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

The ubiquitin code

Komander, D., & Rape, M. (2012) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-060310-170328 · Cited by 3,679

STRUCTURE AND FUNCTIONS OF THE 20S AND 26S PROTEASOMES

Coux, O., Tanaka, K., & Goldberg, A. L. (1996) · Annual Review of Biochemistry · doi:10.1146/annurev.bi.65.070196.004101 · Cited by 2,438

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

Nasir, O. (2013) · Kidney & Blood Pressure Research · doi:10.1159/000350152 · Cited by 2,331

Structure of 20S proteasome from yeast at 2.4Å resolution

Groll, M., Ditzel, L., Löwe, J., Stock, D., Bochtler, M., Bartunik, H. D., & Huber, R. (1997) · Nature · doi:10.1038/386463a0 · Cited by 2,265

Recognition and Processing of Ubiquitin-Protein Conjugates by the Proteasome

Finley, D. (2009) · Annual Review of Biochemistry · doi:10.1146/annurev.biochem.78.081507.101607 · Cited by 1,764

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

Löwe, J., Stock, D., Jap, B. K., Zwickl, P., Baumeister, W. P., & Huber, R. (1995) · Science · doi:10.1126/science.7725097 · Cited by 1,540

Ubiquitin: structures, functions, mechanisms

Pickart, C. M., & Eddins, M. J. (2004) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/j.bbamcr.2004.09.019 · Cited by 1,491

Induced protein degradation: an emerging drug discovery paradigm

Lai, A. C., & Crews, C. M. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.211 · Cited by 1,486

The proteasome: a suitable antineoplastic target

Adams, J. (2004) · Nature reviews. Cancer · doi:10.1038/nrc1361 · Cited by 1,214

The increasing complexity of the ubiquitin code

Yau, R., & Rape, M. (2016) · Nature Cell Biology · doi:10.1038/ncb3358 · Cited by 1,054

Clinical use and toxicities of bortezomib in pediatric patients: a systematic review

LeBlanc, Z. C., Clapp, A., Kaplan, S. J., Shawber, C. J., & Wu, J. K. (2025) · Frontiers in Pharmacology · doi:10.3389/fphar.2025.1661493 · Cited by 2

Non-peptidic immunoproteasome β5i-selective inhibitor as potential treatment for idiopathic pulmonary fibrosis: Virtual screening, hit evolution and lead identification

Li, Y., Nan, G., Hou, X., Yang, Y., Yang, Y., Yang, Y., Li, K., & Xiao, Z. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115856 · Cited by 2

Structural analysis and shape-based identification of novel inhibitors targeting the Trypanosoma cruzi proteasome

Silva, G. M., Gomes, S. Q., Lopes, C. D., de Albuquerque, S., & da Silva, C. H. T. D. P. (2024) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2024.134290 · Cited by 2

Discovery of Novel Nonpeptidic Proteasome Inhibitors Using Covalent Virtual Screening and Biological Evaluation

Zhou, J., Sang, X., Wu, M., Qian, T., Ciechanover, A. J., An, J., Xu, Y., & Huang, Z. (2024) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.4c00321 · Cited by 2

How Should we Teach Medicinal Chemistry in Higher Education to Prepare Students for a Future Career as Medicinal Chemists and Drug Designers? – A Teacher's Perspective

Klahn, P. (2024) · ChemMedChem · doi:10.1002/cmdc.202400791 · Cited by 4

Tetra-anionic porphyrin mimics protein-protein interactions between regulatory particles and the catalytic core, allosterically activating human 20S proteasome

Santoro, A. M., Persico, M., D’Urso, A., Cunsolo, A., Tkachuk, O., Milardi, D., Purrello, R., Tundo, G. R., Sbardella, D., Osmulski, P. A., et al. (2025) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2025.2482892 · Cited by 2

Development of Macrocyclic Peptide-Based Proteasome Inhibitors with Enhanced Blood-Brain Barrier Penetration for Treating Brain Neoplasms

Almaliti, J., Al-Hindy, M., Fajtová, P., Glukhov, E., Berger, T. W., Graf, Y., da Silva, C. E. H., Huang, C., Azizyan, N., He, Y., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00544 · Cited by 2

Novel Treatments for Multiple Myeloma: What Role Do They Have in Older Adults?

