Results 91 to 100 of about 120,389 (309)

An integrated bioinformatics platform for investigating the human E3 ubiquitin ligase-substrate interaction network

open access: yesNature Communications, 2017
Protein stability modulation by E3 ubiquitin ligases is an important layer of functional regulation, but screening for E3 ligase-substrate interactions is time-consuming and costly.
Yang Li   +12 more
doaj   +1 more source

Decoys provide a scalable platform for the identification of plant E3 ubiquitin ligases that regulate circadian function

open access: yeseLife, 2019
The circadian clock relies on regulated degradation of clock proteins to maintain rhythmicity. Despite this, we know few components that mediate protein degradation.
Ann Feke   +6 more
doaj   +1 more source

Ubiquitin-specific protease USP25 functions in endoplasmic reticulum-associated degradation

open access: yes, 2012
Endoplasmic Reticulum (ER)-associated degradation (ERAD) discards abnormal proteins synthesized in the ER. Through coordinated actions of ERAD components, misfolded/anomalous proteins are recognized, ubiquitinated, extracted from the ER and ultimately ...
Amanda Denuc   +14 more
core   +1 more source

Natural Products Inspired Scaffold Diversification Leads to Unnatural Molecular Warhead and Covalent Strategy to Modulating Protein Function through Electrophilic Bromine Transfer

open access: yesAdvanced Science, EarlyView.
We report a new thiolate‐reactive α,α‐gem‐dibromo lactam warhead that activates transcription factor Nrf2 and demonstrates anti‐inflammatory activities, which have implications in cancer, neurodegeneration, and cardiovascular diseases. RNA‐seq illuminated detailed transcriptional profiles, and chemical reactions with cysteine‐containing compounds ...
Beau R. Brummel   +16 more
wiley   +1 more source

IAPs as E3 ligases of Rac1 : shaping the move

open access: yes, 2012
Inhibitors of Apoptosis Proteins (IAPs) are well-studied E3 ubiquitin ligases predominantly known for regulation of apoptosis. We uncovered that IAPs can function as a direct E3 ubiquitin ligase of RhoGTPase Rac1.
Oberoi-Khanuja, Tripat Kaur   +1 more
core   +1 more source

Enhanced Glycolysis‐Driven Histone H3K18 Lactylation Regulates Epileptogenesis by Modulating the E3 Ubiquitin Ligase COP1

open access: yesAdvanced Science, EarlyView.
Neuronal PKM2‐driven glycolysis generates excess lactate that triggers histone H3K18 lactylation (H3K18la), establishing a pathogenic metabolic‐epigenetic axis in epilepsy. Elevated H3K18la enriches the Cop1 promoter, transcriptionally upregulating the E3 ubiquitin ligase COP1, which subsequently drives proteasomal degradation of GABAARβ2 and impairs ...
Yuan Meng   +8 more
wiley   +1 more source

E3 ubiquitin ligases in signaling, disease, and therapeutics

open access: yesTrends in Biochemical Sciences
The ubiquitin-proteasome system (UPS) is a central regulator of protein turnover and signaling, with E3 ubiquitin ligases conferring substrate specificity and chain-type control. Recent advances have revealed new mechanistic classes of E3 ligases and expanded our understanding of their roles in disease, including cancer, neurodegeneration, and immune ...
Pirouz Ebadi   +2 more
openaire   +2 more sources

Molecular Glue cc‐885 Inhibits VHL‐Deficient Clear Cell Renal Cell Carcinoma via ETS1 Degradation

open access: yesAdvanced Science, EarlyView.
VHL‐deficient kidney cancer lacks effective treatments. This study reveals that the molecular glue degrader cc‐885 hijacks the cellular recycling system to selectively destroy the oncogenic protein ETS1, effectively killing VHL‐mutant tumors. Combining CC‐885 with the approved drug belzutifan achieves powerful synergy, offering a promising new ...
Taowei Yang   +15 more
wiley   +1 more source

MDM2-C Functions as an E3 Ubiquitin Ligase.

open access: yesCancer management and research, 2020
Mouse double minute 2 (MDM2) is an E3 ubiquitin ligase that is over-expressed in many cancers and regulates target proteins through ubiquitination. Full-length MDM2 (MDM2-FL) is best known for targeting wild-type p53 for degradation by the proteasome, but the functions of the many splice variants of MDM2 are under-explored.
Kim,Jun Yeob   +4 more
openaire   +4 more sources

Characterisation of the ubiquitin E3 ligase COP1 [PDF]

open access: yes, 2018
Constitutive photomorphogenic 1 (COP1) is a ubiquitin E3 ligase that has been implicated in development of a variety cancers. The goal was to characterise the ubiquitin E3 ligase activity of COP1 and the relationship between COP1 and its interaction ...
Curry, Jack Richard
core   +1 more source

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