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br AD and COX LOX pharmacology Early studies on
2025-02-06
AD and COX/5-LOX pharmacology Early studies on the role of cyclooxygenases in AD were inspired by epidemiological data suggesting that COX inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs) could be beneficial in AD patients (Lucca et al., 1994, McGeer et al., 1990). This line of re
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HT receptors are distributed throughout the brain
2025-02-06
5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and Aminoglycoside antibiotic (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 19
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The synthetic route to M developed
2025-02-06
The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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br Introduction Stroke is a devastating condition that cause
2025-02-06
Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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br Aurora A Aurora B and Aurora
2025-02-06
Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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On the other hand key enzymes also involved in NO
2025-02-06
On the other hand, key YAP-TEAD Inhibitor 1 also involved in NO metabolism are nNOS and eNOS. Apparently, during acute ischemia, eNOS activity and NO concentration surge for a short period of time (Schulz et al., 2004) but eventually the expression and activity of the synthase and consequently NO c
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Angiogenesis refers to the formation of new blood
2025-02-05
Angiogenesis refers to the formation of new blood vessels from pre-existing vasculature [1]. Physiological angiogenesis is necessary for key processes such as wound healing, tissue regeneration and repair. In pathological conditions, including cardiovascular diseases, diabetes, cancer, and other pat
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br Acknowledgements br Introduction The
2025-02-05
Acknowledgements Introduction The angiogenic ocular conditions represent the most common cause of blindness in developed countries [1]. It can affect all ages, for example, retinopathy of prematurity (ROP) in infants [2], [3], diabetic retinopathy (DR) [4] in working age adults and age-related
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br Acknowledgements br Introduction Microbial enzymes
2025-02-05
Acknowledgements Introduction Microbial enzymes have gained interest for their widespread uses in industries and medicine owing to their stability, catalytic activity, and ease of production and optimization than plant and animal enzymes (Singh et al., 2016). Microbial aminopeptidases (amino-a
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br Discussion The patient presented initially only with pari
2025-02-05
Discussion The patient presented initially only with parietal symptoms in the form of acalculia, visuo-spatial deficits, and visuo-perceptual deficits and dressing apraxia. He also had simultognosia as early symptoms. Later when the disease progressed he had recent memory deficits and language in
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IKK-2 inhibitor VIII NF-kB This chemistry paved way for mult
2025-02-05
This chemistry paved way for multi-gram synthesis of which was utilized for extensive piperazine benzamide SAR exploration. Depicted in , the two-step operation towards final targets involved standard amide coupling conditions with EDC or HATU followed by Boc deprotection under acidic conditions.
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To investigate the potential link between G and
2025-02-05
To investigate the potential link between Gβγ and MT assembly in vivo, cultured NIH3T3 and PC12 cells were used. The role of Gβγ in MT assembly was demonstrated using nocodazole, a MT depolymerizing drug [14]. We found that Gβγ was preferentially bound to MTs in NIH3T3 and PC12 cells and treatment w
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br Expression of ADK in the normal
2025-02-05
Expression of ADK in the normal brain In adult brain, ADK is primarily expressed in astrocytes. Immunocytochemical analysis of adult rat and mouse Hypotaurine revealed predominant astrocytic expression throughout the hippocampus and cortex. Two isoforms of ADK have been identified in mammals, a l
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br Introduction Adenosine deaminase ADA which can
2025-02-05
Introduction Adenosine deaminase (ADA), which can catalyze the conversion of AD to inosine by removing an amino group, is a key hydrolytic enzyme of purine metabolism (Conway and Cooke, 1939), and plays an important role in an amount of diseases. For example, an increase of ADA activity in serum
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Small RhoGTPases are single domain nucleotide dependent
2025-02-05
Small RhoGTPases are single-domain nucleotide-dependent binary switches that act as highly-tuned regulators in signal transduction [1]. The cycling between active GTP-bound and inactive GDP-bound forms allows RhoGTPases to bind to or to dissociate from downstream effectors, respectively [2]. Guanine
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