A novel photosensitizer berberine derivative B12 induces apoptosis and suppresses HIF-1α expression in colorectal cancer cells via mitochondria-to-nucleus sequential-targeting [0.03%]
新型光敏剂小分子B12诱导结直肠癌细胞凋亡及抑制HIF-1α表达的线粒体至细胞核序贯靶向作用机制研究
Wen-Bin Pei,Zi-Yu Lei,Fu-Quan Xie et al.
Wen-Bin Pei et al.
Photodynamic therapy (PDT) boasts the advantages of high spatiotemporal selectivity and non-invasiveness, but its clinical application is still limited by the hypoxic tumor microenvironment and inherent drawbacks of traditional photosensiti...
Zinc finger BED-type containing 6 (ZBED6) ameliorates cardiac fibrosis by inhibiting Piezo1 transcription and YAP nuclear translocation [0.03%]
锌指BED型含有6(ZBED6)通过抑制Piezo1转录和YAP核转位改善心脏纤维化
Han Wu,Wei-Tao Jiang,Qiao-Yue Zhao et al.
Han Wu et al.
Cardiac fibroblasts progressively replace deceased cardiomyocytes during the development of myocardial fibrosis, an irreversible pathological repair process that ultimately leads to cardiac dysfunction and heart failure. Cardiac injury was ...
Morchella polysaccharide ameliorates myocardial infarction inflammation in mice through increasing gut microbiota-derived 12-HEPE [0.03%]
狼毒素多糖通过增加肠道菌群衍生的12-HEPE来改善小鼠心肌梗死后炎症反应
Hui-Min Su,Jia-Xin Li,Jun-Fang Wu et al.
Hui-Min Su et al.
Myocardial infarction (MI) initiates robust inflammatory responses. While moderate inflammation facilitates the clearance of necrotic debris, sustained inflammation promotes fibrosis and exacerbates MI progression. Fungal polysaccharides ha...
Cryo-EM structures of GPR75 reveal an occluded orthosteric pocket challenging conventional drug discovery paradigms for an anti-obesity target [0.03%]
冷冻电镜下GPR75结构揭示了闭合的内源性配体口袋，为抗肥胖靶点药物发现提出了挑战
Zi-Ning Zhu,Chong-Zhao You,Qing-Ning Yuan et al.
Zi-Ning Zhu et al.
The global obesity epidemic, affecting over 650 million adults, demands innovative therapeutics. GPR75 has emerged as a promising anti-obesity target, with genetic evidence linking loss-of-function variants to protection against obesity and...
A sinomenine derivative protects life-threatening inflammatory injuries via covalently binding to a novel allosteric inhibition site of IRF3 [0.03%]
一类新的异环糊精通过共价修饰IRF3的新型变构抑制位点发挥保护生命威胁性炎症损伤的作用
Shuo Li,Bing Xu,Ming-Jun Lu et al.
Shuo Li et al.
The severe inflammation associated with infectious or inflammatory diseases significantly contributes to mortality. Interferon regulatory factor 3 (IRF3) represents a potential anti-inflammatory target, but the development of IRF3 inhibitor...
Targeting intrinsic and CAF-mediated signaling by PI3Kα inhibitor CYH33 attenuated metastasis in lung squamous cell carcinoma [0.03%]
I型PI3K抑制剂CYH33通过靶向肿瘤内在和CAF介导的信号通路抑制肺鳞状细胞癌转移
Xiao-Yu Ma,Jie-Ting Deng,Zhe-Rui Cao et al.
Xiao-Yu Ma et al.
Aberrant activation of PI3K signaling is frequently observed in lung squamous cell carcinoma (LUSC) and is strongly associated with metastasis in advanced-stage patients, but the therapeutic efficacy of PI3K inhibitors and underlying mechan...
UBC9-mediated p53 SUMOylation drives tubular senescence and exacerbates acute kidney injury in mice [0.03%]
UBC9介导的p53SUMO化驱动肾小管衰老并加重小鼠急性肾脏损伤
Qi-Mei Wu,Jing Liu,Ying-Song Mu et al.
Qi-Mei Wu et al.
The pathogenesis of acute kidney injury (AKI) is closely related to the senescence of renal tubular epithelial cells (RTECs). The role of small ubiquitin-like modification (SUMOylation) in cellular stress and senescence has been gradually e...
Discovery of a potent and orally bioavailable type Ⅰ PRMTs inhibitor for triple-negative breast cancer treatment [0.03%]
用于治疗三阴性乳腺癌的高效口服生物可利用的一型蛋白精氨酸甲基转移酶抑制剂的发现
Shu-Yan Zhou,Qiang-Sheng Zhang,Lu Li et al.
Shu-Yan Zhou et al.
Triple-negative breast cancer (TNBC) remains the most refractory breast cancer subtype because of its high invasiveness, lack of therapeutic targets and heterogeneity. Type I protein arginine methyltransferases (PRMTs) are important epigene...
PLN-L31A/I40A for the treatment of inherited heart disease caused by PLN-R14del mutations [0.03%]
PLN-L31A/I40A治疗PLN-R14del突变引起的遗传性心脏病
Zi-Yang Chen,Ren Guo,Min Wang et al.
Zi-Yang Chen et al.
Phospholamban (PLN) is a regulatory protein of the SERCA2α calcium transporter, which plays an important role in maintaining calcium homeostasis in cardiomyocytes. Deletion of the 14th arginine of PLN (PLN-R14del) leads to dysregulation of...
MicroRNA-129-5p in the mPFC is involved in the chronic mild stress-induced depression-like behaviors in rats [0.03%]
外侧缰核控制攻击行为的神经环路机制研究
Jing-Yi Xu,Chen-Chen Li,Hao-Chen Zhang et al.
Jing-Yi Xu et al.
Current treatments for depression have focused on improving the dysregulated monoamine neurotransmitter systems in the brain. However, the conventional antidepressants based on the monoamine hypothesis usually exert side effects and unsatis...