Results 41 to 50 of about 5,747 (197)
The Immunoproteasome as a Target in Hematologic Malignancies [PDF]
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
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]
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
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
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]
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]
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
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]
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
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

