Kinetic Properties of Glutamate Carboxypeptidase II Partially Purified from Leukodystrophy Patient's Serum [0.03%]
用溶栓病患者血清粗提的谷氨酸氨基肽酶的部分纯化液的活性性质研究
Aws Z Abdulmajeed,Wasan Nazhan
Aws Z Abdulmajeed
Glutamate carboxypeptidase II (GCPII), a metallopeptidase, is a recently identified pharmacologically targeted protein that is predominantly expressed in the human central nervous system, where it degrades the most abundant neuropeptide in ...
Quinazolinone-Hydrazine Cyanoacetamide Hybrids as Potent Multitarget-Directed Druggable Therapeutics against Alzheimer's Disease: Design, Synthesis, and Biochemical, In Silico, and Mechanistic Analyses [0.03%]
用于治疗阿尔茨海默病的喹唑啉酮-肼类氰基乙酰胺杂环化合物作为多种作用靶点药物的设计、合成及生化分析、计算机辅助分析和机理分析
Kandrakonda Yelamanda Rao,Remya Chandran,K V Dileep et al.
Kandrakonda Yelamanda Rao et al.
The discovery of effective multitarget-directed ligands (MTDLs) against multifactorial Alzheimer's disease (AD) remnants has been focused in an incessant drug discovery pursuit. In this perception, the current study explores the rational de...
Nanoscale Structural Characterization of Amyloid β 1-42 Oligomers and Fibrils Grown in the Presence of Fatty Acids [0.03%]
脂肪酸存在下生长的β淀粉样蛋白1-42寡聚体和原纤维的纳米结构特征分析
Kiryl Zhaliazka,Dmitry Kurouski
Kiryl Zhaliazka
Mono- and polyunsaturated fatty acids (FAs) are broadly used as food supplements. However, their effect on the aggregation of amyloidogenic proteins remains unclear. In this study, we investigated the effect of a large number of mono- and p...
Unraveling the Structure and Dynamics of Ac-PHF6-NH2 Tau Segment Oligomers [0.03%]
解开Ac-PHF6-NH2Tau片段寡聚体的结构和动力学
Iuliia Stroganova,Zenon Toprakcioglu,Hannah Willenberg et al.
Iuliia Stroganova et al.
The aggregation of the proteins tau and amyloid-β is a salient feature of Alzheimer's disease, the most common form of neurodegenerative disorders. Upon aggregation, proteins transition from their soluble, monomeric, and functional state i...
Repurposing Anakinra for Alzheimer's Disease: The In Vitro and In Vivo Effects of Anakinra on LPS- and AC-Induced Neuroinflammation [0.03%]
安卡拉用于阿尔茨海默病的研究：安卡拉对LPS和AC诱导的神经炎症的体内和体外效应研究
Thaarvena Retinasamy,Amber Lot Yee Lee,Hsien Siang Lee et al.
Thaarvena Retinasamy et al.
Alzheimer's disease is a significant global health issue, and studies suggest that neuroinflammation plays a vital role in the advancement of this disease. In this study, anakinra has been shown to display a time- and concentration-dependen...
Discovery of New Highly Potent Histamine H3 Receptor Antagonists, Calcium Channel Blockers, and Acetylcholinesterase Inhibitors [0.03%]
新型高活性组胺H3受体拮抗剂、钙通道阻滞剂和乙酰胆碱酯酶抑制剂的发现
Rim Malek,Kinga Sałat,Perle Totoson et al.
Rim Malek et al.
At present, one of the most promising strategies to tackle the complex challenges posed by Alzheimer's disease (AD) involves the development of novel multitarget-directed ligands (MTDLs). To this end, we designed and synthesized nine new MT...
Insights into Vincristine-Induced Peripheral Neuropathy in Aged Rats: Wallerian Degeneration, Oxidative Damage, and Alterations in ATPase Enzymes [0.03%]
关于老龄大鼠长春新碱诱导的外周神经病变：沃勒变性、氧化损伤及ATP酶改变
Ketlyn P da Motta,Carolina C Martins,Vanessa M E da Rocha et al.
Ketlyn P da Motta et al.
This study aimed to elucidate vincristine (VCR)-induced peripheral neuropathy in aged rats, a poorly understood neurotoxicity. Both young and old Wistar rats were administered VCR (0.1 mg/kg, intraperitoneally (i.p.)) and compared to age-ma...
Single-Molecule Fingerprinting Reveals Different Growth Mechanisms in Seed Amplification Assays for Different Polymorphs of α-Synuclein Fibrils [0.03%]
单分子指纹识别揭示了α-突触核蛋白多晶型原纤维种子放大试验中的不同生长机制
Derrick Lau,Yuan Tang,Vijaya Kenche et al.
Derrick Lau et al.
α-Synuclein (αSyn) aggregates, detected in the biofluids of patients with Parkinson's disease (PD), have the ability to catalyze their own aggregation, leading to an increase in the number and size of aggregates. This self-templated ampli...
Discovery of VU6007496: Challenges in the Development of an M1 Positive Allosteric Modulator Backup Candidate [0.03%]
VU6007496的发现及其作为M1阳性 allosteric调制剂备选药物开发过程中遇到的问题与挑战
Julie L Engers,Katrina A Bollinger,Rory A Capstick et al.
Julie L Engers et al.
Herein we report progress toward a backup clinical candidate to the M1 positive allosteric modulator (PAM) VU319/ACP-319. Scaffold-hopping from the pyrrolo[2,3-b]pyridine-based M1 PAM VU6007477 to isomeric pyrrolo[3,2-b]pyridine and thieno[...
Kappa Opioid Receptor Activation Induces Epigenetic Silencing of Brain-Derived Neurotropic Factor via HDAC5 in Depression [0.03%]
kappa阿片受体通过HDAC5诱导抑郁症中脑源性神经营养因子的表观遗传沉默
Anubhav Yadav,Shalini Dogra,Arun Kumar Boda et al.
Anubhav Yadav et al.
Treatment-resistant depression (TRD) occurs in almost 50% of the depressed patients. Central kappa opioid receptor (KOR) agonism has been demonstrated to induce depression and anxiety, while KOR antagonism alleviates depression-like symptom...