[HTML][HTML] A nut for every bolt: subunit-selective inhibitors of the immunoproteasome and their therapeutic potential

EM Huber, M Groll - Cells, 2021 - mdpi.com
… the discovery of CP subtypes, the interest in selective CP … the peptide substrate Ac-PAL-AMC,
used to selectively monitor … Furthermore, PR-924 and its derivatives show high selectivity

[HTML][HTML] Immunoproteasome-selective inhibitors: the future of autoimmune diseases?

C Zhang, H Zhu, J Shao, R He, J Xi… - Future Medicinal …, 2020 - Taylor & Francis
immunoproteasome-selective inhibitors with electrophilic groups at the C-terminal of the
peptide … important approach for the discovery of novel immunoproteasome-selective inhibitors. …

Discovery of selective fragment-sized immunoproteasome inhibitors

L Kollár, M Gobec, B Szilágyi, M Proj, D Knez… - European Journal of …, 2021 - Elsevier
discovery of 7-chloro-substituted benzoXazole-2-carbonitriles that inhibited the β5i subunit
of iCP in the low micromolar range, showed preferential inhibition … -peptide inhibitors against …

Recent insights how combined inhibition of immuno/proteasome subunits enables therapeutic efficacy

M Basler, M Groettrup - Genes & Immunity, 2020 - nature.com
… β2c, and β5c with the immunoproteasome subunits low molecular mass polypeptide (LMP) 2
(… for longer time periods, whereas PRN1126 remained highly selective for LMP7 and did not …

[HTML][HTML] Site-specific proteasome inhibitors

AF Kisselev - Biomolecules, 2021 - mdpi.com
… Reversible linear and cyclical peptide inhibitors that lack electrophiles have also been … and
immunoproteasomes were elucidated by X-ray diffraction. They are highly selective over β1c …

Structure-based optimization and discovery of M3258, a specific inhibitor of the immunoproteasome subunit LMP7 (β5i)

M Klein, M Busch, M Friese-Hamim… - Journal of medicinal …, 2021 - ACS Publications
… of the constitutive proteasome and immunoproteasome with comparable potency, which …
discovery and structure-based hit optimization of novel amido boronic acids, which selectively

Structure–Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides

W Zhan, PK Singh, Y Ban, X Qing… - Journal of medicinal …, 2020 - ACS Publications
… DPLG3 is a highly selective immunoproteasome β5i inhibitor with single-… inhibition of only
β5i or β5c can induce cell death is still understudied; (2) selective inhibition of β5i by peptide

Identification of N, C-capped di-and tripeptides as selective immunoproteasome inhibitors

G Nan, L Huang, Y Li, Y Yang, Y Yang, K Li… - European Journal of …, 2022 - Elsevier
… 1), a highly selective and potent β5i non-covalent inhibitor, … The aforementioned observations
suggested that selective inhibition of … Most known i-20S inhibitors are featured by a peptide

Development of peptide epoxyketones as selective immunoproteasome inhibitors

X Li, D Hong, M Zhang, L Xu, Y Zhou, J Li… - European Journal of …, 2021 - Elsevier
… , we herein report the discovery of a series of selective β5i inhibitors through fragment-based …
P3 site were the most selective inhibitors, which showed higher selectivity than ONX-0914. …

[PDF][PDF] A Nut for Every Bolt: Subunit-Selective Inhibitors of the Immunoproteasome and Their Therapeutic Potential. Cells 2021, 10, 1929

EM Huber, M Groll - 2021 - pdfs.semanticscholar.org
… of various peptide-based iCP selective inhibitors (see … of the Immunoproteasome Low
Molecular Mass Polypeptide … with a highly selective immunoproteasome inhibitor promotes …