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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Ubiquitin: structures, functions, mechanisms

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Induced protein degradation: an emerging drug discovery paradigm

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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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Proteasome inhibitors in multiple myeloma: 10 years later

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

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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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Proteasome inhibitors in cancer therapy

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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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Waste disposal—An attractive strategy for cancer therapy

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

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

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

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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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Proteasome inhibitors

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

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Thymoproteasome: probable role in generating positively selecting peptides

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

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

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

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The Proteasome Inhibitor Epoxomicin Has Potent Plasmodium falciparum Gametocytocidal Activity

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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

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

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

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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

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

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

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Emerging role of immunoproteasomes in pathophysiology

Kaur, G., & Batra, S. (2016) · Immunology and Cell Biology · doi:10.1038/icb.2016.50 · Cited by 45

Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome

Fan, H., Angelo, N. G., Warren, J. D., Nathan, C., & Lin, G. (2014) · ACS Medicinal Chemistry Letters · doi:10.1021/ml400531d · Cited by 43

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

Structural Elucidation of a Nonpeptidic Inhibitor Specific for the Human Immunoproteasome

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

Moreau, P. (2014) · Expert Review of Hematology · doi:10.1586/17474086.2014.873699 · Cited by 20

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

Groll, M., Korotkov, V. S., Huber, E. M., de Meijere, A., & Ludwig, A. (2015) · Angewandte Chemie International Edition · doi:10.1002/anie.201502931 · Cited by 15

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

Advances in covalent drug discovery

Boike, L., Henning, N. J., & Nomura, D. K. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-022-00542-z · Cited by 823

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

Gehringer, M., & Laufer, S. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01153 · Cited by 772

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

Marshall, R. S., & Vierstra, R. D. (2019) · Frontiers in Molecular Biosciences · doi:10.3389/fmolb.2019.00040 · Cited by 243

From Discovery to Bedside: Targeting the Ubiquitin System

Wertz, I. E., & Wang, X. (2018) · Cell chemical biology · doi:10.1016/j.chembiol.2018.10.022 · Cited by 162

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

Huber, E. M., & Groll, M. (2012) · Angewandte Chemie International Edition · doi:10.1002/anie.201201616 · Cited by 182

Proteasome Inhibitors: Harnessing Proteostasis to Combat Disease

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Computational Approaches for the Discovery of Human Proteasome Inhibitors: An Overview

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Le protéasome, la seconde vie d’une cible thérapeutique validée : aspects structuraux et nouveaux inhibiteurs

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Proteasome Inhibitors: Recent Progress and Future Directions

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