Discovery of Potent Mcl-1/Bcl-xL Dual Inhibitors by Using a ...
2013年11月11日 · Mcl-1 and Bcl-xL are crucial regulators of apoptosis, therefore dual inhibitors of both proteins could serve as promising new anticancer drugs. To design Mcl-1/Bcl-xL dual inhibitors, we performed structure-guided analyses of the corresponding selective Mcl-1 …
A computational perspective for tailor-made selective Mcl-1 and Bcl …
2022年4月5日 · In view of the crucial role of Mcl-1 in tumor survival and resistance as well as the importance of Bcl-XL in platelets homeostasis, an appropriate tuning of binding selectivity between Mcl-1 and Bcl-XL is crucial to discover safer anticancer candidates.
Co-targeting BCL-XL and MCL-1 with DT2216 and AZD8055
2023年1月2日 · We, therefore, aimed to develop an effective and safe strategy targeting these anti-apoptotic proteins with DT2216 (our platelet-sparing BCL-X L degrader) and AZD8055 (an mTOR inhibitor) to avoid...
Identification of BCL-XL as highly active survival factor and
2020年10月17日 · By RNA sequencing analysis of a pan-cancer cohort comprising >1500 patients and subsequent prediction of protein activity, BCL-XL was identified as the only antiapoptotic BCL-2 protein that is...
Mcl-1 and Bcl-xL cooperatively maintain integrity of ... - PubMed
Mcl-1 and Bcl-xL are two major anti-apoptotic Bcl-2 family proteins expressed in the liver and cooperatively control hepatic integrity during liver development and in adult liver homeostasis in a gene dose-dependent manner.
The identification of BCL-XL and MCL-1 as key anti-apoptotic
2023年10月28日 · Collectively, our study identifies that BCL-XL and MCL-1 are the key anti-apoptotic proteins in medulloblastoma, which mediate distinct protective roles. While BCL-XL has a first-line role in...
The identification of BCL-XL and MCL-1 as key anti-apoptotic
2023年10月28日 · Collectively, our study identifies that BCL-XL and MCL-1 are the key anti-apoptotic proteins in medulloblastoma, which mediate distinct protective roles. While BCL-XL has a first-line role in protecting cells from apoptosis basally, MCL-1 represents a second line of defence that compensates for BCL-XL upon its inhibition.
Expression Profile of BCL-2, BCL-XL, and MCL-1 Predicts ... - PubMed
In multiple myeloma cell lines (n = 21), BCL-2 is expressed but sensitivity to venetoclax correlated with high BCL-2 and low BCL-XL or MCL-1 expression. Multiple myeloma cells that coexpress BCL-2 and BCL-XL were resistant to venetoclax but sensitive to a …
QB | 前沿研究：线粒体凋亡通路中Bcl-2和Mcl-1“权重”的系统分析 …
2021年3月22日 · 文章系统分析了线粒体凋亡通路中Bcl-2和Mcl-1的“权重”问题，并建立了两个方程，以期绕过费事费力的实验筛选，找到癌症治疗的最佳药物组合。 文章通过ODEs模型（图1）研究了Bcl-2（在本研究中代表Bcl-2和Bcl-xL）和Mcl-1在细胞凋亡中的权重问题，并通过实验验证了该模型。 图1. 根据Bcl-2蛋白质相互作用制定的Bcl-2控制的MOMP（线粒体外膜通透性）数学模型。 该模型还显示Bcl-2表达水平、Mcl-1表达水平、Mcl-1产生和降解率是Bcl-2 和 Mcl-1依赖性 …
Mcl-1 and Bcl-xL are essential for survival of the developing
2018年10月25日 · We used Nestin-mediated, nervous system-specific conditional deletion of mcl-1, bcl-x or both to identify their distinct and overlapping roles. Individual conditional deletion of mcl-1 (MKO) and...