YAP/TAZ–TEAD为何成为Hippo通路新的突破口?
Hippo通路是调控组织生长、细胞增殖和组织稳态的重要信号网络,其下游YAP/TAZ–TEAD转录模块与多种肿瘤的发生、进展及治疗耐受密切相关。随着TEAD脂质结合口袋和YAP/TAZ–TEAD互作界面的可成药性逐渐明确,这一转录模块正在成为Hippo通路靶向研究的重要突破口。 ...
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Hippo通路是调控组织生长、细胞增殖和组织稳态的重要信号网络,其下游YAP/TAZ–TEAD转录模块与多种肿瘤的发生、进展及治疗耐受密切相关。随着TEAD脂质结合口袋和YAP/TAZ–TEAD互作界面的可成药性逐渐明确,这一转录模块正在成为Hippo通路靶向研究的重要突破口。 ...
The Hippo pathway is an important signaling network that regulates tissue growth, cell proliferation, and tissue homeostasis. Its downstream YAP/TAZ–TEAD transcriptional module is closely associated with the initiation, progression, and treatment resistance of multiple tumors. As the ...
LYSET is an important Golgi membrane protein that maintains the correct trafficking of lysosomal enzymes by regulating GNPT and the mannose-6-phosphate pathway. Under nutrient-limited conditions, some cancer cells depend on lysosomal degradation of extracellular proteins to obtain amino acids, ...
LYSET是维持溶酶体酶正确运输的重要高尔基体膜蛋白,可通过调控GNPT和甘露糖-6-磷酸通路维持溶酶体降解能力。部分肿瘤细胞在营养匮乏环境中依赖溶酶体分解胞外蛋白获取氨基酸,使LYSET成为连接溶酶体功能与癌细胞代谢适应的重要研究靶点。 ...
ENPP1是位于细胞外核苷酸代谢网络中的膜结合酶,可降解肿瘤来源的2′,3′-cGAMP,并通过AMP–CD73途径促进腺苷生成。靶向ENPP1可保护细胞外cGAMP,恢复其对宿主免疫细胞STING通路的激活。
ENPP1 is a membrane-associated enzyme in the extracellular nucleotide-metabolism network that can degrade tumor-derived 2′,3′-cGAMP and promote adenosine production through the AMP–CD73 pathway. Targeting ENPP1 protects extracellular cGAMP and restores its ability to activate the STING pathway ...
KRAS G12D is an important driver mutation in solid tumors such as pancreatic, colorectal, and lung cancers. The emergence of molecules such as MRTX1133 has demonstrated that KRAS G12D can be directly targeted pharmacologically, whereas targeted protein degradation technologies such as PROTACs ...
KRAS G12D是胰腺癌、结直肠癌和肺癌等实体瘤中的重要驱动突变。MRTX1133等分子的出现证明了KRAS G12D可以被直接药理干预,而PROTAC等靶向蛋白降解技术进一步将作用模式从“占据并抑制KRAS”推进到“募集E3连接酶并清除KRAS蛋白”。
神经干细胞具有自我更新和多向神经分化能力,可通过细胞替代、再髓鞘化、神经营养和神经回路重建促进损伤后功能恢复。随着神经干/祖细胞及iPSC来源细胞进入临床研究,细胞移植正成为神经再生的重要研究方向。