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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 AffinitiesOmuralide and vibralactone: differences in the proteasome- β-lactone-γ-lactam binding scaffold alter target preferencesSystematic comparison of peptidic proteasome inhibitors highlights the α-ketoamide electrophile as an auspicious reversible lead motifSelective inhibition of the immunoproteasome by ligand-induced crosslinking of the active sitePotent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibitionSynthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer.Development of inhibitors in the ubiquitination cascade.Highly specific ubiquitin-competing molecules effectively promote frataxin accumulation and partially rescue the aconitase defect in Friedreich ataxia cells.Discovery of new [Formula: see text] proteasome inhibitors using a knowledge-based computational screening approach.A strategy for dual inhibition of the proteasome and fatty acid synthase with belactosin C-orlistat hybrids.Proteomics guided discovery of flavopeptins: anti-proliferative aldehydes synthesized by a reductase domain-containing non-ribosomal peptide synthetase.Total Synthesis and Stereochemical Assignment of Nostosin B.Small-molecule control of intracellular protein levels through modulation of the ubiquitin proteasome systemPharmacophore modeling technique applied for the discovery of proteasome inhibitors.Recent advances in defining the ubiquitylome.Development of novel selective peptidomimetics containing a boronic acid moiety, targeting the 20S proteasome as anticancer agents.Tyropeptins, proteasome inhibitors produced by Kitasatospora sp. MK993-dF2.The Proteasome in Modern Drug Discovery: Second Life of a Highly Valuable Drug Targetα-Boryl isocyanides enable facile preparation of bioactive boropeptides.Development and Elucidation of a Novel Fluorescent Boron-Sensor for the Analysis of Boronic Acid-Containing Compounds.Synthesis and bioactivity of fused- and spiro-β-lactone-lactam systems.Baceridin, a cyclic hexapeptide from an epiphytic bacillus strain, inhibits the proteasome.Heterologous production of glidobactins/luminmycins in Escherichia coli Nissle containing the glidobactin biosynthetic gene cluster from Burkholderia DSM7029.
P2860
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P2860
description
article científic
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article scientifique
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articol științific
@ro
articolo scientifico
@it
artigo científico
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artigo científico
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artigo científico
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artikel ilmiah
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artikull shkencor
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artículo científico
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name
Synthesis and pharmacology of proteasome inhibitors.
@en
type
label
Synthesis and pharmacology of proteasome inhibitors.
@en
prefLabel
Synthesis and pharmacology of proteasome inhibitors.
@en
P2093
P2860
P356
P1476
Synthesis and pharmacology of proteasome inhibitors.
@en
P2093
Andreas Rentsch
Anna-Katharina Girbig
Dirk Landsberg
Leila Bülow
Markus Kalesse
Tobias Brodmann
P2860
P304
P356
10.1002/ANIE.201207900
P407
P577
2013-03-25T00:00:00Z