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

J Xi, R Zhuang, L Kong, R He, H Zhu… - European Journal of …, 2019 - Elsevier
The immunoproteasome, a specialized form of proteasome, is mainly expressed in
lymphocytes and monocytes of jawed vertebrates and responsible for the generation of …

Inhibitors of the immunoproteasome: current status and future directions

Z Miller, L Ao, K Bo Kim, W Lee - Current pharmaceutical …, 2013 - ingentaconnect.com
The ubiquitin-proteasome system (UPS) plays a vital role in maintaining protein
homeostasis and regulating numerous cellular processes. The proteasome, a multi-protease …

Immunoproteasome-selective inhibitors: a promising strategy to treat hematologic malignancies, autoimmune and inflammatory diseases

R Ettari, S Previti, A Bitto, S Grasso… - Current medicinal …, 2016 - ingentaconnect.com
The immunoproteasome is predominantly expressed in monocytes and lymphocytes and is
responsible for the generation of antigenic peptides for cell-mediated immunity. Upon the …

Immunoproteasome-selective inhibitors: the future of autoimmune diseases?

C Zhang, H Zhu, J Shao, R He, J Xi… - Future Medicinal …, 2020 - Taylor & Francis
The immunoproteasome, a specialized variant of the constitutive one, is predominantly
expressed in lymphocytes and monocytes of jawed vertebrates and is considered to be …

Design and evaluation of highly selective human immunoproteasome inhibitors reveal a compensatory process that preserves immune cell viability

E Ladi, C Everett, CE Stivala, BE Daniels… - Journal of Medicinal …, 2019 - ACS Publications
The pan-proteasome inhibitor bortezomib demonstrated clinical efficacy in off-label trials of
Systemic Lupus Erythematosus. One potential mechanism of this clinical benefit is from the …

Development of novel amides as noncovalent inhibitors of immunoproteasomes

R Ettari, C Cerchia, S Maiorana, M Guccione… - …, 2019 - Wiley Online Library
The development of immunoproteasome‐selective inhibitors is a promising strategy for
treating hematologic malignancies, autoimmune and inflammatory diseases. In this context …

Immunoproteasome-selective and non-selective inhibitors: A promising approach for the treatment of multiple myeloma

R Ettari, M Zappalà, S Grasso, C Musolino… - Pharmacology & …, 2018 - Elsevier
The ubiquitin-proteasome system (UPS) is the major non-lysosomal proteolytic system for
the degradation of abnormal or damaged proteins no longer required. The proteasome is …

Amelioration of autoimmunity with an inhibitor selectively targeting all active centres of the immunoproteasome

M Basler, E Maurits, G de Bruin… - British Journal of …, 2018 - Wiley Online Library
Background and Purpose Multicatalytic endopeptidase complex‐like‐1 (β2i), low molecular
mass polypeptide (LMP) 2 (β1i) and LMP7 (β5i) are the proteolytically active subunits of the …

The immunoproteasome: an emerging therapeutic target

W Lee, K Bo Kim - Current topics in medicinal chemistry, 2011 - ingentaconnect.com
The proteasome, a large multisubunit protease complex, has been extensively investigated
over the years, greatly enhancing our understanding of critical roles that the proteasome …

Discovery and early clinical development of selective immunoproteasome inhibitors

CJ Kirk, T Muchamuel, J Wang, RA Fan - Cells, 2021 - mdpi.com
Inhibitors of the proteolytic activity of the 20S proteasome have transformed the treatment of
multiple B-cell malignancies. These agents have also been employed with success in the …