Results 41 to 50 of about 5,747 (197)

The Immunoproteasome as a Target in Hematologic Malignancies [PDF]

open access: yesSeminars in Hematology, 2012
Suppression of proteasome function with the first-in-class small molecule inhibitor bortezomib is a rational therapeutic strategy against several hematologic malignancies, including multiple myeloma and mantle cell lymphoma. Second-generation inhibitors such as carfilzomib, ixazomib, and marizomib that, like bortezomib, target both the constitutive ...
Deborah J, Kuhn, Robert Z, Orlowski
openaire   +2 more sources

Discovery of selective fragment-sized immunoproteasome inhibitors

open access: yes, 2021
Proteasomes contribute to maintaining protein homeostasis and their inhibition is beneficial in certain types of cancer and in autoimmune diseases. However, the inhibition of the proteasomes in healthy cells leads to unwanted side-effects and significant
Imre, Tímea   +10 more
core   +1 more source

Selective Immunoproteasome Inhibitors with Non-Peptide Scaffolds [PDF]

open access: yes, 2017
Compounds useful for inhibiting the immunoproteasome have the formula of [image on patent]. Methods and compounds for inhibiting the immunoproteasome, particularly, immunoproteasome inhibitors with non-peptide scaffolds, are ...
Zhan, Chang-Guo   +3 more
core   +1 more source

Evaluation of Immunoproteasome-Specific Proteolytic Activity Using Fluorogenic Peptide Substrates

open access: yes, 2022
The 26S proteasome irreversibly hydrolyzes polyubiquitylated substrates to maintain protein homeostasis; it also regulates immune responses by generating antigenic peptides.
Lee, Min Jae   +3 more
core   +1 more source

Synthesis and Biochemical Evaluation of Warhead-Decorated Psoralens as (Immuno)Proteasome Inhibitors

open access: yesMolecules, 2021
The immunoproteasome is a multicatalytic protease that is predominantly expressed in cells of hematopoietic origin. Its elevated expression has been associated with autoimmune diseases, various types of cancer, and inflammatory diseases.
Eva Shannon Schiffrer   +7 more
doaj   +1 more source

Role of Immunoproteasomes in Cross-Presentation [PDF]

open access: yesThe Journal of Immunology, 2006
Abstract The evidence that proteasomes are involved in the processing of cross-presented proteins is indirect and based on the in vitro use of proteasome inhibitors. It remains, therefore, unclear whether cross-presentation of MHC class I peptide epitopes can occur entirely within phagolysosomes or whether it requires proteasome ...
Palmowski, M   +10 more
openaire   +3 more sources

Association of immunoproteasomes with the endoplasmic reticulum [PDF]

open access: yesBiochemical Journal, 2000
Proteasomes are complex multisubunit proteases which play a critical role in intracellular proteolysis. Immunoproteasomes, which contain three γ-interferon-inducible subunits, are a subset of proteasomes which have a specialized function in antigen processing for presentation by the MHC class I pathway.
Brooks, P.   +4 more
openaire   +3 more sources

Blood Immunoproteasome Activity Is Regulated by Sex, Age and in Chronic Inflammatory Diseases: A First Population-Based Study

open access: yesCells, 2021
Dysfunction of the immunoproteasome has been implicated in cardiovascular and pulmonary diseases. Its potential as a biomarker for predicting disease stages, however, has not been investigated so far and population-based analyses on the impact of sex and
Ilona Elisabeth Kammerl   +7 more
doaj   +1 more source

PSMB9 codon 60 polymorphisms have no impact on the activity of the immunoproteasome catalytic subunit B1i expressed in multiple types of solid cancer. [PDF]

open access: yesPLoS ONE, 2013
The proteasome is a key regulator of cellular protein homeostasis and is a clinically validated anticancer target. The immunoproteasome, a subtype of proteasome expressed mainly in hematopoietic cells, was initially recognized for its role in antigen ...
Ji Eun Park   +8 more
doaj   +1 more source

Structure of human immunoproteasome with a reversible and noncompetitive inhibitor that selectively inhibits activated lymphocytes

open access: yesNature Communications, 2017
Immunoproteasome selective inhibitors might lead to less toxic drugs for treatment of multiple myeloma and graft rejection. Here, the authors develop immunoproteasome specific asparagine-ethylenediamine (AsnEDA)-based inhibitory compounds, demonstrate ...
Ruda de Luna Almeida Santos   +13 more
doaj   +1 more source

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