Proteasome inhibitors bortezomib and carfilzomib are the backbones of treatments of multiple myeloma, which remains incurable despite many recent advances.
Sondra L. Downey-Kopyscinski +2 more
doaj +1 more source
Abstract OR-12: Cryo-EM of Human and Parasite Proteasomes for Structure-Based Drug Design [PDF]
Background: The increasing spread of Plasmodium falciparum resistance to current antimalarials, including the frontline artemisinin and its derivatives, represents a major global threat to human health and urges the development of novel medicaments.
Pavel Afanasyev +3 more
doaj +1 more source
Next-generation proteasome inhibitor oprozomib synergizes with modulators of the unfolded protein response to suppress hepatocellular carcinoma [PDF]
Hepatocellular carcinoma (HCC) responds poorly to conventional systemic therapies. The first-in-class proteasome inhibitor bortezomib has been approved in clinical use for hematologic malignancies and has shown modest activity in solid tumors, including ...
Bogaerts, Eliene +12 more
core +2 more sources
Axitinib induces senescence-associated cell death and necrosis in glioma cell lines: The proteasome inhibitor, bortezomib, potentiates axitinib-induced cytotoxicity in a p21(Waf/Cip1) dependent manner. [PDF]
Glioblastoma is associated with a poor overall survival despite new treatment advances. Antiangiogenic strategies targeting VEGF based on tyrosine kinase inhibitors (TKIs) are currently undergoing extensive research for the treatment of glioma.
Amantini, C +7 more
core +1 more source
Thiazole antibiotic thiostrepton synergize with bortezomib to induce apoptosis in cancer cells. [PDF]
Thiazole antibiotic, thiostrepton was recently identified as proteasome inhibitor. We investigated the therapeutic potential of the combination of thiostrepton and proteasome inhibitor bortezomib (Velcade) on various human tumor cell lines.
Bulbul Pandit, Andrei L Gartel
doaj +1 more source
The proteasome cap RPT5/Rpt5p subunit prevents aggregation of unfolded ricin A chain [PDF]
The plant cytotoxin ricin enters mammalian cells by receptor-mediated endocytosis, undergoing retrograde transport to the endoplasmic reticulum (ER) where its catalytic A chain (RTA) is reductively separated from the holotoxin to enter the cytosol and ...
Afshar +61 more
core +2 more sources
The ubiquitin‐proteasome pathway and proteasome inhibitors [PDF]
AbstractThe ubiquitin‐proteasome pathway has emerged as a central player in the regulation of several diverse cellular processes. Here, we describe the important components of this complex biochemical machinery as well as several important cellular substrates targeted by this pathway and examples of human diseases resulting from defects in various ...
J, Myung, K B, Kim, C M, Crews
openaire +2 more sources
BH3 mimetic ABT-737 sensitizes colorectal cancer cells to ixazomib through MCL-1 downregulation and autophagy inhibition. [PDF]
The proteasome inhibitor MLN9708 is an orally administered drug that is hydrolyzed into its active form, MLN2238 (ixazomib). Compared with Bortezomib, MLN2238 has a shorter proteasome dissociation half-life and a lower incidence and severity of ...
Barkhouse, Darryll +7 more
core +2 more sources
Emerging evidence suggests that dysfunction of the ubiquitin-proteasome system is involved in the pathogenesis of numerous senile degenerative diseases including retinal disorders.
J. Emanuel Ramos de Carvalho +6 more
doaj +1 more source
Assessment of the direct and indirect effects of MPP+ and dopamine on the human proteasome: implications for Parkinson's disease aetiology [PDF]
Mitochondrial impairment, glutathione depletion and oxidative stress have been implicated in the pathogenesis of Parkinson’s disease (PD), linked recently to proteasomal dysfunction.
Beck, KE +5 more
core +1 more source

