Beneficial Effects of a Novel Fructose-1,6-Bisphosphatase Inhibitor Cpd96 on Insulin Secretion in Type 2 Diabetes [0.03%]
一种新型果糖-1,6-双磷酸酶抑制剂Cpd96对2型糖尿病胰岛素分泌的有益作用
Kejia Xu,Jiaxuan Zhao,Liran Lei et al.
Kejia Xu et al.
Fructose-1,6-bisphosphatase (FBPase) is a rate-limiting enzyme in gluconeogenesis, and its inhibition has the potential to improve glucose homeostasis. We characterize Cpd96, a novel inhibitor of FBPase, and demonstrate its multifaceted ant...
On-Chip Microfluidic Production of Sonosensitizer-Loaded Liposomes for Sonodynamic Therapy of Hepatocellular Carcinoma [0.03%]
芯片微流控产生声敏剂载脂质体用于肝细胞癌声动力治疗
Wei Luo,Alap Ali Zahid,Aishik Chakraborty et al.
Wei Luo et al.
Hepatocellular carcinoma (HCC) is a major contributor to cancer-related deaths worldwide. Among the emerging therapies, ultrasound-mediated sonosensitizers have shown promise in the treatment of HCC. Sonosensitizers exposed to low-intensity...
Measurement of Endogenous Fatty Acid Esters of Hydroxy Fatty Acid (FAHFA) and Alkyl-diacylglycerol (TG(O)) from Human Breast Milk [0.03%]
人乳内源性羟基脂肪酸酯和烷基二酰基甘油的测定方法研究
Megan Li Xian Lee,Kim Ngan T Nguyen,Wei Wei Pang et al.
Megan Li Xian Lee et al.
Fatty acid esters of hydroxy fatty acids (FAHFAs) and alkyl-diacylglycerols (TG-(O)-s) are endogenous lipids that exert protective effects against diabetes, inflammation, and the development of childhood obesity. They have been identified a...
Toll-Like Receptor 7/8 Antagonist Promotes Interleukin-10-Mediated Anti-inflammatory Therapy [0.03%]
toll样受体7/8拮抗剂促进 interleukin-10介导的抗炎治疗
Grahmm A Funk,Jin Xie,Tamara A Kucaba et al.
Grahmm A Funk et al.
Toll-like receptors (TLR) 7 and 8 are pattern recognition receptors expressed in immune cells, such as dendritic cells (DC) and macrophages, that respond to viral and bacterial infections. TLR7/8 activation triggers a pro-inflammatory immun...
Decoding of Inconsistent Biological Data: A Critical Step toward Enhanced AI Predictivity in Drug Discovery [0.03%]
不一致生物数据的解码：提高药物发现中人工智能预测性的关键步骤
Mira A M Behnam,Andrea Cavalli,Diana Lousa et al.
Mira A M Behnam et al.
Combining bioactivity data of assays against the same target, which are obtained from different sources, was recently shown to lead to considerable noise for training data sets of machine learning (ML) models. In this Viewpoint, we address ...
Preclinical Evaluation of a 177Lu-Labeled Gastrin-Releasing Peptide Receptor Antagonist and Prostate Cancer Treatment with Monotherapy and in Combination with Everolimus [0.03%]
177Lu标记胃泌素释放肽受体拮抗剂的药代动力学和放射生物学：单用以及与Everolimus联用治疗前列腺癌的前期评估研究
Naveen Kumar,Adrianna Bilinska,Elena Menéndez et al.
Naveen Kumar et al.
This study evaluates the potential of a 177Lu-labeled GRPR-targeting antagonist as a radiotherapeutic agent for tumors expressing the gastrin-releasing peptide receptor (GRPR). The therapeutic effect of the radioligand was investigated both...
Metabolism, Pharmacokinetics, and Tissue Distribution of a Selective FK506-Binding Protein 12 F36V Mutant Degrader in Mice [0.03%]
小鼠体内选择性FK506结合蛋白12F36V突变降解剂的代谢、药代动力学和组织分布研究
Shenzhi Zhou,Xuan Qin,Kevin Tran et al.
Shenzhi Zhou et al.
dTAG-13 is a heterobifunctional molecule that induces proteasomal degradation of FKBP12F36V-tagged proteins and is widely used in the dTAG system. To better understand its in vivo behavior, we investigated its metabolism in vitro and its me...
Dysbiosis-Driven Reprogramming of Secondary Bile Acid Metabolism in Metabolic Dysfunction-Associated Steatotic Liver Disease: Insights from an Ex Vivo Human Fecal Microbiota Model [0.03%]
代谢功能异常相关性脂肪型肝病中菌群驱动的次级胆汁酸代谢重构：来自体外人体粪便菌群模型的启示
Daniel Zhi Wei Ng,Adrian Low,Khairul Rifdi Bin Khairul Sani et al.
Daniel Zhi Wei Ng et al.
Gut microbial dysbiosis-induced perturbations in bile acid (BA) metabolism are implicated in metabolic dysfunction-associated steatotic liver disease (MASLD), yet evidence remains largely associative. Using an optimized ex vivo fecal microb...
Effects of Ezetimibe, Statins, and Their Combination on Nuclear Factor Erythroid 2‑Related Factor 2/Heme Oxygenase-1/Kelch-like ECH-Associated Protein‑1 Signaling and Inflammatory Markers in Indomethacin-Induced Gastric Ulcer in Rats [0.03%]
依折麦布、他汀及其联合用药对炎性介质及诱导型胃溃疡大鼠核因子E2相关因子2/血红素加氧酶1/刺鼠相关蛋白1信号通路的影响
Ibrahim Ali Erfan,Ahmed Khodir,Maivel H Ghattas et al.
Ibrahim Ali Erfan et al.
Gastric ulcers (GUs), a frequent gastrointestinal condition, cause mucosal injury and inflammation. We aimed to investigate the protective effects and underlying mechanisms of ezetimibe, statins, and their combination in indomethacin-induce...
Differential Sensitivity of TRPC- and ORAI-Mediated Calcium Entries to 1‑[2-(4-Methoxyphenyl)-2-[3-(4-methoxyphenyl)propoxy]ethyl]imidazole Chloride (SKF-96365) [0.03%]
1-[2-(4-甲氧基苯基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑氯化物（SKF-96365）对由瞬时受体电位通道和钙离子释放激活的钙模导钙内流的不同敏感性
Sebastián Susperreguy,Karina Formoso,Julieta Mansilla Ricartti et al.
Sebastián Susperreguy et al.
Background and purpose: SKF-96365 is widely used as a broad-spectrum inhibitor of calcium entry. It was initially identified as a Receptor-Operated Ca2+ Entry (ROCE) blocker and was later shown to inhibit ORAI1-STIM1-medi...