Structure-based screening and identification of a novel Aurora-A-targeting peptide with antiproliferative activity against prostate cancer cells [0.03%]
基于结构的筛选和鉴定针对前列腺癌细胞的新型Aurora-A靶向肽
Bei-Bei Huang,Haijing Jiang,Yaozhi Hu et al.
Bei-Bei Huang et al.
Aurora-A is a potential therapeutic target in prostate cancer. In this study, virtual screening identified four Aurora-A-targeting peptides, among which Peptide-1 showed the most favourable profile. Molecular docking and MST assays demonstr...
Recent progress in small molecules targeting the acidic tumor microenvironment [0.03%]
靶向肿瘤酸毒微环境的小分子研究进展
Yinuo Fu,Jiahui Song,Chenyang Yu et al.
Yinuo Fu et al.
The acidic tumour microenvironment (pHe 6.5-6.9) is sustained by the Warburg effect and pH regulators, such as monocarboxylate transporters 1 and 4, Na+/H + exchanger 1, vacuolar ATPase, and carbonic anhydrases IX and XII. This environment ...
Context matters in PROTAC design: navigating the trade-off between degradation and developability [0.03%]
上下文影响PROTAC设计：在降解和可开发性之间进行权衡
Boxin Zhang,Yunfei Zhang,Bingxing Zhang et al.
Boxin Zhang et al.
Proteolysis-targeting chimaeras (PROTACs) couple target recognition to ubiquitin-dependent degradation, but their translation requires coordinated optimisation of degradation efficiency and developability. This review frames PROTAC design a...
Solvent-controlled Rh-catalysed hydrodehalogenation and construction of phenanthridinone skeleton from a common precursor in one-step sequence and the antitumor activity of its derivatives [0.03%]
一种前体一步构建螺缩酮并菲啶酮骨架及其衍生物抗肿瘤活性研究
De-Xuan Hu,Chao Qin,Xiang Gao et al.
De-Xuan Hu et al.
Herein, we report a solvent-controlled, operationally convenient and highly efficient rhodium(II)-catalysed protocol enabling hydrodehalogenation and phenanthridinone skeleton construction from 2-halobenzamide. This methodology facilitates ...
Virtual screening and experimental validation of a METTL3-targeting peptide with in vitro antiproliferative activity against non-small cell lung cancer cells [0.03%]
虚拟筛选及实验验证METTL3靶向肽并对其体外抗非小细胞肺癌活性进行评价
Ying Dai,Hanying Wu,Yahui Shen et al.
Ying Dai et al.
The METTL3-METTL14 protein-protein interaction (PPI) plays an important role in tumour progression, and disruption of this interaction has been explored as a potential strategy. In this study, four peptides were identified from a peptide da...
A novel approach to improving solubility of drugs: chelation-assisted solubility enhancement (CHASE) [0.03%]
一种改善药物溶解度的新方法：螯合辅助溶解度增强（CHASE）
TanPhat Nguyen,Nicola Bauer,Samer Gozem et al.
TanPhat Nguyen et al.
We explore a novel concept of metal Chelation-assisted Solubility Enhancement (CHASE). This study is based on complexation with Na+ or K+. A series of 6 compounds are studied by conjugating a hydrophobic moiety with benzo-15-crown-5. LogP v...
Exploration of tropocollagen unwinding by cathepsin K dimer with chondroitin 4-sulphate through microsecond timescale molecular dynamics [0.03%]
微秒时间尺度上的分子动力学模拟研究硫酸软骨素介导的基质内胶原降解中cathepsin K二聚体的作用机制
Mengyi Shan,Yue Wu,Chen Jiang et al.
Mengyi Shan et al.
Cathepsin K (CatK), a promising therapeutic target for bone-related diseases, uniquely unfolds triple-helical collagen and digests tropocollagen into soluble peptides in the presence of chondroitin 4-sulphate (C4-S). However, the molecular ...
A comprehensive review of small molecule drugs approved by the FDA in 2025: advance and prospect [0.03%]
2025年FDA批准的小分子药物全面回顾：进展与前景
Yi-Ru Bai,Ruifang Li,Xin-Hui Zhang et al.
Yi-Ru Bai et al.
In 2025, the FDA approved 46 drug marketing applications, 31 of which were small molecule drugs. Despite the advancements in biotechnologies such as antibody drugs, RNA-based treatments, and antibody-drug conjugates, small molecule drugs re...
Trichodermin exhibits potent anti-glioblastoma activity by inducing cell cycle arrest and apoptosis, suppressing invasion, and enhancing temozolomide efficacy [0.03%]
曲霉三酮通过诱导细胞周期阻滞和凋亡、抑制侵袭和增强替莫唑胺疗效对胶质母细胞瘤具有较强的活性
Hung-Pei Tsai,Tzong-Huei Lee,Hong-Liang Lin et al.
Hung-Pei Tsai et al.
Trichodermin, a sesquiterpene antibiotic from Trichoderma species, shows anticancer potential. In this study, anti-glioblastoma activity was evaluated by (3-(4,5-di methyl thiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay, colony f...