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Although the role of apelin and APJ receptor in
2023-12-25
Although the role of apelin and APJ receptor in cardiovascular functions has been well-elucidated, little is known for the effect of the central apelinergic system on gastrointestinal (GI) functions. In mice, it has been found previously that central exogenous apelin-13 decreased gastric emptying (G
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Voriconazole Nanoparticles are submicrometric systems smalle
2023-12-25
Nanoparticles are submicrometric systems smaller than 1000 nm which high surface area and composite materials may allow their greater interaction with biological membranes and control of the drug release. These features are directly associated with the efficacy of treatment and the presence of adver
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br Alzheimer s disease AD is an irreversible age associated
2023-12-22
Alzheimer’s disease (AD) is an irreversible, age-associated neurodegenerative disorder that is characterized by progressive memory loss and cognitive decline. AD is also the leading cause of dementia, accounting for 5 million cases in the United States and 44 million cases worldwide. In 2015, AD c
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ALDHs also act as opposite roles in the initiation
2023-12-22
ALDHs also act as opposite roles in the initiation and development of carcinoma. For example, ALDH2, as a key enzyme which oxidises acetaldehyde, participates in alcohol metabolism and is associated with alcohol-mediated carcinogenesis [37]. It has been reported that up to 8% of the world's populati
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Analyses of brain CSCs isolated from pediatric
2023-12-22
Analyses of flt3 CSCs isolated from 24 pediatric and six adult brain tumors detected ALDH levels proportional to tumor type and aggressiveness. ALDH-expressing cells (ALDH+) formed spheroids while ALDH1 pharmacological inhibition by a combination of DEAB and RA decreased significantly sphere number
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ras inhibitor Medium spiny neurons MSNs in the
2023-12-22
Medium spiny neurons (MSNs) in the striatum start from a deeply hyperpolarized resting membrane potential, slowly depolarize and show a delayed start of firing during a current injection (Kawaguchi, 1993, Nisenbaum and Wilson, 1995, Planert et al., 2013). The firing pattern during the current inject
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The importance of insulin in controlling
2023-12-22
The importance of insulin in controlling lipolysis and fat mass is further emphasized by mouse models with alterations in the insulin signaling pathway of adipocytes. For example, mice with a tamoxifen-inducible knockout of the insulin receptor in mature adipocytes reveal a substantial decrease of a
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VEGFR Tyrosine Kinase Inhibitor II sale Derivatives of M tha
2023-12-22
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these VEGFR Tyrosine Kinase Inhibitor II sale to maintain 5-HTR antagonist properties
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br AD and COX LOX pharmacology Early
2023-12-22
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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The cellular mechanism underlying the CGS
2023-12-22
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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The benzimidazole group seems to be a
2023-12-22
The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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Elevated expression of Aurora A and B frequently detected in
2023-12-22
Elevated expression of Aurora-A and -B frequently detected in a wide variety of human cancers strongly indicate that high expression of these kinases play roles in the development of cancer associated phenotypes. While Aurora-A has been shown to function as an oncogene when over expressed in mammali
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The acidification of endocytic compartments is
2023-12-22
The acidification of endocytic compartments is closely related to endocytic activity, although the mechanism linking acidification and membrane dynamics is largely unknown. In a recent RNA interference (RNAi)-based screen, V-ATPase depletion blocked the formation of clathrin-coated vesicles, an effe
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The distribution and subcellular localization
2023-12-22
The distribution and subcellular localization differs between the subtypes of mGlu receptors. Most mGlu receptors are broadly expressed in the brain, except for mGlu6, which is restricted to the retina. Some mGlu receptors are additionally found in glial cells, such as mGlu3 and mGlu5 (Aronica et al
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From an historical perspective ligands for GPCRs adrenaline
2023-12-22
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, AS1404 or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were rapi
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