Results 31 to 40 of about 223,575 (250)

A clinically relevant pulse treatment generates a bortezomib-resistant myeloma cell line that lacks proteasome mutations and is sensitive to Bcl-2 inhibitor venetoclax

open access: yesScientific Reports, 2022
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]

open access: yesInternational Journal of Biomedicine, 2019
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]

open access: yes, 2016
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]

open access: yes, 2017
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]

open access: yesPLoS ONE, 2011
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]

open access: yes, 2013
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]

open access: yesMedicinal Research Reviews, 2001
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]

open access: yes, 2016
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

Involvement of the ubiquitin-proteasome system in the expression of extracellular matrix genes in retinal pigment epithelial cells

open access: yesBiochemistry and Biophysics Reports, 2018
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]

open access: yes, 2008
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

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