Article ; Online: Modulation of Cullin-RING E3 ubiquitin ligase-dependent ubiquitination by small molecule compounds.
The Journal of biological chemistry
2024 Volume 300, Issue 3, Page(s) 105752
Abstract: Cullin (CUL)-RING (Really Interesting New Gene) E3 ubiquitin (Ub) ligases (CRLs) are the largest E3 family. The E3 CRL core ligase is a subcomplex formed by the CUL C-terminal domain bound with the ROC1/RBX1 RING finger protein, which acts as a hub that ... ...
Abstract | Cullin (CUL)-RING (Really Interesting New Gene) E3 ubiquitin (Ub) ligases (CRLs) are the largest E3 family. The E3 CRL core ligase is a subcomplex formed by the CUL C-terminal domain bound with the ROC1/RBX1 RING finger protein, which acts as a hub that mediates and organizes multiple interactions with E2, Ub, Nedd8, and the ARIH family protein, thereby resulting in Ub transfer to the E3-bound substrate. This report describes the modulation of CRL-dependent ubiquitination by small molecule compounds including KH-4-43, #33, and suramin, which target the CRL core ligases. We show that both KH-4-43 and #33 inhibit the ubiquitination of CK1α by CRL4 |
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MeSH term(s) | Animals ; Humans ; Mice ; beta Catenin/metabolism ; beta-Transducin Repeat-Containing Proteins/metabolism ; Cullin Proteins/metabolism ; Ligands ; Suramin/pharmacology ; Ubiquitin/metabolism ; Ubiquitin-Protein Ligases/genetics ; Ubiquitin-Protein Ligases/metabolism ; Ubiquitination/drug effects ; NEDD8 Protein/metabolism |
Chemical Substances | beta Catenin ; beta-Transducin Repeat-Containing Proteins ; BTRC protein, human ; CRBN protein, human ; CSNK1A1 protein, human (EC 2.7.11.1) ; CULL-RING ligase, human (EC 2.3.2.27) ; Cullin Proteins ; Ligands ; NEDD8 protein, human ; Suramin (6032D45BEM) ; Ubiquitin ; Ubiquitin-Protein Ligases (EC 2.3.2.27) ; NEDD8 Protein |
Language | English |
Publishing date | 2024-02-13 |
Publishing country | United States |
Document type | Journal Article |
ZDB-ID | 2997-x |
ISSN | 1083-351X ; 0021-9258 |
ISSN (online) | 1083-351X |
ISSN | 0021-9258 |
DOI | 10.1016/j.jbc.2024.105752 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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