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...
Pharmacological advances in Candida auris: emerging antifungal mechanisms and next-generation therapeutic strategies [0.03%]
药理学在耳念珠菌研究中的进展：新型抗真菌机制和下一代治疗策略
Shuaibu Abdullahi Hudu,Najlaa Saadi,Emad A Morad et al.
Shuaibu Abdullahi Hudu et al.
Candida auris is a major public health concern worldwide due to its efficient transmission, environmental persistence, and broad resistance to approved antifungal classes. This review consolidates recent pharmacological developments in this...
A multipurpose probe for identification and mechanistic analysis of prenylation inhibitors [0.03%]
一种用于异戊二烯基化抑制剂鉴定和机理分析的多功能探针
Ruba Yehia,Moshe Giladi,Yoni Haitin
Ruba Yehia
Protein prenylation is a critical post-translational modification that controls many cancer-related signalling pathways and represents an important therapeutic target currently lacking effective pharmacological agents. Here, we establish th...
Discovery of a novel STING-binding peptide associated with reduced cGAMP-induced inflammatory gene expression [0.03%]
一种新型的STING结合肽与降低cGAMP诱导的炎性基因表达有关的发现
Junling Lu,Rui Dong,Shudan Yang et al.
Junling Lu et al.
cGAMP-induced STING activation contributes to inflammatory and interferon-related signalling, making STING a relevant target for inhibitor development. In this study, a 59,319-sequence peptide library was screened against STING by molecular...
Influence of adrenomedullin on the enzymatic activity of dipeptidyl peptidase 3 in vitro [0.03%]
肾上腺髓质素对自由基引发的DNA损伤和体外二肽基肽酶3酶活性的影响
Ruqayyah Nissen,Amin Yourdkhani,Marie-Louise Hollerbach et al.
Ruqayyah Nissen et al.
Circulating Dipeptidyl Peptidase 3 (DPP3) hydrolyses dipeptides from the amino terminus of its substrates and excess levels represent a target for the treatment of cardiogenic shock. Known substrates include Angiotensin II (Ang II), but the...