Discovery of New Inhibitors of Human Activated Protein C to Treat Hemophilia [0.03%]
治疗血友病的活化蛋白C新型抑制剂的发现
Kholoud F Aliter,Rami A Al-Horani
Kholoud F Aliter
Background: Activated Protein C (APC) is a plasma serine protease with antithrombotic function. APC acts as an anticoagulant by promoting the degradation of factors Va and VIIIa, thus inhibiting the formation of thrombin....
Challenges in the Discovery and Optimization of mGlu2/4 Heterodimer Positive Allosteric Modulators [0.03%]
第二类代谢型谷氨酸受体异二聚体阳性变构调节剂的发现与优化挑战
Mark Gallant Fulton,Matthew Thomas Loch,Caroline Anne Cuoco et al.
Mark Gallant Fulton et al.
Background: This article describes the challenges in the discovery and optimization of mGlu2/4 heterodimer Positive Allosteric Modulators (PAMs). Methods:...
L-Carnitine Supplementation Improves Self-Rating Depression Scale Scores in Uremic Male Patients Undergoing Hemodialysis [0.03%]
左卡尼汀治疗能改善尿毒症性透析男患者的抑郁症状
Kyoko Tashiro,Yusuke Kaida,Sho-Ichi Yamagishi et al.
Kyoko Tashiro et al.
Background: Depression is highly prevalent in uremic patients undergoing hemodialysis (HD). We previously found that low free-carnitine levels are associated with depression severity in male patients undergoing HD. Howeve...
Estrogen catechols detection as biomarkers in schistosomiasis induced cancer and infertility [0.03%]
应用于血吸虫病致癌症和不育的雌激素儿茶酚类生物标志物的检测技术研究
M C Botelho,H Alves,J Richter
M C Botelho
Urogenital schistosomiasis is a chronic infection caused by the human blood fluke Schistosoma haematobium. Schistosomiasis haematobium is a known risk factor for cancer leading to squamous cell carcinoma of the urinary bladder (SCC). This i...
Potent and Orally Bioavailable Antiplatelet Agent, PLD-301, with the Potential of Overcoming Clopidogrel Resistance [0.03%]
高效口服抗血小板药物PLD-301有望克服氯吡格雷抵抗现象
Jingyu Chen,Michael Zhiyan Wang
Jingyu Chen
PLD-301, a phosphate prodrug of clopidogrel thiolactone discovered by Prelude Pharmaceuticals with the aim to overcome clopidogrel resistance, was evaluated for its in vivo inhibitory effect on ADP-induced platelet aggregation in rats. The ...
4-Substituted-2-Methoxyphenol: Suitable Building Block to Prepare New Bioactive Natural-like Hydroxylated Biphenyls [0.03%]
4-取代的2-甲氧基苯酚：构建具有生物活性的类似天然茋化合物羟基联苯的新构件
Maria Antonietta Dettori,Davide Fabbri,Marina Pisano et al.
Maria Antonietta Dettori et al.
A small collection of eugenol- and curcumin-analog hydroxylated biphenyls was prepared by straightforward methods starting from natural 4-substituted-2-methoxyphenols and their antitumoral activity was evaluated in vitro. Two curcumin-biphe...
A Preliminary Assessment of the Structure-Activity Relationship of Benzimidazole-Based Anti-Proliferative Agents [0.03%]
苯并咪唑衍生物抗增殖活性的结构-活性关系研究初步报告
Leyte L Winfield,Dayle M Smith,Kalani Halemano et al.
Leyte L Winfield et al.
PDK1 is pivotal in the development and progression of several cancers. A 3D pharmacophore was developed for pyrazole derivatives displaying anti-proliferative activity and PDK1 inhibition. The pharmacophore was utilized in the design of ben...
In-vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models [0.03%]
新型四氢异喹啉（THIQ）及其三维药效团模型对 Ishikawa 细胞的体外抗增殖活性研究
Suresh Kumar V K Eyunni,Madhavi Gangapuram,Kinfe K Redda
Suresh Kumar V K Eyunni
The antiproliferative activities of new substituted tetrahydroisoquinolines (THIQs) are described. Their cytotoxicities against Ishikawa human endometrial cell line were determined after 72 h drug expose employing Celtiter-Glo assay at conc...
Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking [0.03%]
新双结合位点胆碱酯酶抑制剂的设计、合成及分子对接体外活性研究
Muhammad Yar,Marek Bajda,Rana Atif Mehmood et al.
Muhammad Yar et al.
Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzh...
Discovery of BRM Targeted Therapies: Novel Reactivation of an Anti-cancer Gene [0.03%]
靶向BRM的抗癌疗法发现：激活抑癌基因的新方法
Sarah Gramling,David Reisman
Sarah Gramling
Drug discovery in the field of oncology has been advanced mainly through the targeting of receptor tyrosine kinases. Both antibodies and small molecule inhibitors have been found to have successful applications in blocking the proliferative...