Structure‐Based Design of Fluorogenic Substrates Selective for Human Proteasome Subunits
Sign Up to like & getrecommendations! Published in 2020 at "Chembiochem"
DOI: 10.1002/cbic.202000375
Abstract: Proteasomes are established therapeutic targets for hematological cancers and promising targets for autoimmune diseases. In the past, we have designed and synthesized mechanism‐based proteasome inhibitors that are selective for the individual catalytic activities of human… read more here.
Keywords: design fluorogenic; proteasome; structure based; based design ... See more keywords
PCPS: A Web Server to Predict Proteasomal Cleavage Sites.
Sign Up to like & getrecommendations! Published in 2020 at "Methods in molecular biology"
DOI: 10.1007/978-1-0716-0389-5_23
Abstract: The proteasome complex is mainly responsible for proteolytic degradation of cytosolic proteins, generating the C-terminus of MHC I-restricted peptide ligands and CD8 T cell epitopes. Therefore, prediction of proteasomal cleavage sites is relevant for anticipating… read more here.
Keywords: proteasomal cleavage; cleavage; proteasome; pcps web ... See more keywords
Bassoon inhibits proteasome activity via interaction with PSMB4
Sign Up to like & getrecommendations! Published in 2020 at "Cellular and Molecular Life Sciences"
DOI: 10.1007/s00018-020-03590-z
Abstract: Abstract Proteasomes are protein complexes that mediate controlled degradation of damaged or unneeded cellular proteins. In neurons, proteasome regulates synaptic function and its dysfunction has been linked to neurodegeneration and neuronal cell death. However, endogenous… read more here.
Keywords: protein; proteasome; psmb4; activity ... See more keywords
Putting it all together: intrinsic and extrinsic mechanisms governing proteasome biogenesis
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DOI: 10.1007/s11515-017-1439-1
Abstract: BackgroundThe 26S proteasome is at the heart of the ubiquitin-proteasome system, which is the key cellular pathway for the regulated degradation of proteins and enforcement of protein quality control. The 26S proteasome is an unusually… read more here.
Keywords: putting together; proteasome biogenesis; proteasome; proteasome assembly ... See more keywords
NMR 1H, 13C, 15N backbone and side chain resonance assignment of the N-terminal domain of yeast proteasome lid subunit Rpn5
Sign Up to like & getrecommendations! Published in 2019 at "Biomolecular NMR Assignments"
DOI: 10.1007/s12104-018-9840-5
Abstract: The 26S proteasome is responsible for the selective, ATP-dependent degradation of polyubiquitinated proteins in eukaryotic cells. It consists of a 20S barrel-shaped core particle capped by two 19S regulatory particle at both ends. The Rpn5… read more here.
Keywords: terminal domain; 13c 15n; proteasome; subunit ... See more keywords
Dynamic changes of proteasome and protective effect of bortezomib, a proteasome inhibitor, in mice with acute pancreatitis.
Sign Up to like & getrecommendations! Published in 2018 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2018.09.066
Abstract: The proteasome is involved in the activation of NF-κB and can regulate the progression of inflammatory diseases. However, the role of proteasome in acute pancreatitis (AP) has not been demonstrated. In this study, we first… read more here.
Keywords: acute pancreatitis; proteasome; inhibitor; mice ... See more keywords
Repurposing of auranofin: Thioredoxin reductase remains a primary target of the drug.
Sign Up to like & getrecommendations! Published in 2019 at "Biochimie"
DOI: 10.1016/j.biochi.2019.03.015
Abstract: Auranofin is a gold (I)-containing compound used for the treatment of rheumatic arthritis. Auranofin has anticancer activity in animal models and is approved for clinical trials for lung and ovarian carcinomas. Both the cytosolic and… read more here.
Keywords: thioredoxin reductase; inhibitor; proteasome; activity ... See more keywords
Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.12.064
Abstract: The potential of specific proteasome inhibitors to act as anti-cancer agents has attracted intensive investigations. The proteasome can be covalently inhibited by epoxyketone derivatives via a two-step reaction. Several computational approaches have been developed to… read more here.
Keywords: docking modelling; proteasome inhibitors; proteasome; covalent docking ... See more keywords
Biological consequences of structural and functional proteasome diversity
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DOI: 10.1016/j.heliyon.2018.e00894
Abstract: Cell homeostasis and regulation of metabolic pathways are ensured by synthesis, proper folding and efficient degradation of a vast amount of proteins. Ubiquitin-proteasome system (UPS) degrades most intracellular proteins and thus, participates in regulation of… read more here.
Keywords: consequences structural; proteasome; proteasome diversity; structural functional ... See more keywords
A comparative analysis between proteasome and immunoproteasome inhibition in cellular and humoral alloimmunity
Sign Up to like & getrecommendations! Published in 2017 at "International Immunopharmacology"
DOI: 10.1016/j.intimp.2017.06.009
Abstract: Abstract Triggered by the successful administration of the proteasome inhibitor bortezomib in kidney transplant recipients with acute or chronic antibody‐mediated rejection, we evaluated the effect of the proteasome inhibitor CEP‐18770 and of the selective immunoproteasome… read more here.
Keywords: alloimmunity; inhibitor; proteasome; immunoproteasome ... See more keywords
Synthesis of novel 3-(quinazol-2-yl)-quinolines via SNAr and aluminum chloride-induced (hetero) arylation reactions and biological evaluation as proteasome inhibitors
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DOI: 10.1016/j.tetlet.2020.151805
Abstract: Abstract A new series of 3-(quinazol-2-yl)-quinolines was synthesized by SNAr reaction from easily prepared 4-chloro-2-(2-chloroquinolin-3-yl)quinazolines and a range of phenols and thiophenol as nucleophiles. The AlCl3-mediated C C bond formation was also successfully exploited to… read more here.
Keywords: quinazol; synthesis novel; proteasome; novel quinazol ... See more keywords