Recent developments in the discovery of indole-based scaffolds as promising targeted cancer therapeutics [0.03%]
基于吲哚骨架的靶向抗癌药物的研究进展
Prasanna A Yakkala,Venkatesh Erram,Sajeli A Begum et al.
Prasanna A Yakkala et al.
Cancer remains the leading cause of mortality worldwide, driving the need for new and more effective therapeutics. Indole-based scaffolds have emerged as highly versatile structural frameworks in drug discovery in view of their structural d...
Matthias Schild,Dennis Gillingham
Matthias Schild
The success of antibody-drug conjugates has demonstrated the value of targeted delivery strategies for cytotoxic molecules. However, many oncogenic drivers remain inaccessible to antibodies due to their intracellular location, and these dri...
Revealing deamidation and isoaspartate formation during peptide analysis, purification and storage by tandem mass spectrometry [0.03%]
利用串联质谱检测肽段分析、纯化及储存过程中的脱氨和异天冬氨酸形成反应
V Erckes,L Chamera Rendueles,A Misiek et al.
V Erckes et al.
Interest in peptides and peptidomimetics continues to grow, particularly in the context of drug discovery and development. However, spontaneous chemical modifications such as deamidation and isoaspartate formation present significant challe...
Integrated computational screen and validation of thalidomide-based PROTACs targeting SARS-CoV-2 main protease [0.03%]
基于噻唑 omide的蛋白质降解剂筛选及针对SARS-CoV-2主要蛋白酶的计算验证
Li-Na Guo,Yu-Hua Li,Rou-Yu Zhu et al.
Li-Na Guo et al.
The persistent evolution of SARS-CoV-2 underscores the need for antiviral strategies. The viral main protease (Mpro) represents a conspicuous target due to its essential role in viral replication and high conservation across SARS-CoV-2. Con...
From lab to environment: forecasting pharmaceutical impact using in silico and analytical tools [0.03%]
从实验室到环境:利用计算机模拟和分析工具预测医药影响
Hamza Boucetta,Peije Russell,David Rudd et al.
Hamza Boucetta et al.
Pharmaceuticals are increasingly detected in the environment, raising concerns about their ecological impact. Global monitoring efforts have revealed widespread contamination, with many sites exceeding safety thresholds for aquatic health. ...
Comprehensive multi-omics analysis and experimental validation indicate that VPS35 is a promising biomarker for prognosis, immunotherapy, and chemotherapy in LIHC [0.03%]
全面的多组学分析及实验验证表明VPS35可作为LIHC预后、免疫和化疗标志物的潜力
Dan Wan,Yajie Qi,Yali Kang et al.
Dan Wan et al.
Background : Vacuolar protein sorting 35 (VPS35) is a key subunit of the retromer complex, and several previous studies have shown that VPS35 plays an important role in the progression of hepatocellular carcinoma (LIHC). However, the compre...
Theranostic advances in Alzheimer's disease: structure-guided design of near-infrared fluorescent probes targeting amyloid-β and cholinergic dysfunction [0.03%]
阿尔茨海默病诊疗新进展:结构导向的近红外荧光探针的设计及针对淀粉样蛋白和胆碱能损伤的作用机制研究
Upesh Mandloi,Namita Giri,Saroj Kumar et al.
Upesh Mandloi et al.
Alzheimer's disease (AD) is a complex neurodegenerative disorder, with unmet clinical challenges due to the lack of early diagnosis and an efficient treatment. Theranostics, an integrated approach that combines diagnosis and therapy, has em...
Discovery of novel polymyxin E adjuvants against Acinetobacter baumannii guided by a stacking-based machine learning model [0.03%]
基于堆积的机器学习模型指导的新多粘菌素E佐剂对抗阿氏不动杆菌的新发现
Yuce Chen,Kunkun Shen,Ting Lin et al.
Yuce Chen et al.
The rapid spread of antibiotic resistance poses an escalating global health crisis. Polymyxin E, the antibiotic of last resort, is limited by dose-dependent toxicity. Antibiotic adjuvants offer a promising strategy to enhance efficacy while...
An overview of recent advancements in targeted cancer therapies and their potential clinical impact [0.03%]
靶向癌症治疗的近期进展及其潜在临床影响综述
Shujauddin Ahmed,Akash P Sakla,Kousar Jahan et al.
Shujauddin Ahmed et al.
Recent advances in medicine and drug development have significantly changed how cancer is treated. The success of inhibitors like sotorasib and adagrasib has expanded options for targeting once 'undruggable' oncogenic drivers such as KRAS. ...
Mitochondria-targeting symmetric diiminoguanidines: potent and selective anticancer agents against pancreatic tumors [0.03%]
线粒体靶向对称二亚胺胍类化合物:针对胰腺肿瘤的高效和选择性抗肿瘤制剂
Sigrid Lacaille,Andreea R Schmitzer
Sigrid Lacaille
Pancreatic cancer remains one of the deadliest malignancies of the 21st century, with a five-year survival rate below 12%. Its growing incidence is strongly linked to modern lifestyles, marked by obesity, diabetes, overnutrition, and physic...