The Proteasome in Modern Drug Discovery: Second Life of a Highly Valuable Drug Target

The ubiquitin code

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STRUCTURE AND FUNCTIONS OF THE 20S AND 26S PROTEASOMES

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Renal and Extrarenal Effects of Gum Arabic (Acacia Senegal) - What Can be Learned from Animal Experiments?

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Structure of 20S proteasome from yeast at 2.4Å resolution

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Recognition and Processing of Ubiquitin-Protein Conjugates by the Proteasome

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Crystal Structure of the 20 S Proteasome from the Archaeon T. acidophilum at 3.4 Å Resolution

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Induced protein degradation: an emerging drug discovery paradigm

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Ubiquitin: structures, functions, mechanisms

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The proteasome: a suitable antineoplastic target

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The increasing complexity of the ubiquitin code

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Proteasome inhibitors in cancer therapy

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Role of Rpn11 Metalloprotease in Deubiquitination and Degradation by the 26 S Proteasome

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A Subcomplex of the Proteasome Regulatory Particle Required for Ubiquitin-Conjugate Degradation and Related to the COP9-Signalosome and eIF3

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Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma

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Phase I Trial of the Proteasome Inhibitor PS-341 in Patients With Refractory Hematologic Malignancies

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A cryptic protease couples deubiquitination and degradation by the proteasome

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Antitumor Activity of PR-171, a Novel Irreversible Inhibitor of the Proteasome

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A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis

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Regulation of CD8 + T Cell Development by Thymus-Specific Proteasomes

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Proteasome Inhibitors in Cancer Therapy: Lessons from the First Decade

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Proteasome Inhibitors: An Expanding Army Attacking a Unique Target

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Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical Models of Human Cancer

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Proteasome inhibitors in multiple myeloma: 10 years later

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Immuno- and Constitutive Proteasome Crystal Structures Reveal Differences in Substrate and Inhibitor Specificity

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Targeted Protein Degradation: from Chemical Biology to Drug Discovery

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The proteasomal system

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Mobilizing the proteolytic machine: cell biological roles of proteasome activators and inhibitors

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Proteasomes in immune cells: more than peptide producers?

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United States Food and Drug Administration Approval Summary: Bortezomib for the Treatment of Progressive Multiple Myeloma after One Prior Therapy

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Bortezomib for the Treatment of Mantle Cell Lymphoma

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Crystal Structures of Salinosporamide A (NPI-0052) and B (NPI-0047) in Complex with the 20S Proteasome Reveal Important Consequences of β-Lactone Ring Opening and a Mechanism for Irreversible Binding

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Crystal Structure of Epoxomicin:20S Proteasome Reveals a Molecular Basis for Selectivity of α‘,β‘-Epoxyketone Proteasome Inhibitors

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Proteasome inhibitors in cancer therapy

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Waste disposal—An attractive strategy for cancer therapy

Salami, J., & Crews, C. M. (2017) · Science · doi:10.1126/science.aam7340 · Cited by 279 · see citing works

Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy

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Design and Synthesis of an Orally Bioavailable and Selective Peptide Epoxyketone Proteasome Inhibitor (PR-047)

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Crystal structure of epoxomicin:20s proteasome reveals a molecular basis for selectivity of alpha,beta-epoxyketone proteasome inhibitors

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The immunoproteasome in antigen processing and other immunological functions

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Apoptosis induction resulting from proteasome inhibition

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Regulated protein turnover: snapshots of the proteasome in action

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Structure- and function-based design of Plasmodium-selective proteasome inhibitors

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Structural Biology of the Proteasome

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Inhibition of the chymotrypsin-like activity of the pituitary multicatalytic proteinase complex

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A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma

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Targeted inhibition of the immunoproteasome is a potent strategy against models of multiple myeloma that overcomes resistance to conventional drugs and nonspecific proteasome inhibitors

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Lactacystin, a Specific Inhibitor of the Proteasome, Induces Apoptosis in Human Monoblast U937 Cells

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The immunoproteasome and viral infection: a complex regulator of inflammation

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Inhibitors for the Immuno‐ and Constitutive Proteasome: Current and Future Trends in Drug Development

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Role of Proteasomes in Cellular Regulation

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Proteasome Inhibitors Block Development of Plasmodium spp

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Proteasome inhibitors

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Crystal Structure of the Human 20S Proteasome in Complex with Carfilzomib

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Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11

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Proteasome Activation by Small Molecules

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The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects

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Thymoproteasome: probable role in generating positively selecting peptides

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Pharmacokinetics, Pharmacodynamics, Metabolism, Distribution, and Excretion of Carfilzomib in Rats

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Comprehensive study of proteasome inhibitors against Plasmodium falciparum laboratory strains and field isolates from Gabon

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Assembly of the 20S proteasome

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Inhibition of the proteolytic activity of the multicatalytic proteinase complex (proteasome) by substrate-related peptidyl aldehydes.