Mian, H. S., & Wildes, T. M. (2018) · Drugs & Aging · doi:10.1007/s40266-018-0539-1 · Cited by 2

Development of peptide epoxyketones as selective immunoproteasome inhibitors

Li, X., Hong, D., Zhang, M., Xu, L., Zhou, Y., Li, J. X., & Liu, T. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113556 · Cited by 2

Lower-Risk Myelodysplastic Syndrome (MDS) Patients Exhibit Diminished Proteasome Proteolytic Activity and High Intracellular Reactive Oxygen Species (ROS) Levels

Zafeiropoulou, K., Kalampounias, G., Alexis, S., Androutsopoulou, T., Katsoris, P., & Symeonidis, A. S. (2023) · Cureus · doi:10.7759/cureus.49843 · Cited by 2

Synthesis and Application of a Versatile Immunoproteasome Activity Probe

Halder, S., Loy, C. A., & Trader, D. J. (2024) · ChemBioChem · doi:10.1002/cbic.202400571 · Cited by 2

Simultaneous proteome localization and turnover analysis reveals spatiotemporal features of protein homeostasis disruptions

Currie, J., Manda, V., Robinson, S. K., Lai, C., Agnihotri, V., Hidalgo, V., Ludwig, R. W., Zhang, K., Pavelka, J., Wang, Z. V., et al. (2023) · doi:10.1101/2023.01.04.521821 · Cited by 2

An Optimized Route to the Syringolin Natural Products Enables Combinatorial Synthesis of Selective, Bioactive Inhibitors of the Plasmodium falciparum 20S Proteasome

Gu, X., Fajtová, P., Yan, N., Saxena, A., Fei, F., Zhu, J., Tse, E., Melo, A., Yoo, E., Buchwald, N. H., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c03223 · Cited by 1

Structural mechanism of 26S proteasome regulation and its pharmacological modulation

Pei, K., Zhao, L., Hu, J., & Mao, Y. (2026) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2026.113256 · Cited by 1

Design and synthesis of amino-substituted N -arylpiperidinyl-based inhibitors of the (immuno)proteasome

Gobec, M., Obreza, A., Jukič, M., Baumgartner, A., Mihelčič, N., Potočnik, Š., Virant, J., Mlinarič, I., Stanislav, R., & Sosič, I. (2023) · Acta Pharmaceutica · doi:10.2478/acph-2023-0032 · Cited by 1

Clickable Probes for Pathogen Proteasomes: Synthesis and Applications

Liu, L. J., Lucero, B., Manriquez-Rodriguez, C., Francisco, K. R., Teixeira, T. R., Yohannan, D. J., Ballatore, C., Myers, S. A., O’Donoghue, A. J., & Caffrey, C. R. (2024) · ACS Omega · doi:10.1021/acsomega.4c04316 · Cited by 1

Targeting Host and Bacterial Signaling Pathways in Tuberculosis: An Effective Strategy for the Development of Novel Anti-tubercular Therapies

Fatima, S., Bhardwaj, B., & Dwivedi, V. P. (2021) · Springer eBooks · doi:10.1007/978-981-33-6827-9_16 · Cited by 1

Science’s Response to COVID-19Preprint

Aye, Y., & Long, M. J. C. (2021) · Preprints.org · doi:10.20944/preprints202103.0416.v1 · Cited by 1

Creating and leveraging bespoke large-scale knowledge graphs for comparative genomics and multi-omics drug discovery with SocialGenePreprint

Clark, C. M., & Kwan, J. C. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.08.16.608329 · Cited by 1

[Research progress on selective immunoproteasome inhibitors].

Kong, L., Lu, J., Zhu, H., & Zhang, J. (2019) · PubMed Central · doi:10.3785/j.issn.1008-9292.2019.12.15

Targeting the Ubiquitin Proteasome System in Pulmonary Fibrosis

Thorley, A. J., Krautwald, S., & Rowlands, D. J. (2020) · Royal Society of Chemistry eBooks · doi:10.1039/9781788015783-00165

Synthesis of proteasome inhibitor 6-deoxy-omuralide and its enantiomer using stereoselective alkylation of substituted proline ester

Li, F., & Jäger, V. (2020) · Organic & Biomolecular Chemistry · doi:10.1039/d0ob01053g

Inhibition studies on the human 20S proteasome: molecular insights from a computational approach

Serrano-Aparicio, N. (2022) · doi:10.6035/14122.2022.684242

An effective method studies the β5 subunit activity of immunoproteasome in vitroPreprint

Lv, H., Yue, H., & FU, D. (2022) · Research Square · doi:10.21203/rs.3.rs-1656980/v1

Decoding ubiquitination in the fight against malaria: a network-based exploration of E1-E2-E3 enzyme triples in Plasmodium falciparum

Cano, L. H. (2023) · doi:10.11606/d.95.2023.tde-09012024-171914

An Effective Method for Studying the β5 Subunit Activity of the Immunoproteasome In VitroPreprint

Guo, J., & Fu, D. B. (2024) · Research Square · doi:10.21203/rs.3.rs-3964880/v1

Design, Synthesis, and Biological Evaluation of Thiourea‐Based Colchicine Derivatives as Proteasome Inhibitors in Cancer Therapy

Rahman, A., Khan, A. T., Khan, S. M., Singh, S., Chowdhury, S., Trivedi, A. K., Ali, A., & Hoda, N. (2025) · ChemistrySelect · doi:10.1002/slct.202503782

Study and applications of [3,3] sigmatropic rearrangement of allyl cyanates for the synthesis of molecules of biological interest.

