Discovery of N8: a novel IKKε inhibitor with potent anticancer activity via cytotoxicity, migration suppression, and autophagy modulation [0.03%]
N8的发现：一种新型IKKε抑制剂通过细胞毒作用、迁移抑制和自噬调节具有潜在的抗肿瘤活性
Wei Ye,Siying Zheng,Hongmei Xie et al.
Wei Ye et al.
The serine/threonine kinase IKKε is overexpressed or activated in various cancers, making it a promising therapeutic target. Through a large-scale virtual screening of over 12 million compounds, we identified N8 as a novel IKKε inhibitor,...
Insights into the complexity of SARS-CoV-2 Mpro inhibition: Ebselen and its derivatives impair dimerisation of the enzyme [0.03%]
关于SARS-CoV-2 Mpro抑制的复杂性见解：依贝硒及其衍生物可干扰该酶二聚化
Simone Fabbian,Silvia Fabi,Laurin Schwarz et al.
Simone Fabbian et al.
The SARS-CoV-2 Main Protease (Mpro), a key enzyme for viral replication, represents a highly attractive target for the development of broad-spectrum anti-coronavirus therapeutics. The organoselenium drug Ebselen has shown potent in vitro in...
From bench to brain: novel thieno-oxazine hybrids as potent pleiotropic anti-Alzheimer's agents with in vivo/ in vitro validation and in silico insights [0.03%]
从体外到体内：新型噻并噁嗪类化合物作为抗阿尔茨海默病多靶点潜在药物的验证与理论研究
Eman A Fayed,Mazin A A Najm,Khulood H Oudah et al.
Eman A Fayed et al.
Due to their various pharmacological effects, several substituted sulphur heterocycles containing thiophene have recently attracted a great deal of attention. A novel 2,3-diaryl-2,3,5,6,7,8-hexahydro-4H-benzo[4,5]thieno[3,2-e][1,3]oxazin-4-...
Discovery of 2-phenylethyl chromones as potent and selective CYP1B1 inhibitors [0.03%]
2-苯乙基色原酮类化合物作为CYP1B1强效选择性抑制剂的发现
Wenming Chen,Wenchong Ye,Yinghong Long et al.
Wenming Chen et al.
Cytochrome P4501B1 (CYP1B1), overexpressed in solid tumours but minimally in healthy tissues, is a promising anticancer target linked to chemoresistance. While CYP1B1 inhibitors can restore drug efficacy, most suffer from limited scaffold d...
Effect of trypsin inhibitor isolated from tamarind seed (TTI) on caenorhabditis elegans survival under bacterial infection [0.03%]
绿豆凝集素改善细菌感染状态下线虫的寿命及免疫反应
Lídia Leonize Rodrigues Matias,Riva de Paula Oliveira,Rafael Oliveira de Araújo Costa et al.
Lídia Leonize Rodrigues Matias et al.
The study aimed to evaluate the effect of a trypsin inhibitor isolated from tamarind seeds (TTI) on Caenorhabditis elegans as an anti-infective agent. No statistical difference was found in the toxicity test to TTI for locomotion, ovipositi...
Antitumor activity and structure-activity relationship of poly (ADP-ribose) polymerase (PARP)-based dual inhibitors [0.03%]
聚(腺苷二磷酸核糖)聚合酶(PARP)双靶点抑制剂的抗肿瘤活性及其构效关系研究
Chunhui Yang,Yunpeng Shang,Xin Li et al.
Chunhui Yang et al.
Poly(ADP-ribose) polymerase (PARP) inhibitors constitute a significant class of targeted anticancer therapies that leverage the principle of synthetic lethality in tumours deficient in homologous recombination (HR) repair. Although these ag...
Study on the phosphorylation of NAD+-specific isocitrate dehydrogenase in the pathogenic bacteria Stenotrophomonas maltophilia and Xanthomonas sacchari [0.03%]
植物病原菌马氏顿螺杆菌和木糖氧化亚硝基细菌NAD+特异苹果酸酶磷酸化研究
Qian Tian,Yongmei Zhang,Chunxu Pan et al.
Qian Tian et al.
Isocitrate dehydrogenases (IDHs) regulate the distribution of carbon flux between the TCA cycle and glyoxylate shunt through reversible phosphorylation that influences pathogen virulence. Current studies only indicate that NADP+-specific ID...
Identification of novel PTP1B inhibitor for the treatment of LPS-induced myocardial apoptosis: machine learning based virtual screening and biological evaluation [0.03%]
基于机器学习的虚拟筛选结合生物实验评价PTP1B新型抑制剂的抗LPS诱导的心肌细胞凋亡活性
Xu Dong,Bing Shang,Xin Li et al.
Xu Dong et al.
Sepsis-induced cardiovascular dysfunction (SICD) poses a serious threat to human life. Protein tyrosine phosphatase 1B (PTP1B) displays an essential role in SICD occurrence, so discovering novel inhibitors targeting PTP1B is an effective st...
Sulphonamide derivatives with a triazine core as novel inducers of apoptosis and pyroptosis in glioblastoma multiforme cells [0.03%]
三嗪核心磺胺衍生物作为新型诱导多形性胶质母细胞瘤细胞凋亡和细胞焦亡剂
Olga Klaudia Szewczyk-Roszczenko,Katarzyna Kotwica-Mojzych,Piotr Roszczenko et al.
Olga Klaudia Szewczyk-Roszczenko et al.
Glioblastoma multiforme (GBM) is a highly aggressive brain tumour with few effective treatment options. This study evaluated two novel triazine-based sulphonamides, MM118 and MM119, for their anticancer effects on GBM cells. In vitro cell v...
Targeting RIPK1 to modulate cell death and tumour microenvironment in cancer therapy [0.03%]
靶向RIPK1以调节细胞死亡和肿瘤微环境以治疗癌症
Jing Chen,Shijie Mao,Lingling Huang et al.
Jing Chen et al.
Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) is crucial in regulating inflammation, apoptosis, and necroptosis. Accumulating evidence highlights RIPK1 as a promising therapeutic target for various human diseases, including...