Shikonin suppresses diffuse large B-cell lymphoma progression by inducing ferritinophagy and ferroptosis via lncRNA ADPGK-AS1 downregulation [0.03%]
芍药苷通过下调长链非编码RNA ADPGK-AS1诱导铁死亡自噬从而抑制弥漫性大B细胞淋巴瘤进展
Can Chen,Xiaofei Chen,Xilian Huang et al.
Can Chen et al.
Shikonin, a natural compound, exhibits antitumor effects in DLBCL, but its mechanism remains unclear. Shikonin's cytotoxicity in DLBCL cells was assessed by MTT assays. Ferroptosis and lipid peroxidation markers were analysed via flow cytom...
Discovery of a novel and potent KRASG12V-targeting peptide with antiproliferative activity against colorectal cancer cells [0.03%]
一种针对KRASG12V的新型抗增殖多肽及其对结直肠癌细胞的作用研究
Hai Zhang,Shudan Yang,Yuting Wang et al.
Hai Zhang et al.
Despite the clinical relevance of KRASG12V in colorectal cancer, KRASG12V-specific inhibitors remain limited. Through structure-based virtual screening of a 59,319-member peptide library, we identified four KRASG12V-targeting peptides, amon...
Lidocaine enhances antitumor effects of sorafenib and GW5074 in colorectal cancer cells [0.03%]
利多卡因增强索拉非尼和GW5074在结直肠癌细胞中的抗肿瘤效应
Tzu-Chiao Lin,Zih-Syuan Wu,Shih-Ming Huang et al.
Tzu-Chiao Lin et al.
Targeted therapies have broadened the treatment landscape for colorectal cancer (CRC), highlighting the need for rational combination strategies. Although sorafenib and GW5074 show therapeutic promise and lidocaine may sensitise cancer cell...
Design, synthesis, and anti-inflammatory evaluation of novel analogues derived from the natural product reticuline [0.03%]
来源于天然产物网地辛的新型类似物的设计、合成及抗炎活性评价
Yanyan Feng,Tong Li,Cheng Chen et al.
Yanyan Feng et al.
The natural alkaloid reticuline exhibits promising anti-inflammatory activity in preclinical models; however, its development is hindered by moderate potency and limited accessibility. To overcome these hurdles, we developed an efficient sy...
Targeting the BMX in cancer: molecular mechanisms and emerging therapeutic strategies [0.03%]
癌症中的BMX靶向治疗：分子机制和新兴的治疗策略
Man Zhang,Jinchi Chen,Rong Liang et al.
Man Zhang et al.
Bone Marrow Tyrosine Kinase on Chromosome X (BMX), also known as epithelial/endothelial cell kinase (ETK), is a core member of the Tec family of non-receptor tyrosine kinases. Structurally, BMX kinase contains an N-terminal PH domain, a BH ...
Design, synthesis, anticancer activity, and mechanistic investigation of 4,5,6,7-tetrahydrobenzo[ b]thiophene carboxamides as CDK-2 inhibitors: in vitro and in silico DFT and molecular docking study [0.03%]
设计、合成及抗癌活性和机制研究：作为CDK-2抑制剂的4,5,6,7-四氢苯并噻吩类羧酸胺：体外实验以及基于密度泛函理论与分子对接的计算模拟研究
Kurls E Anwer,Ramadan M Ramadan,Eman S Nossier et al.
Kurls E Anwer et al.
Utilising drug design methodologies including bioisosteric modification and substituents variation, sets of 4,5,6,7-tetrahydrobenzo[b]thiophene carboxamides were synthesised, by conventional heating and eco-friendly microwave-assisted techn...
Discovery of azaindole/indole-fused pyrimidine tetracyclic scaffolds as novel potent CDK7 inhibitors [0.03%]
新型 potency CDK7抑制剂的aza-indole/indole拼杂嘧啶四环骨架的研究发现
Fan Pu,Axiao Tao,Pengxiang Qiu et al.
Fan Pu et al.
CDK7 has emerged as a highly promising anticancer target, as its dual indispensable roles in cell cycle progression and transcriptional regulation for cancer cell proliferation and survival. Herein, we describe the rational design and ident...
Design and Pictet-Spengler enabled synthesis of carboxamide-substituted imidazo[1,2- a]quinoxalines as dual EGFR and tubulin targeting anticancer agents [0.03%]
设计并通过Pictet-Spengler反应合成带有羧胺取代基的imidazo[1,2-a]quinoxaline类化合物作为靶向EGFR和微管的抗肿瘤药物
Joydeep Chatterjee,Gaurav Joshi,Vibhu Jha et al.
Joydeep Chatterjee et al.
In this study, we report the Pictet-Spengler enabled synthesis of a series of eighteen carboxamide-substituted imidazo[1,2-a]quinoxaline derivatives (JRC-1-JRC-18) targeting epidermal growth factor receptor (EGFR) and tubulin. Compounds JRC...
Systematic identification of bacterial neuraminidase inhibitors from Psoralea corylifolia using ultrafiltration-UPLC-Q-Orbitrap-MS and molecular dynamics [0.03%]
利用超滤-超高性能液相色谱- Orbit 持久性自由基质谱及分子动力学系统地筛选补骨脂中抗细菌神经氨酸酶的成分
Yu Jin Kim,Seol Jang,Youn-Hwan Hwang
Yu Jin Kim
Bacterial neuraminidase (BNA) is a potential target for discovering anti-infective agents. Here, the BNA inhibitory activity of the ethanolic extract of Psoralea corylifolia (EEPC) was investigated using integrated experimental and computat...
Mechanisms of traditional Chinese medicine in enhancing the efficacy and reducing the toxicity of immune checkpoint inhibitors via regulation of the tumor microenvironment and gut microbiota [0.03%]
通过调节肿瘤微环境和肠道菌群增强免疫检查点抑制剂疗效和降低毒性的中医药作用机制
Junying Pan,Liying Yang,Haoyu Wang et al.
Junying Pan et al.
Immune checkpoint inhibitors (ICIs) face challenges of drug resistance and immune-related adverse events (irAEs). Traditional Chinese medicine (TCM)-including single herbs, compounds, and active monomers-enhances ICI efficacy and reduces to...