Henrion, S. (2017) · theses.fr (ABES) · doi:10.70675/064b9720zf4fez4ab6zbc11z7917be1ced46

Développement de méthodes de spectrométrie de masse pour l'étude de la dynamique des complexes de protéasome : application aux cellules stromales/souches mésenchymateuses humaines

Menneteau, T. (2018) · theses.fr (ABES) · doi:10.70675/62c892e6za61bz4865zac89za9a362f99ade

Analysis of the proteasome-autophagy crosstalk under proteotoxic stress conditions in acute myeloid leukemia

Lopez-Reyes, R. G. (2020) · theses.fr (ABES) · doi:10.70675/0cf3c9baz63d4z4ebfzb6efza0a5f5a241b2

Regulation of NFATc3 stability by SUMO and E3 ubiquitin-ligases Trim39 and Trim17

Basu-Shrivastava, M. (2020) · theses.fr (ABES) · doi:10.70675/0aa33054zc607z413dz8aedz05ed052d5438 · Cited by 1

A Cell-Permeable β-Hairpin Peptide Biosensor for Real-Time, Single-Cell Quantification of Proteasome Activity

Rahnama, A., Chadwick, A., DeBock, R., Liu, D., Gauthier, T. J., & Melvin, A. T. (2026) · ACS Sensors · doi:10.1021/acssensors.5c04243

Stereoselective reactions of nitro compounds in the synthesis of natural compound analogs and active pharmaceutical ingredients: recent advances

Sukhorukov, A. Y., Turova, O. V., & Zlotin, S. G. (2026) · Russian Chemical Reviews · doi:10.59761/rcr5237

BindingDB Entry 50002937: Structure-based design of human immuno- and constitutive proteasomes inhibitors.

BindingDB (2020) · UC San Diego · doi:10.7270/q2959m74

BindingDB Entry 50014527: Development of peptide epoxyketones as selective immunoproteasome inhibitors.

BindingDB (2022) · UC San Diego · doi:10.7270/q2br8wzn

BindingDB Entry 50013925: Discovery of selective fragment-sized immunoproteasome inhibitors.

BindingDB (2022) · UC San Diego · doi:10.7270/q2bp06kq

BindingDB Entry 50022441: Non-peptidic immunoproteasome β5i-selective inhibitor as potential treatment for idiopathic pulmonary fibrosis: Virtual screening, hit evolution and lead identification.

BindingDB (2025) · UC San Diego · doi:10.7270/q2np294p

BindingDB Entry 50023503: Discovery of Novel Nonpeptidic Proteasome Inhibitors Using Covalent Virtual Screening and Biological Evaluation.

BindingDB (2026) · UC San Diego · doi:10.7270/q2mg7vfv

BindingDB Entry 50011604: Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors.

BindingDB (2022) · UC San Diego · doi:10.7270/q2xp78j1

BindingDB Entry 50013199: A new class of α-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities.

BindingDB (2022) · UC San Diego · doi:10.7270/q2fn19xd

BindingDB Entry 50009282: Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.

BindingDB (2021) · UC San Diego · doi:10.7270/q2154mhb

BindingDB Entry 50007812: Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.

BindingDB (2021) · UC San Diego · doi:10.7270/q2959mwn

BindingDB Entry 50018635: Covalent Small Molecule Immunomodulators Targeting the Protease Active Site.

BindingDB (2024) · UC San Diego · doi:10.7270/q2t72nnm

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

Sherman, D. J., & Li, J. (2020) · Molecules · doi:10.3390/molecules25030671 · Cited by 77

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

Guedes, R. A., Serra, P., Salvador, J. A. R., & Guedes, R. C. (2016) · Molecules · doi:10.3390/molecules21070927 · Cited by 33

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

Reboud‐Ravaux, M. (2021) · Biologie Aujourd hui · doi:10.1051/jbio/2021005 · Cited by 9

Proteasome Inhibitors: Recent Progress and Future Directions

Wehenkel, M., Ho, Y. K., & Kim, K. (2009) · Cited by 1