Results 21 to 30 of about 1,016,262 (299)
Constitutive degradation of IκBα in human T lymphocytes is mediated by calpain
Background Activation-induced induction of transcription factor NFκB in T lymphocytes is regulated by its inhibitor IκBα. NFκB activation has been demonstrated to occur either by phosphorylation on serine residues 32 and 36 of the inhibitor, IκBα ...
Cullen Sarah J +2 more
doaj +1 more source
The ex vivo sensitivity of pediatric leukemia cells to the proteasome inhibitor bortezomib was compared to 3 next generation proteasome inhibitors: the epoxyketone-based irreversible proteasome inhibitors carfilzomib, its orally bio-available analog ONX ...
Denise Niewerth +13 more
doaj +1 more source
Inhibition of NGLY1 inactivates the transcription factor Nrf1 and potentiates proteasome inhibitor cytotoxicity [PDF]
We discovered that the proteostasis modulating transcription factor Nrf1 requires cytosolic de-N-glycosylation by the N-glycanase NGly1 as part of its activation mechanism.
Diana, Ordoñez-Rueda +18 more
core +2 more sources
Proteasome dysfunction triggers activation of SKN-1A/Nrf1 by the aspartic protease DDI-1
Proteasomes are essential for protein homeostasis in eukaryotes. To preserve cellular function, transcription of proteasome subunit genes is induced in response to proteasome dysfunction caused by pathogen attacks or proteasome inhibitor drugs.
Nicolas J Lehrbach, Gary Ruvkun
doaj +1 more source
Assembly of the Drosophila 26 S proteasome is accompanied by extensive subunit rearrangements [PDF]
The subunit contacts in the regulatory complex of the Drosophila 26 S proteasome were studied through the cross-linking of closely spaced subunits of the complex, and analysis of the cross-linking pattern in an immunoblot assay with the use of subunit ...
Kapelari, Barbara +13 more
core +2 more sources
The degradation of p53 and its major E3 ligase Mdm2 is differentially dependent on the proteasomal ubiquitin receptor S5a. [PDF]
p53 and its major E3 ligase Mdm2 are both ubiquitinated and targeted to the proteasome for degradation. Despite the importance of this in regulating the p53 pathway, little is known about the mechanisms of proteasomal recognition of ubiquitinated p53 and
J Das +11 more
core +1 more source
Carfilzomib, a second-generation proteasome inhibitor, has significantly improved the survival rate of multiple myeloma (MM) patients, but its clinical application is still restricted by drug resistance and cardiotoxicity.
Xuxing Shen +10 more
doaj +1 more source
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
Syrbactin-class dual constitutive- and immuno-proteasome inhibitor TIR-199 impedes myeloma-mediated bone degeneration in vivo [PDF]
Proteasome-addicted neoplastic malignancies present a considerable refractory and relapsed phenotype with patients exhibiting drug resistance and high mortality rates.
Vala, Ruturajsinh M. +18 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

