Cited by 144Ubiquitin and proteasome pathwaysProtein Degradation and InhibitorsProtease and Inhibitor Mechanisms

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

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Cromm, Philipp M., Crews, Craig M.·2017·ACS Central Science

DOI 10.1021/acscentsci.7b00252PMC PMC5571462

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Abstract

As the central figure of the cellular protein degradation machinery, the proteasome is critical for cell survival. Having been extensively targeted for inhibition, the constitutive proteasome has proven its role as a highly valuable drug target. However, recent advances in the protein homeostasis field suggest that additional chapters can be added to this successful story. For example, selective immunoproteasome inhibition promises high clinical efficacy for autoimmune disorders and inflammation, and proteasome inhibitors might serve as novel therapeutics for malaria or other microorganisms. Furthermore, utilizing the destructive force of the proteasome for selective degradation of essential drivers of human disorders has opened up a new and exciting area of drug discovery. Thus, the field of proteasome drug discovery still holds exciting questions to be answered and does not simply end with inhibiting the constitutive proteasome.

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Authors: Cromm, P. M., & Crews, C. M.
Affiliations: Yale University (US)
Corresponding author: Cromm, Philipp M.
Crews, Craig M.
ORCID: Cromm, Philipp M.
Crews, Craig M.
Venue: ACS Central Science
Publisher: American Chemical Society (ACS)
Published: 2017-08-07
Volume: 3
Issue: 8
Pages: 830-838
ISSN: 2374-7943 (ISSN-L)
2374-7951
DOI: 10.1021/acscentsci.7b00252
PMC: PMC5571462
OpenAlex: W2744284720
Cited by: 136
References: 85
Citations by year: 2026: 5 · 2025: 11 · 2024: 12 · 2023: 18 · 2022: 13 · 2021: 18 · 2020: 27 · 2019: 16 · 2018: 14 · 2017: 2
FWCI: 1.54
Type: journal article
Language: en
Open access: diamond
doi.org
Licence: other-oa
pubs.acs.org/page/policy/authorchoice_termsofuse.html (vor)
Locations: ACS Central Science (publishedVersion, other-oa)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders: National Cancer Institute (R35 CA197589)
Alexander von Humboldt-Stiftung
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ubiquitin and proteasome pathways
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Protease and Inhibitor Mechanisms
Keywords: proteasome, proteasome inhibitors, therapeutic target, proteostasis, selective protein degradation, autoimmune disease, inflammation, malaria, antimicrobial agents

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

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