of NFkappaB (nuclear factor kappaB) in response to TNF-alpha (tumour necrosis factor-alpha) and the proliferation of cancer cells. Finally, we identified capped di-peptides that show differential selectivity for the beta5 site of the constitutively expressed proteasome and immunoproteasome in vitro and in B-cell lymphomas. Collectively, these studies describe the synthesis, activity and binding mode of a new series of non-covalent proteasome inhibitors with unprecedented potency and selectivity for the beta5 site, and which can discriminate between the constitutive proteasome and immunoproteasome in vitro and in cells.

Reviews - 3mg0 mentioned but not cited (1)

  1. Computational Approaches for the Discovery of Human Proteasome Inhibitors: An Overview. Guedes RA, Serra P, Salvador JA, Guedes RC. Molecules 21 E927 (2016)

Articles - 3mg0 mentioned but not cited (3)

  1. Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit. Blackburn C, Gigstad KM, Hales P, Garcia K, Jones M, Bruzzese FJ, Barrett C, Liu JX, Soucy TA, Sappal DS, Bump N, Olhava EJ, Fleming P, Dick LR, Tsu C, Sintchak MD, Blank JL. Biochem J 430 461-476 (2010)
  2. The carmaphycins: new proteasome inhibitors exhibiting an α,β-epoxyketone warhead from a marine cyanobacterium. Pereira AR, Kale AJ, Fenley AT, Byrum T, Debonsi HM, Gilson MK, Valeriote FA, Moore BS, Gerwick WH. Chembiochem 13 810-817 (2012)
  3. New Insights into the Roles of Mg in Improving the Rate Capability and Cycling Stability of O3-NaMn0.48Ni0.2Fe0.3Mg0.02O2 for Sodium-Ion Batteries. Zhang C, Gao R, Zheng L, Hao Y, Liu X. ACS Appl Mater Interfaces 10 10819-10827 (2018)


Reviews citing this publication (21)

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  15. Site-Specific Proteasome Inhibitors. Kisselev AF. Biomolecules 12 54 (2021)
  16. Structure-Driven Developments of 26S Proteasome Inhibitors. Śledź P, Baumeister W. Annu Rev Pharmacol Toxicol 56 191-209 (2016)
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  18. Recent advances in proteasome inhibitor discovery. Pevzner Y, Metcalf R, Kantor M, Sagaro D, Daniel K. Expert Opin Drug Discov 8 537-568 (2013)
  19. Small-Molecule Inhibitors of the Proteasome's Regulatory Particle. Muli CS, Tian W, Trader DJ. Chembiochem 20 1739-1753 (2019)
  20. Pharmacophore modeling technique applied for the discovery of proteasome inhibitors. Pautasso C, Troia R, Genuardi M, Palumbo A. Expert Opin Drug Discov 9 931-943 (2014)
  21. Proteasome Inhibitors in Cancer Therapy and their Relation to Redox Regulation. Sari G, Okat Z, Sahin A, Karademir B. Curr Pharm Des 24 5252-5267 (2018)

Articles citing this publication (59)

