Roles of PI3K/AKT/PTEN Pathway as a Target for Pharmaceutical Therapy [0.03%]
PI3K/AKT/PTEN途径的药理学治疗作用及靶点功能探讨
Satoru Matsuda,Atsuko Nakanishi,Yoko Wada et al.
Satoru Matsuda et al.
Multiple enzymes participate in the phosphorylation of a group of phosphoinositide lipids. Because of their important role in signal transduction, the dysregulated metabolism of phosphoinositides represents a key step in many disease settin...
Development of a Peptide-derived orally-active kappa-opioid receptor agonist targeting peripheral pain [0.03%]
一种衍生肽口服活性κ-阿片受体激动剂的开发用于外周镇痛
Francis M Hughes Jr,Brooke E Shaner,Justin O Brower et al.
Francis M Hughes Jr et al.
Kappa-opioid agonists are particularly efficacious in the treatment of peripheral pain but suffer from central nervous system (CNS)-mediated effects that limit their development. One promising kappa-agonist is the peptidic compound CR665. A...
Design and Synthesis of Hydroxyethylene-Based BACE-1 Inhibitors Incorporating Extended P1 Substituents [0.03%]
基于羟基乙烯的β-分泌酶抑制剂的设计、合成及生物活性研究
Veronica Sandgren,Marcus Bäck,Ingemar Kvarnström et al.
Veronica Sandgren et al.
Novel BACE-1 inhibitors with a hydroxyethylene central core have been developed. Modified P1´ and extended P1 substituents were incorporated with the aim to explore potential interactions with the S1´ and the S1-S3 pocket, respectively, o...
ChemVassa: A New Method for Identifying Small Molecule Hits in Drug Discovery [0.03%]
化学瓦萨：一种新的药物发现中的小分子筛选方法
Brian Moldover,Ada Solidar,Christa Montgomery et al.
Brian Moldover et al.
ChemVassa, a new chemical structure search technology, was developed to allow rapid in silico screening of compounds for hit and hit-to-lead identification in drug development. It functions by using a novel type of molecular descriptor that...
Identification of G-Quadruplex Inducers Usinga Simple, Inexpensiveand Rapid High Throughput Assay, and TheirInhibition of Human Telomerase [0.03%]
使用简单、快速且低成本的高通量筛选鉴定诱导G-四链体的小分子并抑制人端粒酶活性
Maria Florencia Sassano,Alexander P Schlesinger,Michael B Jarstfer
Maria Florencia Sassano
Telomeres are protein and DNA complexes located atchromosome ends. Telomeric DNA is composed of a double stranded region of repetitive DNA followed by single-stranded 3' extension of aG-rich sequence. Single-stranded G-rich sequencescan fol...
Virtual Screening for Finding Novel COX-2 Inhibitors as Antitumor Agents [0.03%]
虚拟筛选发现新型COX-2抑制剂抗肿瘤先导化合物的研究
Zohreh S Badieyan,Seyed Adel Moallem,Soghra Mehri et al.
Zohreh S Badieyan et al.
The cyclooxygenase-2 (COX-2) enzyme binds to arachidonic acid resulting in the release of metabolites that induce pain and inflammatory responses. Recent studies have shown that strong COX-2 expression is highly correlated with increased tu...
Tricyclic Pyrazoles. Part 5. Novel 1,4-Dihydroindeno[1,2-c]pyrazole CB2 Ligands Using Molecular Hybridization Based on Scaffold Hopping [0.03%]
三环吡唑类化合物. 第5部分：基于骨架跃迁的分子杂交设计新型1,4-二氢吲哚并[1,2-c]吡唑类CB2配体
Gabriele Murineddu,Battistina Asproni,Stefania Ruiu et al.
Gabriele Murineddu et al.
In search of new selective CB2 ligands, the synthesis and preliminary biological evaluation of novel 1,4-dihydroindeno[1,2-c]pyrazole hybrids of the highly potent prototypicals 5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-N-fenchyl-1H-pyr...
Ernest Adeghate,Abdu Adem,Mohamed Y Hasan et al.
Ernest Adeghate et al.
Peroxisome proliferator-activated receptor (PPAR) agonists are used as adjunct therapy in the treatment of diabetes mellitus. Fibrates, including fenofibrate, gemfibrozil, benzafibrate, ciprofibrate, and clofibrate act on PPAR alpha to redu...
Medicinal Chemistry and Applications of Incretins and DPP-4 Inhibitors in the Treatment of Type 2 Diabetes Mellitus [0.03%]
肠促胰素和二肽基肽酶-4抑制剂的药物化学及在2型糖尿病治疗中的应用
Mohamed Lotfy,Jaipaul Singh,Huba Kalász et al.
Mohamed Lotfy et al.
Diabetes mellitus (DM) is a major metabolic disorder currently affecting over 200 million people worldwide. Approximately 90% of all diabetic patients suffer from Type 2 diabetes mellitus (T2DM). The world's economy coughs out billions of d...
Amylin analogues in the treatment of diabetes mellitus: medicinal chemistry and structural basis of its function [0.03%]
胰淀素类似物在糖尿病治疗中的作用及其功能的作用机制和药物化学研究进展
Ernest Adeghate,Huba Kalász
Ernest Adeghate
Amylin, (islet amyloid polypeptide) or diabetes-associated peptide is co-secreted with insulin in the islet of Langerhans of diabetic patients in approximately 1:100, amylin-insulin ratio. The soluble form of amylin, an analogue of amylin, ...