Inhibition mechanism and behaviour of wedelolactone against α-glucosidase [0.03%]
Wedelolactone的α-糖苷酶抑制机制和行为研究
Jianjun Zhang,Min Zhao,Fan Wu et al.
Jianjun Zhang et al.
The quest for effective and safe treatments for diabetes mellitus has led to the exploration of natural metabolites as potential α-glucosidase inhibitors. This study delves into the inhibition mechanism of wedelolactone against α-glucosid...
Discovery of a brain penetrant SGK1 inhibitor using a ligand- and structure-based virtual screening methodology [0.03%]
基于配体和结构的虚拟筛选方法发现一种可以进入大脑的SGK1抑制剂
Enrique Madruga,Cecilia Sanchez-Santos,Ignacio Valenzuela-Martínez et al.
Enrique Madruga et al.
Serum and glucocorticoid-regulated kinase 1 (SGK1) is an underexplored kinase involved in several neurodegenerative diseases. Although SGK1 inhibitors are not available on the market, the absence of side effects in two SGK1 knockout mouse m...
Bio-guided discovery of antibacterial metabolites from Penicillium chrysogenum [0.03%]
生物导向发现源自青霉菌的抗菌代谢物
Amira Mira,Fatma M Abdel Bar,Ahmed I Foudah et al.
Amira Mira et al.
Bio-guided isolation from the Red Sea-derived Penicillium chrysogenum yielded two new metabolites, 15-deoxy-15-amino-citreohybridonol (6) and chrysogenotoxin (7), alongside five known compounds: emodin (1), chrysophanol (2), bis(2-ethylhexy...
José L Pereira Filho,Renato B Pereira,Tatiana F Vieira et al.
José L Pereira Filho et al.
Eugenol (4-allyl-2-methoxyphenol), is the major chemical constituent in the essential oil of numerous plant species. Several biological properties have been described for this molecule, including modulation of enzymatic targets relevant for...
Inhibition of 12/15-LOX hyperactivation mitigates cognitive decline in a chronic cerebral hypoperfusion mouse model and in H2O2-induced HT22 cells: therapeutic effects of brozopine [0.03%]
12/15-LOX过度激活的抑制缓解慢性脑低灌注小鼠模型和H2O2诱导的HT22细胞中的认知衰退：Brozopine的治疗作用
Xuening Wang,Zhizai Lu,Qiuji Shao et al.
Xuening Wang et al.
Brozopine (BZP), a novel inhibitor of 12/15-lipoxygenase (12/15-LOX), has previously demonstrated efficacy in mitigating inflammatory and oxidative stress-related injury in cerebral ischaemia models. This study aimed to evaluate the therape...
Development of triaryl antimicrobials by scaffold hopping from an aminopropanol hit targeting bacterial RNA polymerase-NusG interactions [0.03%]
通过支架跳跃从氨基丙醇hit开发三芳环抗菌剂以靶向细菌rna聚合酶-nusg相互作用
Tiankuang Liu,Cheuk Hei Kan,Yingbo Zheng et al.
Tiankuang Liu et al.
Bacterial RNA polymerase (RNAP) requires the NusG factor to facilitate transcription, with the RNAP clamp-helix domain (CH) serving as the primary binding site for NusG and representing a promising target for antimicrobial intervention. In ...
High-throughput virtual screening, identification and in vitro biological evaluation of novel inhibitors of PLK1 and NRP1 [0.03%]
高效虚拟筛选、鉴定及体外活性评价新型PLK1和NRP1抑制剂
Yang Xia,Yuting Chang,Lixia Guan et al.
Yang Xia et al.
Overexpression of PLK1 and NRP1 correlate with enhanced proliferative activity in lung cancer cells, thus the development of dual-target PLK1/NRP1 inhibitors holds great therapeutic promise. In this study, five compounds (PLN 1-5) targeting...
Hwa Young Kim,Mi-Sun Kim,Dong Hae Shin
Hwa Young Kim
Poxviruses regulate their replication cycle through host phosphorylation pathways, with dual-specific phosphatase H1(DUSP-H1) playing a key role in immune evasion by dephosphorylating STAT1 and inhibiting interferon(IFN) responses. Given it...
Structure-based design of new potent and highly selective PARP-1 inhibitor for treating colorectal cancer [0.03%]
结构导向设计新型有效的PARP-1抑制剂用于治疗结直肠癌
Chunying Jiang,Shudan Yang,Yuting Wang et al.
Chunying Jiang et al.
Poly (ADP-ribose) polymerase 1 (PARP-1) exhibits high expression levels in colorectal cancer (CRC) patients and participates in multiple DNA damage repair pathways, thereby emerging as an attractive target. Herein, we identified a series of...
N-alkyl and N-benzyl indoles are anti-SARS-CoV-2 agents and nsp13 inhibitors [0.03%]
N-烷基和N-苄基吲哚是抗SARS-CoV-2和nsp13抑制剂
Aurora Albano,Roberta Emmolo,Riccardo De Santis et al.
Aurora Albano et al.
COVID-19 pandemic stimulated tremendous efforts to develop therapeutic strategies targeting SARS-CoV-2, leading to the evaluation of a wide range of potential treatments in clinical trials. However, effective therapeutics remain elusive whe...