Anticancer drug discovery by targeting cullin neddylation
نویسندگان
چکیده
منابع مشابه
miR-148b-3p promotes migration of Schwann cells by targeting cullin-associated and neddylation-dissociated 1
MicroRNAs (miRNAs) are small, non-coding RNAs that negatively adjust gene expression in multifarious biological processes. However, the regulatory effects of miRNAs on Schwann cells remain poorly understood. Previous microarray analysis results have shown that miRNA expression is altered following sciatic nerve transaction, thereby affecting proliferation and migration of Schwann cells. This st...
متن کاملThe TFIIH subunit Tfb3 regulates cullin neddylation.
Cullin proteins are scaffolds for the assembly of multisubunit ubiquitin ligases, which ubiquitylate a large number of proteins involved in widely varying cellular functions. Multiple mechanisms cooperate to regulate cullin activity, including neddylation of their C-terminal domain. Interestingly, we found that the yeast Cul4-type cullin Rtt101 is not only neddylated but also ubiquitylated, and...
متن کاملEDITORIALS Anticancer Drug Discovery
The National Cancer Institute's (NCI's) human tumor cell line panel for screening potential new anticancer drugs is now operational (/). Its implementation and the demonstration of its feasibility represent a technical and organizational tour de force. The rationale for the change in the primary screen from leukemias in mice to the array of 60 human cancer cell lines was earlier debated in cont...
متن کاملTargeting Cullin–RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation
In the last decade, the ubiquitin-proteasome system has emerged as a valid target for the development of novel therapeutics. E3 ubiquitin ligases are particularly attractive targets because they confer substrate specificity on the ubiquitin system. CRLs [Cullin-RING (really interesting new gene) E3 ubiquitin ligases] draw particular attention, being the largest family of E3s. The CRLs assemble ...
متن کاملThe Discovery of a Reciprocal Relationship between Tyrosine-Kinase Signaling and Cullin Neddylation
While neddylation is known to activate cullin (CUL)-RING ubiquitin ligases (CRLs), its role in regulating T cell signaling is poorly understood. Using the investigational NEDD8 activating enzyme (NAE) inhibitor, MLN4924, we found that neddylation negatively regulates T cell receptor (TCR) signaling, as its inhibition increases IL-2 production, T cell proliferation and Treg development in vitro....
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ژورنال
عنوان ژورنال: Acta Pharmaceutica Sinica B
سال: 2020
ISSN: 2211-3835
DOI: 10.1016/j.apsb.2019.09.005