Menin-MLL1 Interaction Small Molecule Inhibitors: A Potential ...
2023年3月28日 · Encoded by the MEN1 gene, menin protein is a fusion protein that is essential for the oncogenic transformation of mixed-lineage leukemia (MLL) and leads to acute leukemia …
Menin抑制剂靶向急性髓性白血病又一亚型，潜力无限！ - 知乎
DS-1594是一种有效的选择性小分子menin抑制剂，被设计用于靶向和破坏menin和MLL的蛋白-蛋白相互作用，以抑制白血病细胞的生长和增殖。在临床前研究中，DS-1594显示出对AML …
Challenges and opportunities in targeting the menin-MLL interaction
Menin is an essential co-factor of oncogenic MLL fusion proteins and the menin-MLL interaction is critical for development of acute leukemia in vivo. Targeting the menin-MLL interaction with …
The menin-MLL1 interaction is a molecular dependency in
2022年2月10日 · Menin is critical for the proliferation and survival of MLL-rearranged (MLL-r) and NPM1-mutant (NPM1c) leukemia. 14,15 MLL1 and menin directly interact via a 5 amino acid …
Menin-MLL蛋白相互作用及相关抑制剂在 MLL 基因重排白血病中 …
分子机制研究发现，Menin蛋白是MLL-FP致白血病必不可少的辅助因子，通过与MLL-N端特定区域相互作用形成关键致病复合体，导致特定靶基因的异常表达。 这为Menin-MLL相互作用抑制 …
Menin–MLL1 Interaction Small Molecule Inhibitors: A Potential ...
The disruption of menin–MLL mediated by MI-503 results in the abrogation of OXPHOS-related gene transcription and a loss of cellular capacity to produce ATP. Members of the menin−MLL …
Disruption of the menin-MLL interaction triggers menin protein ...
Menin, a protein encoded by the MEN1 gene, suppresses cancers associated with multiple endocrine neoplasia type 1 (MEN1), but promotes the development of a subset of leukemia …
Menin-MLL蛋白相互作用及相关抑制剂在MLL基因重排白血病中应 …
混合谱系白血病(mixed lineage leukemia,MLL)基因重排(MLL-rearranged,MLL-r)引起的急性白血病亚型侵袭性高且预后不良,缺少特异性治疗手段.MLL蛋白具有组蛋白甲基转移酶活性,在胚胎发 …
Pharmacologic Inhibition of the Menin-MLL Interaction Blocks ...
2015年4月13日 · MLL fusion proteins require menin for leukemogenic activity, and selective targeting of the menin-MLL interaction represents a potential therapeutic approach for acute …
A Menin-MLL inhibitor induces specific chromatin changes and …
2019年12月9日 · Inhibition of the Menin (MEN1) and MLL (MLL1, KMT2A) interaction is a potential therapeutic strategy for MLL-rearranged (MLL-r) leukemia. Structure-based design …