Ubiquitylation in immune disorders and cancer: from molecular mechanisms to therapeutic implications [PDF]
, 2012 Conjugation of ubiquitin to proteins (ubiquitylation) has emerged to be one of the most crucial post-translational modifications controlling virtually all cellular processes.
Fulda, Simone +2 more
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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 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.
Adams J. +31 more
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Activation of the E3 ubiquitin ligase Parkin [PDF]
Biochemical Society Transactions, 2015 The PINK1 (phosphatase and tensin homologue-induced putative kinase 1)/Parkin-dependent mitochondrial quality control pathway mediates the clearance of damaged organelles, but appears to be disrupted in Parkinson's disease (PD) [Springer and Kahle (2011) Autophagy 7, 266–278].
Thomas R, Caulfield +2 more
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Science-Business eXchange, 2010 Two groups of researchers have identified inhibitors of E3 ubiquitin ligase, which has been considered difficult, if not impossible, to target with small molecules. The findings could lead to compounds that are more specific disrupters of tumor cell proliferation than the proteasome inhibitor Velcade bortezomib.
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The Role of HECT E3 Ubiquitin Ligases in Colorectal Cancer
Biomedicines, 2023 Colorectal cancer (CRC) is estimated to rank as the second reason for cancer-related deaths, and the prognosis of CRC patients remains unsatisfactory. Numerous studies on gastrointestinal cell biology have shown that the E3 ligase-mediated ubiquitination
Aiqin Sun +3 more
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The MALDI TOF E2/E3 ligase assay as universal tool for drug discovery in the ubiquitin pathway [PDF]
, 2017 In many diseases, components of the ubiquitin system - such as E2/E3 ligases and deubiquitylases - are dysregulated. The ubiquitin system has therefore become an emergent target for the treatment of a number of diseases, including cancer ...
Barlow, Victoria +5 more
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Entropy-Driven Mechanism of an E3 Ligase [PDF]
Biochemistry, 2011 Ubiquitin-like modifications are macromolecular chemistry for which our understanding of the enzymatic mechanisms is lacking. Most E3 ligases in ubiquitin-like modifications do not directly participate in chemistry but are thought to confer allosteric effects; however, the nature of the allosteric effects has been elusive.
Khue, Truong +3 more
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Ubiquitin Ligases at the Heart of Skeletal Muscle Atrophy Control
Molecules, 2021 Skeletal muscle loss is a detrimental side-effect of numerous chronic diseases that dramatically increases mortality and morbidity. The alteration of protein homeostasis is generally due to increased protein breakdown while, protein synthesis may also be
Dulce Peris-Moreno +4 more
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The structure and regulation of Cullin 2 based E3 ubiquitin ligases and their biological functions. [PDF]
, 2016 BACKGROUND: Cullin-RING E3 ubiquitin ligase complexes play a central role in targeting cellular proteins for ubiquitination-dependent protein turnover through 26S proteasome.
Cai, Weijia, Yang, Haifeng
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Computational and Structural Biotechnology Journal, 2022 Protein ubiquitination plays a vital role in controlling the degradation of intracellular proteins and in regulating cell signaling pathways. Functionally, E3 ubiquitin ligases control the transfer of ubiquitin to the target substrates. As a major family
Xiaohua Lou +7 more
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