Results 21 to 30 of about 752,942 (288)

Fluorescence-based proteasome activity profiling [PDF]

, 2011
With the proteasome emerging as a therapeutic target for cancer treatment, accurate tools for monitoring proteasome (inhibitor) activity are in demand.
Jong, A., Rodenko, B., Berkers, C.R., Schuurman, K.G., Ovaa, H., Boris Rodenko, Annemieke de Jong, Celia R. Berkers, Karianne G. Schuurman, Huib Ovaa   +9 more
core   +1 more source

Regulation of TRIB1 abundance in hepatocyte models in response to proteasome inhibition

Scientific Reports, 2023
Tribbles related homolog 1 (TRIB1) contributes to lipid and glucose homeostasis by facilitating the degradation of cognate cargos by the proteasome. In view of the key metabolic role of TRIB1 and the impact of proteasome inhibition on hepatic function ...
Sébastien Soubeyrand, Paulina Lau, Ruth McPherson   +2 more
doaj   +1 more source

Paradoxical inhibition of cellular protein expression by proteasome inhibitors

Biomolecular Concepts, 2012
Proteasome inhibitors are used as anticancer drugs, however, the precise mechanisms of their selective activity against cancer cells are not understood well.
Gartel Andrei L.
doaj   +1 more source

Autophagy-independent enhancing effects of Beclin 1 on cytotoxicity of ovarian cancer cells mediated by proteasome inhibitors

BMC Cancer, 2012
Background The ubiquitin-proteasome system and macroautophagy (hereafter referred to autophagy) are two complementary pathways for protein degradation. Emerging evidence suggests that proteasome inhibition might be a promising approach for tumor therapy.
Liu Chuan, Yan Xu, Wang Hua-Qin, Gao Yan-Yan, Liu Juanjuan, Hu Zhenhua, Liu Dawo, Gao Jian, Lin Bei   +8 more
doaj   +1 more source

Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von hippel-lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities [PDF]

, 2014
E3 ubiquitin ligases are attractive targets in the ubiquitin-proteasome system, however, the development of small-molecule ligands has been rewarded with limited success.
Dias, David M, Carles Galdeano (1305135), Galdeano, Carles, Dias, David M., David M. Dias (1340694), Van Molle, Inge, Gadd, Morgan Stuart, Ciulli, Alessio, Sarah Hewitt (1340700), Soares, Pedro, Galdeano , Carles, Pedro Soares (393566), Gadd, Morgan S., Salvatore Scaffidi (1340703), Inge Van Molle (1284120), Morgan S. Gadd (149371), Scaffidi, Salvatore, Ipek Birced (1340697), Alessio Ciulli (762789), Hewitt, Sarah, Birced, Ipek   +20 more
core   +1 more source

Different effect of proteasome inhibition on vesicular stomatitis virus and poliovirus replication. [PDF]

PLoS ONE, 2008
Proteasome activity is an important part of viral replication. In this study, we examined the effect of proteasome inhibitors on the replication of vesicular stomatitis virus (VSV) and poliovirus.
Nickolay Neznanov, Eugenia M Dragunsky, Konstantin M Chumakov, Lubov Neznanova, Ronald C Wek, Andrei V Gudkov, Amiya K Banerjee   +6 more
doaj   +1 more source

The proteasome cap RPT5/Rpt5p subunit prevents aggregation of unfolded ricin A chain [PDF]

, 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 ...
Spooner, Robert A., Roberts, David M, Roberts, Lynne M, Lord, J Michael, Cook, Jonathan P., Pietroni, Paola, Roberts, David M., Lord, Mike, Roberts, L. M. (Lynne M.), Spooner, Robert A, Vasisht, Nishi, Hartmann-Petersen, Rasmus, Cook, Jonathan P   +12 more
core   +1 more source

Higher ratio immune versus constitutive proteasome level as novel indicator of sensitivity of pediatric acute leukemia cells to proteasome inhibitors

Haematologica, 2013
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, Niels E. Franke, Gerrit Jansen, Yehuda G. Assaraf, Johan van Meerloo, Christopher J. Kirk, Jeremiah Degenhardt, Janet Anderl, Aaron D. Schimmer, Sonja Zweegman, Valerie de Haas, Terzah M. Horton, Gertjan J.L. Kaspers, Jacqueline Cloos   +13 more
doaj   +1 more source

The degradation of p53 and its major E3 ligase Mdm2 is differentially dependent on the proteasomal ubiquitin receptor S5a. [PDF]

, 2014
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, S Menendez, Menendez, S., Saville, M. K., S Dayal, Das, J., M K Saville, Dayal, S., A Sparks, Robertson, P., P Robertson, Sparks, A.   +11 more
core   +1 more source

New Scaffolds of Proteasome Inhibitors: Boosting Anticancer Potential by Exploiting the Synergy of In Silico and In Vitro Methodologies

Pharmaceuticals, 2023
Cancer is a complex multifactorial disease whose pathophysiology involves multiple metabolic pathways, including the ubiquitin–proteasome system, for which several proteasome inhibitors have already been approved for clinical use. However, the resistance
Romina A. Guedes, Jorge H. Grilo, Andreia N. Carvalho, Pedro M. P. Fernandes, Ana S. Ressurreição, Vanessa Brito, Adriana O. Santos, Samuel Silvestre, Eleonora Gallerani, Maria João Gama, Riccardo Gavioli, Jorge A. R. Salvador, Rita C. Guedes   +12 more
doaj   +1 more source