Investigating the role of cytochrome bd oxidases in the antibacterial activity of madecassic acid and derivatives thereof [0.03%]
穿心莲内酯衍生物抗菌活性的作用机制研究
Samantha A Henry,Geraud N Sansom,Thao Thi Phuong Tran et al.
Samantha A Henry et al.
Natural products are valuable starting points for drug discovery, although individual modes of action are often difficult to pin down. Ursanes such as madecassic acid have been shown to have antibacterial properties, but a variety of mechan...
Kupffer cell M2-like polarization increases liver metastatic burden via the uptake of exosomal KRAS mutant protein from hypoxic colorectal carcinoma cells [0.03%]
库普弗细胞M2型极化通过摄取缺氧结直肠癌细胞释放的含KRAS突变蛋白外泌体促进肝转移负担增加
Yu You,Zhihao Feng,Jiao Lu et al.
Yu You et al.
Background: this study investigates the metastasis-promoting effect of colorectal carcinoma cell-derived exosomes in liver metastasis, M2-like polarization of Kupffer cells, and the underlying mechanism. Methods: mouse liver metastasis mode...
Targeted degradation of Pin1 by an antagonistic peptide enhances gemcitabine therapy in pancreatic cancer [0.03%]
靶向胰腺癌PIN1的拮抗肽增强吉西他滨治疗效果
Mengting Chen,Xiangyu Chu,Haipeng Zhao et al.
Mengting Chen et al.
Targeted protein degradation (TPD) has emerged as a powerful strategy for eliminating disease-causing proteins. The prolyl isomerase Pin1 is an attractive therapeutic target given its oncogenic function. Here, we develop PIPWF, a novel pept...
Sterically hindered catechol-derived Schiff bases: design, synthesis, SAR analysis and mechanisms of the antioxidant activity [0.03%]
合成受限的儿茶酚衍生物希夫碱：设计、合成、构效关系分析及抗氧化活性机制研究
Maxim Gvozdev,Iveta Turomsha,Nikolai Osipovich et al.
Maxim Gvozdev et al.
Sterically hindered phenols represent a fascinating class of redox-active compounds with unique radical regulatory properties. In this comprehensive study, we explored the in vitro antioxidant activity of 24 novel sterically hindered catech...
Parallels between the chloro and methoxy groups for potency optimization [0.03%]
氯代和甲氧基团在活性优化中的相似性研究
Debora Chiodi,Yoshihiro Ishihara
Debora Chiodi
Small substituents such as chloro (Cl), fluoro, methyl, and methoxy (OCH3) are often used in drug discovery to optimize ligand-protein interactions. Even though Cl is an electron-withdrawing group and OCH3 is an electron-donating group exer...
Small molecule-mediated spatial targeting of mitochondria and the Golgi apparatus in cancer cells [0.03%]
小分子介导的癌细胞中线粒体和高尔基体的空间靶向
Phanindra Kumar,Asima Sahu,Tripti Mishra et al.
Phanindra Kumar et al.
Cancer remains one of the most dynamic and complex diseases, driven by intricate interplay and cross-talk among various sub-cellular organelles. Among these, mitochondria and the Golgi apparatus (GA) have garnered significant attention due ...
Strategies to inhibit steroid cytochrome P450 enzymes to benefit human health: development of steroid ligands for P450s 17A1, 19A1, and 8B1 to treat cancer and obesity [0.03%]
抑制类固醇细胞色素P450酶以造福人类健康的策略：开发用于治疗癌症和肥胖症的P450 17A1、19A1及8B1类固醇配体
Tu M Ho,Francis K Yoshimoto
Tu M Ho
Several human cytochrome P450 enzymes (P450s) found in steroid/oxysterol biosynthesis are therapeutic targets to treat disease. This review article describes current research strategies to develop various inhibitors of three steroid P450s (...
Potent and selective indole-based inhibitors targeting disease-transmitting mosquitoes [0.03%]
一类高效且具有高度选择性的针对传播疾病的蚊虫的吲哚类抑制剂
R Rajeshwari,V Duvauchelle,C Lindgren et al.
R Rajeshwari et al.
Vector control with insecticides is an important preventive measure against mosquito-borne infectious diseases, such as malaria and dengue. The intensive usage of few insecticides has resulted in emerging resistance in mosquitoes, and unwan...
Ferrocenyl ferroptosis inducers as an emerging class of anticancer agents: a mini review [0.03%]
含铁烃基诱导剂作为一类新兴的抗癌剂：迷你综述
Mateusz Klarek,Aryan Gautam,Konrad Kowalski
Mateusz Klarek
Ferroptosis is one of the regulated cell death pathways. Molecular mechanisms underlying ferroptosis involve iron-dependent lipid peroxidation, which results in cell-deleterious membrane damage. Ferroptosis-inducing agents have been identif...
Novel Pt@BSA nanoparticles improve radiotherapeutic outcomes in breast cancer [0.03%]
新型Pt @ BSA纳米颗粒可改善乳腺癌的放射治疗效果
Yuhui Zhang,Yihui Liu,Dongju Zheng
Yuhui Zhang
Radiotherapy is a standard treatment for breast cancer, but its therapeutic efficacy is often limited by tumor radioresistance and systemic toxicity. Hence, the development of effective radiosensitizers with favorable biocompatibility is ur...