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A Set of Activity‐Based Probes to Visualize Human (Immuno)proteasome Activities

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Structure-Based Design of β1i or β5i Specific Inhibitors of Human Immunoproteasomes

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The Proteasome Inhibitor Epoxomicin Has Potent Plasmodium falciparum Gametocytocidal Activity

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Selective Inhibition of the Immunoproteasome by Ligand‐Induced Crosslinking of the Active Site

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The ubiquitin–proteasome system: opportunities for therapeutic intervention in solid tumors

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Immunoproteasomes at the interface of innate and adaptive immune responses: two faces of one enzyme

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Synthesis and Pharmacology of Proteasome Inhibitors

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Validation of the Proteasome as a Therapeutic Target in Plasmodium Using an Epoxyketone Inhibitor with Parasite-Specific Toxicity

Li, H., Ponder, E. L., Verdoes, M., Ásbjörnsdóttir, K., Deu, E., Edgington‐Mitchell, L. E., Lee, J. T., Kirk, C. J., Demo, S. D., Williamson, K. C., et al. (2012) · Chemistry & Biology · doi:10.1016/j.chembiol.2012.09.019 · Cited by 89 · see citing works

The proteasome of malaria parasites: A multi-stage drug target for chemotherapeutic intervention?

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Discovery of an Inhibitor of the Proteasome Subunit Rpn11

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Bortezomib-Resistant Mutant Proteasomes: Structural and Biochemical Evaluation with Carfilzomib and ONX 0914

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Inhibition and deficiency of the immunoproteasome subunit LMP7 suppress the development and progression of colorectal carcinoma in mice

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Comparison of biochemical and biological effects of ML858 (salinosporamide A) and bortezomib

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Identification of Potent and Selective Non-covalent Inhibitors of the Plasmodium falciparum Proteasome

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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. A., Warrier, T., Vaubourgeix, J., Blackburn, C., Gigstad, K. M., Sintchak, M. D., Dick, L. R., & Nathan, C. (2013) · Journal of the American Chemical Society · doi:10.1021/ja400021x · Cited by 59 · see citing works

Assessing Subunit Dependency of the Plasmodium Proteasome Using Small Molecule Inhibitors and Active Site Probes

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Structure of the Blm10–20 S Proteasome Complex by Cryo-electron Microscopy. Insights into the Mechanism of Activation of Mature Yeast Proteasomes

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Nonpeptidic Selective Inhibitors of the Chymotrypsin‐Like (β5 i) Subunit of the Immunoproteasome

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Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome

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Emerging role of immunoproteasomes in pathophysiology

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Selective Inhibition of the Immunoproteasome by Structure‐Based Targeting of a Non‐catalytic Cysteine

Dubiella, C., Baur, R., Cui, H., Huber, E. M., & Groll, M. (2015) · Angewandte Chemie International Edition · doi:10.1002/anie.201506631 · Cited by 28 · see citing works

Structural Elucidation of a Nonpeptidic Inhibitor Specific for the Human Immunoproteasome

Cui, H., Baur, R., Chapelain, C. L., Dubiella, C., Heinemeyer, W., Huber, E. M., & Groll, M. (2017) · ChemBioChem · doi:10.1002/cbic.201700021 · Cited by 21 · see citing works

The emerging role of carfilzomib combination therapy in the management of multiple myeloma

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A Minimal β‐Lactone Fragment for Selective β5c or β5i Proteasome Inhibitors

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Rational Design of Proteasome Inhibitors as Antimalarial Drugs

Chapelain, C. L., & Groll, M. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201602519 · Cited by 13 · see citing works

Advances in covalent drug discovery

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Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology

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Targeting the ubiquitin-proteasome pathway to overcome anti-cancer drug resistance

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Dynamic Regulation of the 26S Proteasome: From Synthesis to Degradation

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From Discovery to Bedside: Targeting the Ubiquitin System

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Expanding the arsenal of E3 ubiquitin ligases for proximity-induced protein degradation

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Proteasome Inhibition Is an Effective Treatment Strategy for Microsporidia Infection in Honey Bees

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