Over-expression, purification, and kinetic analysis of Mycobacterium tuberculosis WecA [0.03%]
结核分枝杆菌WecA蛋白的过表达、纯化及生化酶活鉴定
Yishu Zhao,Haiying Jia,Yan Wang et al.
Yishu Zhao et al.
The N-acetylglucosamine-1-phosphate transferase (WecA)is a potential target for developing anti-tuberculosis drugs, due to its critical role in the synthesis of mycobacterial cell wall. The enzymatic study of WecA and the discovery of WecA ...
Discovery of novel N-(prop-2-yn-1-yl)-1,2,3,4-tetrahydronaphthalen-1-amine derivatives as MAO-B inhibitors for the treatment of Parkinson's disease [0.03%]
作为帕金森病治疗的MAO-B抑制剂的新型N-(prop-2-yn-1-yl)-1,2,3,4-四氢萘-1-胺衍生物的发现
Ziwei Wang,Jing Feng,Chengwan Yi et al.
Ziwei Wang et al.
Monoamine oxidase B (MAO-B) inhibitors may be an effective therapeutic approach for Parkinson's disease. This study designed and synthesised a series of N-(prop-2-yn-1-yl)-1,2,3,4-tetrahydronaphthalen-1-amine derivatives and evaluated their...
Renalase stimulates aldosterone production via PMCA4b/cAMP in NCI-H295R cells [0.03%]
肾分泌素通过PMCA4b/cAMP促进NCI-H295R细胞皮质醇合成
Ru Fu,Miao Huang,Tao Liu et al.
Ru Fu et al.
We recently observed a significantly higher level of renalase (RNLS) in aldosterone-producing adenomas (APAs) than in the APA-adjacent adrenal glands (AAGs). RNLS is a flavin adenine dinucleotide-dependent monoamine oxidase. In this study, ...
Substrate cooperativity shapes competitive inhibitor responses in mycobacterial inosine 5'-monophosphate dehydrogenase [0.03%]
底物共价性塑造分枝杆菌次黄嘌呤单磷酸脱氢酶的竞争性抑制剂响应
Zdeněk Knejzlík,Ondřej Bulvas,Matteo Dedola et al.
Zdeněk Knejzlík et al.
Inosine 5'-monophosphate dehydrogenase (IMPDH) is a promising antimicrobial target due to its central role in guanine nucleotide biosynthesis. Accurate and reliable kinetic measurements are essential for evaluating inhibitors. However, the ...
Identification of novel HIF2α inhibitors: a structure-based virtual screening approach [0.03%]
基于结构的虚拟筛选方法识别新型HIF2α抑制剂
Shasha Zhou,Shengnan Yin,Shudan Yang et al.
Shasha Zhou et al.
HIF2α is aberrantly upregulated in some renal cell carcinomas due to VHL mutations, supporting HIF2α inhibition as a compelling therapeutic approach for such cases. Therefore, the six compounds (designated as Compounds 1-6) were screened ...
Advancing infection therapy: the role of novel menthol-based antimicrobials [0.03%]
感染治疗的新进展：新型薄荷醇抗菌素的作用
Annalisa Di Rienzo,Abdelmoujoud Faris,Marina Mingoia et al.
Annalisa Di Rienzo et al.
In this work, 17 derivatives were synthesised by combining halogenated and non-halogenated cinnamoyl scaffolds with menthol and tested against a panel of Gram-positive and Gram-negative bacteria. Among the synthesised derivatives, MF1 and M...
Imidazole-2-thione derivatives as new selective anticancer agents with anti-metastatic properties: synthesis and pharmacological evaluation [0.03%]
具有抗转移性质的新选择性抗癌剂——咪唑并噻二酮衍生物的合成与药理学评估
Božena Golcienė,Natalia Maciejewska,Anoop Kallingal et al.
Božena Golcienė et al.
Imidazole scaffolds are attractive in drug design for bioactivity and synthetic accessibility. We developed S-substituted imidazole-2-thione derivatives, focusing on compound 24, which showed potent cytotoxicity against lung, cervical, and ...
Identification of the first peptide inhibitor of UBE2C enzymatic activity: insights from metadynamics-guided folding and binding studies [0.03%]
基于元动力学折叠及结合研究鉴定首个UBE2C酶活肽类抑制剂及其作用机制
Luciano Pirone,Bianca Fiorillo,Annarita Del Gatto et al.
Luciano Pirone et al.
UBE2C (also known as UbcH10) is a ubiquitin-conjugating enzyme essential for mitotic progression and a potential therapeutic target in cancer. Here, we report a structure-based design and characterisation of peptides derived from a natural ...
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...