Liquidambaric acid as a non-competitive α-glucosidase inhibitor: multi-level evidence from enzyme kinetics, molecular docking, molecular dynamics simulations, and a Drosophila hyperglycaemic model [0.03%]
液状黎巴嫩香脂酸作为非竞争性α-糖苷酶抑制剂：来自酶动力学，分子对接，分子动力学模拟和果蝇高血糖模型的多级证据
Liwei Jia,Yan Liu,Bo Fu et al.
Liwei Jia et al.
Liquidambaric acid, a pentacyclic triterpenoid from Liquidambar formosana Hance, was evaluated as a novel α-glucosidase inhibitor for type 2 diabetes mellitus (T2DM) management. Enzyme kinetic assays revealed its potent non-competitive inh...
2,5-Dihydroxyphenylethanone: an anti-melanogenic bioactive compound isolated from Ganoderma cochlear [0.03%]
从柄苞灵芝中分离得到的一种新的促黑素生成抑制化合物2,5-二羟基苯乙酮
Meng Ning,Xiao-Cui Liu,Min He et al.
Meng Ning et al.
2,5-dihydroxyacetophenone, a natural product from the fruiting bodies of Ganoderma cochlear, can effectively and safely inhibit the production of melanin in zebrafish model. To achieve analogues with more significant inhibition, 9 analogs w...
Profiling and cheminformatics bioprospection of curcurbitacin I and momordin Ic from Momordica balsamina on α-amylase and α-glucosidase [0.03%]
Momordica balsamina 中活性成分.curcurbitacin I 和 momordin Ic 的酶学评价及化学信息学筛选研究
Viruska Jaichand,Adedayo Ayodeji Lanrewaju,Himansu Baijnath et al.
Viruska Jaichand et al.
Momordica spp. has been traditionally used to manage type 2 diabetes mellitus, but the mechanisms and metabolites remain unclear. This study evaluated the inhibitory potential of Momordica balsamina extracts on α-amylase and α-glucosidase...
Discovery and biological evaluation of a novel and highly potent JAK2 inhibitor for the treatment of triple negative breast cancer [0.03%]
一种新型高效JAK2抑制剂的发现及三阴性乳腺癌治疗评价研究
Yingxiang Miao,Shudan Yang,Fang Zhang et al.
Yingxiang Miao et al.
Janus kinase 2 (JAK2) is considered an attractive target for the treatment of triple-negative breast cancer (TNBC). Herein, we discovered six JAK2 inhibitors using structure-based virtual screening and molecular docking. Among them, JNN-5 w...
Medicinal chemistry breakthroughs on ATM, ATR, and DNA-PK inhibitors as prospective cancer therapeutics [0.03%]
靶向ATM、ATR和DNA-PK的抑制剂作为潜在抗癌药物的研究进展与突破点
Ram Sharma,Anshul Mishra,Monika Bhardwaj et al.
Ram Sharma et al.
This review discusses the critical roles of Ataxia Telangiectasia Mutated Kinase (ATM), ATM and Rad3-related Kinase (ATR), and DNA-dependent protein kinase (DNA-PK) in the DNA damage response (DDR) and their implications in cancer. Emphasis...
Shan Wang,Feifan Li,Xilong Feng et al.
Shan Wang et al.
Skin ageing is a complex physiological process primarily characterised by the deepening of wrinkles and the sagging of the skin. Collagen is essential for maintaining skin elasticity and firmness. As skin ages, it experiences structural and...
Discovery of lignans as the effective inhibitors of CES1A alleviate lipid droplets formation [0.03%]
番荔枝素通过抑制CES1A活性缓解脂质 droplets形成
Jie Mu,Si-Si Chen,Shi-Qing Li et al.
Jie Mu et al.
ER carboxylesterase 1A (CES1A) is an important metabolic enzyme involved in lipid metabolism. Targeting the CES1A is a promising approach for diseases associated with disorders of lipid metabolism therapy. In this study, screening of 26 nat...
Design, synthesis and biological activity of novel Xuetongsu derivatives as potential anticancer agents by inducing apoptosis [0.03%]
新型血通素衍生物的合成及体内外抗肿瘤活性研究
Qi Jiang,Hui Zhong,Cong Wu et al.
Qi Jiang et al.
Xuetongsu (XTS, Schisanlactone E) is one of the main active compounds and considered as the star molecule isolated from Kadsura heteroclita (Roxb.) Craib. In order to improve XTS anti-tumour bioactivities, a series of novel XTS derivatives ...
Study on the synthesis and biological activity of kojic acid triazol thiosemicarbazide Schiff base derivatives [0.03%]
棓酸三氮唑硫半卡罢腙之合成及其生物活性之研究
Yayuan Luo,Zhiyong Peng,Junyuan Tang et al.
Yayuan Luo et al.
A series of kojic acid triazol thiosemicarbazide Schiff base derivatives were designed and synthesised. Evaluation on the inhibition of tyrosinase activity showed that these compounds possessed potent inhibit tyrosinase activity, and the co...
Tetra-anionic porphyrin mimics protein-protein interactions between regulatory particles and the catalytic core, allosterically activating human 20S proteasome [0.03%]
四负电荷类卟啉模拟调控颗粒与催化核心之间的蛋白质-蛋白质相互作用，从而激活人类20S蛋白酶体
A M Santoro,M Persico,A D&#x;Urso et al.
A M Santoro et al.
Decreased proteasome activity is a hallmark of brain and retinal neurodegenerative diseases (Alzheimer's, Parkinson's diseases, glaucoma) boosting the search for molecules acting as proteasome activators. Based on the hypothesis of an elect...