WDR5-MYC-IN-1 (compound 4o) is an effective inhibitor of the WDR5-MYC interaction, demonstrating a Ki value of 1.0 µM and exhibiting antiproliferative activity. 体外活性 WDR5-MYC-IN-1(compound 4o)在多种细胞系中展现了抗增殖效果,其对RAJI、RAMOS、SUDHL4、HL-60、H1299细胞的IC50分别达到...
A MYC inhibitor selectively alters the MYC and MAX cistromes and modulates the epigenomic landscape to regulate target gene expression. Authors - Austin G Holmes View Article human WB,IF Proc Natl Acad Sci U S A Compensatory functions of histone deacetylase 1 (HDAC1) and HDAC2 regulate transcrip...
GlueFree——智能控糖微针贴片获“挑战杯”全国金奖糖响应胰岛素周制剂的制备及药效探究荣获第十五届全国大学生药苑论坛创新成果特等奖基于蛋白语言模型的新冠病毒演化趋势预测系统荣获“挑战杯”“揭榜挂帅”专项赛全国特等奖 WDR5/MYC结合抑制剂SXY12的发现及其作用机制研究全国大学生药苑论坛特等奖 04 通识教育白皮书...
WD repeat-containing protein 5 (WDR5)is a chromatin associated protein found in multiple chromatin regulatory complexes. It serves as an adaptor protein for these complexes and is particularly associated with MYC transcription factor and MLL1, a methyltransferase. ...
neuroblastomaWDR5WBM siteprotein-protein interaction interruptersdrug combination therapyNeuroblastoma is the most common and deadliest tumor in infancy. WDR5 (WD Repeat Domain 5), a critical factor supporting an N-myc transcriptional complex via its WBM site and interacting with chromosome via its ...
To ask whether WIN site inhibition impacts some or all of the functions of WDR5, we compared the effects of acute depletion of WDR5 with those of WIN site inhibition in Ramos cells, a Burkitt lymphoma line harboring a c-MYC translocation and expressing mutant p5328. Because both WDR5 loss...
Coimmunoprecipitation of endogenous MYC, MAX, and WDR5 proteins from HEK293 cells treated with proteasome inhibitor MG132 for 90 min. Extracts were subject to IP with antibodies against MYC, or an IgG control, and immunoblotted with the indicated antibodies. A total of 0.04% of the input is...
Currently, there are two main types therapeutic strategies for targeting c-Myc. One is to inhibit the transcriptional regulation of c-Myc, represented by the BET bromine domain inhibitor compound JQ1, but these compounds are only limited to the situation where the expression of c-Myc is driven ...
(non-specific lethal complex) for H4 lysine 16 acetylation (H4K16ac) [15, 17, 18], interacting with Oct4, Myc, p53 or lncRNAs to facilitate their target gene expression, controlling expression of genes related to protein 1MOE Key Laboratory of Biosystems Homeostasis & Protection, College of...
et al. WDR5 supports an N-Myc transcriptional complex that drives a protumorigenic gene expression signature in neuroblastoma. Cancer Res. 75, 5143–5154 (2015). 17. Wu, M. Z. et al. Interplay between HDAC3 and WDR5 is essential for hypoxia- induced epithelial-mesenchymal transition. Mol....