Fourth-generation EGFR-TKI to overcome C797S mutation: past, present, and future [0.03%]
克服C797S突变的第四代EGFR-TKI：过去、现在和未来
Die Zhang,Jumei Zhao,Yue Yang et al.
Die Zhang et al.
Overactivation of the epidermal growth factor receptor (EGFR) is prevalent in various tumours, rendering it a promising target for cancer therapy, particularly in the treatment of non-small cell lung cancer (NSCLC). Although the first throu...
Discovery and development of steroidal enzyme inhibitors as anti-cancer drugs: state-of-the-art and future perspectives [0.03%]
类固醇酶抑制剂抗肿瘤药物的研究与开发：现状及未来展望
Bruno Cerra,Antimo Gioiello
Bruno Cerra
Steroidal compounds have emerged as effective therapeutic agents in oncology. Beyond natural-occurring and synthetic steroids that act as cytotoxic anti-tumoral agents, steroidal derivatives can be designed to mime the endogenous substrates...
Discovery of a novel PLK1 inhibitor with high inhibitory potency using a combined virtual screening strategy [0.03%]
结合虚拟筛选策略发现了一种新型PLK1抑制剂具有很强的抑制功效
Zhen Xu,Lixia Guan,Yuting Wang et al.
Zhen Xu et al.
PLK1 is essential for cell cycle regulation and proliferation, and its elevated expression in prostate cancer is associated with high tumour grade. Therefore, PLK1 inhibition is considered a promising strategy for the treatment of prostate ...
Rational design, synthesis, and molecular modelling insights of dual DNA binders/DHFR inhibitors bearing arylidene-hydrazinyl-1,3-thiazole scaffold with apoptotic and anti-migratory potential in breast MCF-7 cancer cells [0.03%]
具有细胞凋亡和抗迁移潜能的双重DNA结合剂/二氢叶酸还原酶抑制剂的理性设计、合成及分子建模研究以及在乳腺癌MCF-7细胞中的应用
Marwa H El-Wakil,Rasha A Ghazala,Hadeel A El-Dershaby et al.
Marwa H El-Wakil et al.
In light of searching for new breast cancer therapies, DNA-targeted small molecules were rationally designed to simultaneously bind DNA and inhibit human dihydrofolate reductase (hDHFR). Fourteen new arylidene-hydrazinyl-1,3-thiazoles (5-18...
Design and synthesis of novel HDAC6 inhibitor dimer as HDAC6 degrader for cancer treatment by palladium catalysed dimerisation [0.03%]
通过钯催化的二聚化设计合成新型HDAC6抑制剂二聚体作为HDAC6降解物用于癌症治疗
Ching Lin,Jui-Ling Hsu,Yu-Tung Hsu et al.
Ching Lin et al.
The enigmatic histone deacetylase 6 (HDAC6) is one of a kind among its family. Recent reports revealed that HDAC6 CD1 exhibits E3 ligase activity. Inspired by these researches, we attempted to develop drugs targeting HDAC6 via novel mechani...
Natural product as a lead for impairing mitochondrial respiration in cancer cells [0.03%]
天然产物作为影响癌细胞线粒体呼吸的先导化合物
Agnieszka Pyrczak-Felczykowska,Anna-Karina Kaczorowska,Artur Giełdoń et al.
Agnieszka Pyrczak-Felczykowska et al.
The impact of the isoxazole derivative of usnic acid, ISOXUS (formerly known as 2b) on cancer and non-cancerous cell metabolism was investigated. ISOXUS significantly reduced the utilisation of most metabolic substrates that produce NADH or...
Synthesis and evaluation of 5, 6-dihydro-8 H-isoquinolino[1, 2- b]quinazolin-8-one derivatives as novel non-lipogenic ABCA1 up-regulators with inhibitory effects on macrophage-derived foam cell formation [0.03%]
5,6-二氢-8H-异喹啉并[1,2-b]喹唑啉-8-酮衍生物的合成与评价：作为一种新型非脂质生成的ABCA1上调剂，可抑制巨噬细胞来源泡沫细胞形成
Changhuan Yang,Lin Chen,Yanmei Jiang et al.
Changhuan Yang et al.
Increasing the expression of ATP-binding cassette transporter A1 (ABCA1) can lower cellular cholesterol levels and prevent foam cell formation. In this study, a series of 5, 6-dihydro-8H-isoquinolino[1, 2-b]quinazolin-8-one derivatives were...
A stable GH31 α-glucosidase as a model system for the study of mutations leading to human glycogen storage disease type II [0.03%]
稳定的GH31葡萄糖淀粉酶作为研究导致人类II型糖原贮积病的突变的模型系统
Roberta Iacono,Francesca Maria Pia Paragliola,Andrea Strazzulli et al.
Roberta Iacono et al.
GH31 glycosidases are widespread across organisms, but remarkably, less than 1% of them have been biochemically characterised to date. Among them, human lysosomal acid α-glucosidase (GAA) stands out due to its link to Pompe disease, a rare...
Discovery of a selective PI3Kα inhibitor via structure-based virtual screening for targeted colorectal cancer therapy [0.03%]
通过基于结构的虚拟筛选发现选择性的PI3Kα抑制剂用于结肠癌靶向治疗
Hussam Albassam,Omar Almutairi,Majed Alnasser et al.
Hussam Albassam et al.
Colorectal cancer (CRC) remains a leading cause of cancer-related mortality globally, driving an urgent need for effective therapies. A promising avenue of research focuses on the PI3K/AKT/mTOR signalling pathway, which is frequently disrup...
Bioactivity profiling of Sanghuangporus lonicerinus: antioxidant, hypoglycaemic, and anticancer potential via in-vitro and in-silico approaches [0.03%]
桑黄的生物活性谱：通过体外和计算机模拟方法评估其抗氧化，降血糖和抗癌潜能
Yusufjon Gafforov,Sofija Bekić,Manzura Yarasheva et al.
Yusufjon Gafforov et al.
This study investigates the mycochemical profile and biological activities of hydroethanolic (EtOH), chloroform (CHCl3), and hot water (H2O) extracts of Sanghuangporus lonicerinus from Uzbekistan. Antioxidant capacity was assessed using 2,2...