Preclinical validation of tetrahydroquinoline derivatives as EGFR inhibitor inducing glioblastoma cell death [0.03%]
Akshaya Murugesan,Saravanan Konda Mani,Aleksei Smirnov et al.
Akshaya Murugesan et al.
Glioblastoma multiforme, a malignant brain tumor has a dismal prognosis and lacks effective treatment. Epidermal growth factor receptor (EGFR) is an attractive drug target for GBM treatment, yet no therapeutic effect has been reported. Here...
FOSL1 Mediates Collagen Synthesis and Myofibroblast Transformation in Aortic Fibroblasts Under Ang II-Induced Aortic Dissection Conditions [0.03%]
Lin Zhong,Hui Zhang,Youqi Huang et al.
Lin Zhong et al.
Due to the lack of effective drug therapies, aortic dissection is associated with extremely high mortality rates. Previous studies have demonstrated that FOS-like antigen 1 (FOSL1) plays a role in atherosclerosis and tumor progression. Howe...
Asbjørn Jaensch Rasmussen,Matteo Guidetti,Rolf Hilfiker et al.
Asbjørn Jaensch Rasmussen et al.
Co-crystals have recently attracted growing interest as enabling formulations for poorly soluble drugs, due to their ability to enhance various physicochemical properties of active pharmaceutical ingredients (APIs). Different co-crystals of...
Computational modeling of the early-stage solubilization of a fenofibrate aggregate into mixed bile salt and fatty acids micelles [0.03%]
胆盐和脂肪酸混合胶束溶剂化菲诺贝特聚集体早期过程的计算模拟研究
Fatmegyul Mustan,Anela Ivanova,Slavka Tcholakova
Fatmegyul Mustan
The behavior of a fenofibrate aggregate in water and its interaction with pure sodium taurodeoxycholate (TDC) micelles, as well as with mixed micelles of TDC and fatty acids (myristic, oleic, and stearic), was studied using atomistic molecu...
LeiCNS-PK3.2: A Physiologically Based Pharmacokinetic Model Framework for Predicting intracellular Concentrations of Acyclovir and Ganciclovir Active Metabolites [0.03%]
LeiCNS-PK3.2：一个用于预测阿昔洛韦和更昔洛韦活性代谢物脑内浓度的生理药动学模型框架
Ming Sun,Martijn L Manson,Tingjie Guo et al.
Ming Sun et al.
Background: Effective treatment of viral infections in the central nervous system (CNS) requires adequate nucleoside analogs exposure and conversion into phosphorylated metabolites (TP) in brain cells. ...
Targeting the Xylosyltransferase TMEM5 in Glioblastoma to Modulate CLOCK and CRY1 Expression and Restore Temozolomide Sensitivity via the Circadian Signaling Axis [0.03%]
靶向胶质母细胞瘤中的岩藻糖基转移酶TMEM5以调节CLOCK和CRY1的表达并通过昼夜节律信号轴恢复替莫唑胺敏感性
Yu-Kai Su,Hao-Yu Chuang,Heng-Wei Liu et al.
Yu-Kai Su et al.
Background: Glioblastoma (GBM) is the most aggressive primary brain tumor and exhibits marked resistance to standard therapies, including temozolomide (TMZ). Circadian rhythm disruption is increasingly recognized in GBM; ...
Development and characterization of a carrier-free dry powder inhaler formulation of clarithromycin [0.03%]
一种无载体克拉霉素干粉吸入剂型的开发与表征研究
Cemre İrem Aygüler,Hanan Fael,Mayram Hacıoğlu et al.
Cemre İrem Aygüler et al.
Carrier-free systems are a highly substantial research area due to the side effects of excipients on the lungs and the limited number of excipients suitable for lung-targeted drug delivery systems. The goal of this study is the preparation ...
Call for data: High dose empty liposome control data for a collaborative open access publication (>LIPOTOX [0.03%]
呼吁共享数据：发表关于高剂量空脂质体对照的开放存取合作论文的数据请求（>LIPOTOX）
Simon Drescher
Simon Drescher
In vitro inhibition of organic anion transporting polypeptide 2B1 (OATP2B1) is common among marketed drugs [0.03%]
市场上的药物中有机阴离子转运多肽2B1(OATP2B1)的体外抑制作用广泛存在
Mohsin Ali Raza,Alli Sinokki,Marju Monnonen et al.
Mohsin Ali Raza et al.
Organic anion transporting polypeptide 2B1 (OATP2B1) is a cell membrane influx transporter that may have a role in drug absorption and disposition. Inhibition of intestinal OATP2B1 has been suggested to decrease the oral bioavailability of ...
Glycyl-l-histidyl-l-lysine as a novel co-former in co-amorphous systems: Enhanced aqueous solubility and physical stability [0.03%]
甘氨-h-组氨-l-赖氨作为共无定形体系中的新型共形式剂：增强的水溶性和物理稳定性
Qiang Huang,Zhiren Zou,Dian Cheng et al.
Qiang Huang et al.
Co-amorphous systems have emerged as a promising strategy to enhance the aqueous solubility of poorly water-soluble drugs. Although amino acids have been widely studied as co-formers, some amino acid-based co-amorphous systems exhibit limit...