  1. Immuno- and constitutive proteasome crystal structures reveal differences in substrate and inhibitor specificity. Huber EM, Basler M, Schwab R, Heinemeyer W, Kirk CJ, Groettrup M, Groll M. Cell 148 727-738 (2012)
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  4. Brief treatment with a highly selective immunoproteasome inhibitor promotes long-term cardiac allograft acceptance in mice. Sula Karreci E, Fan H, Uehara M, Mihali AB, Singh PK, Kurdi AT, Solhjou Z, Riella LV, Ghobrial I, Laragione T, Routray S, Assaker JP, Wang R, Sukenick G, Shi L, Barrat FJ, Nathan CF, Lin G, Azzi J. Proc Natl Acad Sci U S A 113 E8425-E8432 (2016)
  5. N,C-Capped dipeptides with selectivity for mycobacterial proteasome over human proteasomes: role of S3 and S1 binding pockets. Lin G, Chidawanyika T, Tsu C, Warrier T, Vaubourgeix J, Blackburn C, Gigstad K, Sintchak M, Dick L, Nathan C. J Am Chem Soc 135 9968-9971 (2013)
  6. Co-inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity. Basler M, Lindstrom MM, LaStant JJ, Bradshaw JM, Owens TD, Schmidt C, Maurits E, Tsu C, Overkleeft HS, Kirk CJ, Langrish CL, Groettrup M. EMBO Rep 19 e46512 (2018)
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  8. Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome. Xie SC, Gillett DL, Spillman NJ, Tsu C, Luth MR, Ottilie S, Duffy S, Gould AE, Hales P, Seager BA, Charron CL, Bruzzese F, Yang X, Zhao X, Huang SC, Hutton CA, Burrows JN, Winzeler EA, Avery VM, Dick LR, Tilley L. J Med Chem 61 10053-10066 (2018)
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  14. Anti-leukemic activity and mechanisms underlying resistance to the novel immunoproteasome inhibitor PR-924. Niewerth D, van Meerloo J, Jansen G, Assaraf YG, Hendrickx TC, Kirk CJ, Anderl JL, Zweegman S, Kaspers GJ, Cloos J. Biochem Pharmacol 89 43-51 (2014)
  15. Proteasome inhibition mediates p53 reactivation and anti-cancer activity of 6-gingerol in cervical cancer cells. Rastogi N, Duggal S, Singh SK, Porwal K, Srivastava VK, Maurya R, Bhatt ML, Mishra DP. Oncotarget 6 43310-43325 (2015)
  16. Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor. Bhatia S, Krieger V, Groll M, Osko JD, Reßing N, Ahlert H, Borkhardt A, Kurz T, Christianson DW, Hauer J, Hansen FK. J Med Chem 61 10299-10309 (2018)
  17. Immunoproteasome β5i-Selective Dipeptidomimetic Inhibitors. Singh PK, Fan H, Jiang X, Shi L, Nathan CF, Lin G. ChemMedChem 11 2127-2131 (2016)
  18. Pro-inflammatory Cytokines Alter the Immunopeptidome Landscape by Modulation of HLA-B Expression. Javitt A, Barnea E, Kramer MP, Wolf-Levy H, Levin Y, Admon A, Merbl Y. Front Immunol 10 141 (2019)
  19. Amelioration of autoimmunity with an inhibitor selectively targeting all active centres of the immunoproteasome. Basler M, Maurits E, de Bruin G, Koerner J, Overkleeft HS, Groettrup M. Br J Pharmacol 175 38-52 (2018)
  20. Proteasome subunit expression analysis and chemosensitivity in relapsed paediatric acute leukaemia patients receiving bortezomib-containing chemotherapy. Niewerth D, Kaspers GJ, Jansen G, van Meerloo J, Zweegman S, Jenkins G, Whitlock JA, Hunger SP, Lu X, Alonzo TA, van de Ven PM, Horton TM, Cloos J. J Hematol Oncol 9 82 (2016)
  21. A humanized yeast proteasome identifies unique binding modes of inhibitors for the immunosubunit β5i. Huber EM, Heinemeyer W, de Bruin G, Overkleeft HS, Groll M. EMBO J 35 2602-2613 (2016)
  22. An inhibitor of proteasome β2 sites sensitizes myeloma cells to immunoproteasome inhibitors. Downey-Kopyscinski S, Daily EW, Gautier M, Bhatt A, Florea BI, Mitsiades CS, Richardson PG, Driessen C, Overkleeft HS, Kisselev AF. Blood Adv 2 2443-2451 (2018)
