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Activity-based E3 ligase profiling uncovers an E3 ligase with esterification activity [PDF]

open access: yesNature, 2018
Ubiquitination is initiated by transfer of ubiquitin (Ub) from a ubiquitin-activating enzyme (E1) to a ubiquitin-conjugating enzyme (E2), producing a covalently linked intermediate (E2-Ub) 1 . Ubiquitin ligases (E3s) of the 'really interesting new gene' (
Virdee, Satpal; id_orcid   +19 more
core   +5 more sources

Structural Diversity of Ubiquitin E3 Ligase [PDF]

open access: yesMolecules, 2021
The post-translational modification of proteins regulates many biological processes. Their dysfunction relates to diseases. Ubiquitination is one of the post-translational modifications that target lysine residue and regulate many cellular processes ...
Sachiko Toma-Fukai, Toshiyuki Shimizu
core   +5 more sources

Discovery of E3 Ligase Ligands for Target Protein Degradation

open access: yesMolecules, 2022
Target protein degradation has emerged as a promising strategy for the discovery of novel therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a cellular ubiquitin-dependent proteolysis system for the efficient ...
Jaeseok Lee   +5 more
doaj   +2 more sources

A Comprehensive Atlas of E3 Ubiquitin Ligase Mutations in Neurological Disorders

open access: yesFrontiers in Genetics, 2018
Protein ubiquitination is a posttranslational modification that plays an integral part in mediating diverse cellular functions. The process of protein ubiquitination requires an enzymatic cascade that consists of a ubiquitin activating enzyme (E1 ...
Arlene J. George   +4 more
doaj   +2 more sources

IAPs as E3 ligases of Rac1 : shaping the move [PDF]

open access: yesSmall GTPases, 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   +4 more sources

Pharmacophore-based ML model to filter candidate E3 ligands and predict E3 Ligase binding probabilities

open access: yesInformatics in Medicine Unlocked
Among the plethora of E3 Ligases, only a few have been utilized for the novel PROTAC technology. However, extensive knowledge of the preparation of E3 ligands and their utilization for PROTACs is already present in several databases.
Reagon Karki   +4 more
doaj   +2 more sources

Pseudophosphatase as E3 ubiquitin ligase inhibitor

open access: yesScience Signaling, 2017
The pseudophosphatase STYX prevents the substrate recognition subunit FBXW7 from binding the catalytic E3 ubiquitin ligase complex.
Nancy R. Gough
core   +3 more sources

Emerging roles of the HECT E3 ubiquitin ligases in gastric cancer

open access: yesPathology and Oncology Research, 2023
Gastric cancer (GC) is one of the most pernicious gastrointestinal tumors with extraordinarily high incidence and mortality. Ubiquitination modification of cellular signaling proteins has been shown to play important roles in GC tumorigenesis ...
Aiqin Sun   +5 more
doaj   +1 more source

Differential requirement for BRCA1-BARD1 E3 ubiquitin ligase activity in DNA damage repair and meiosis in the Caenorhabditis elegans germ line.

open access: yesPLoS Genetics, 2023
The tumor suppressor BRCA1-BARD1 complex regulates many cellular processes; of critical importance to its tumor suppressor function is its role in genome integrity.
Qianyan Li   +4 more
doaj   +1 more source

Activity-based probe profiling of RNF12 E3 ubiquitin ligase function in Tonne-Kalscheuer syndrome

open access: yesLife Science Alliance, 2022
The authors use photocrosslinking activity-based probes to monitor RNF12/RLIM E3 ubiquitin ligase activity and report the impact of Tonne-Kalscheuer syndrome (TOKAS) patient variants on catalysis.
Francisco Bustos   +6 more
doaj   +1 more source

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