  23. Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. Johnson HWB, Anderl JL, Bradley EK, Bui J, Jones J, Arastu-Kapur S, Kelly LM, Lowe E, Moebius DC, Muchamuel T, Kirk C, Wang Z, McMinn D. ACS Med Chem Lett 8 413-417 (2017)
  24. N-(2-{3-[3,5-bis(trifluoromethyl)phenyl]ureido}ethyl)-glycyrrhetinamide (6b): a novel anticancer glycyrrhetinic acid derivative that targets the proteasome and displays anti-kinase activity. Lallemand B, Chaix F, Bury M, Bruyère C, Ghostin J, Becker JP, Delporte C, Gelbcke M, Mathieu V, Dubois J, Prévost M, Jabin I, Kiss R. J Med Chem 54 6501-6513 (2011)
  25. Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors. Ozcan S, Kazi A, Marsilio F, Fang B, Guida WC, Koomen J, Lawrence HR, Sebti SM. J Med Chem 56 3783-3805 (2013)
  26. Selective Inhibition of the Immunoproteasome by Structure-Based Targeting of a Non-catalytic Cysteine. Dubiella C, Baur R, Cui H, Huber EM, Groll M. Angew Chem Int Ed Engl 54 15888-15891 (2015)
  27. Structural Basis for the Species-Selective Binding of N,C-Capped Dipeptides to the Mycobacterium tuberculosis Proteasome. Hsu HC, Singh PK, Fan H, Wang R, Sukenick G, Nathan C, Lin G, Li H. Biochemistry 56 324-333 (2017)
  28. Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti-malaria Activity in Humanized Mice. Zhan W, Zhang H, Ginn J, Leung A, Liu YJ, Michino M, Toita A, Okamoto R, Wong TT, Imaeda T, Hara R, Yukawa T, Chelebieva S, Tumwebaze PK, Lafuente-Monasterio MJ, Martinez-Martinez MS, Vendome J, Beuming T, Sato K, Aso K, Rosenthal PJ, Cooper RA, Meinke PT, Nathan CF, Kirkman LA, Lin G. Angew Chem Int Ed Engl 60 9279-9283 (2021)
  29. Vitamin D analogue TX 527 down-regulates the NF-κB pathway and controls the proliferation of endothelial cells transformed by Kaposi sarcoma herpesvirus. González-Pardo V, Verstuyf A, Boland R, Russo de Boland A. Br J Pharmacol 169 1635-1645 (2013)
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  31. A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor. Hasegawa M, Yasuda Y, Tanaka M, Nakata K, Umeda E, Wang Y, Watanabe C, Uetake S, Kunoh T, Shionyu M, Sasaki R, Shiina I, Mizukami T. Eur J Med Chem 71 290-305 (2014)
  32. Inhibition of autophagy by autophagic inhibitors enhances apoptosis induced by bortezomib in non-small cell lung cancer cells. Wu G, Li H, Ji Z, Jiang X, Lei Y, Sun M. Biotechnol Lett 36 1171-1178 (2014)
  33. PSMB9 codon 60 polymorphisms have no impact on the activity of the immunoproteasome catalytic subunit B1i expressed in multiple types of solid cancer. Park JE, Ao L, Miller Z, Kim K, Wu Y, Jang ER, Lee EY, Kim KB, Lee W. PLoS One 8 e73732 (2013)
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  35. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. Kazi A, Ozcan S, Tecleab A, Sun Y, Lawrence HR, Sebti SM. J Biol Chem 289 11906-11915 (2014)
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  37. Structure-Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides. Zhan W, Singh PK, Ban Y, Qing X, Ah Kioon MD, Fan H, Zhao Q, Wang R, Sukenick G, Salmon J, Warren JD, Ma X, Barrat FJ, Nathan CF, Lin G. J Med Chem 63 13103-13123 (2020)
  38. Biological Evaluation of Naproxen-Dehydrodipeptide Conjugates with Self-Hydrogelation Capacity as Dual LOX/COX Inhibitors. Moreira R, Jervis PJ, Carvalho A, Ferreira PMT, Martins JA, Valentão P, Andrade PB, Perreira DM. Pharmaceutics 12 E122 (2020)
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