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A straightforward synthetic pathway was adopted to
2024-12-27

A straightforward synthetic pathway was adopted to synthesize the target compounds as outlined in . The starting chloromethylquinazolinones (–) were synthesized from anthranilic Histone deacetylase inhibitor in two steps following reported procedures., , , The first step involves chloroacetylation o
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In brief serotonin can interact with classes of receptors ar
2024-12-26

In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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In this study high concentrations mM
2024-12-26

In this study, high concentrations (0.5–4 mM) of thuringiensin were required to stimulate the basal adenylate cyclase activity Fig. 2, Fig. 3, Fig. 4, but low concentrations of thuringiensin (1–100 μM) were sufficient to inhibit the forskolin-stimulated adenylate cyclase activity in rat cerebral cor
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Adenosine is a ubiquitous homeostatic substance released fro
2024-12-26

Adenosine is a ubiquitous homeostatic substance released from most cells, including neurons and glias. Endogenous adenosine acts at four principal G-protein-associated receptor subtypes: A1, A2a, A2b and A3 (Ralevic and Burnstock, 1998). The stimulation of adenosine receptors by extracellular adenos
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It is worth mentioning that cordycepin as an
2024-12-26

It is worth mentioning that cordycepin, as an adenosine analogue, is structurally similar to adenosine. A previous study has shown that the anti-apoptotic effects of cordycepin are partially dependent on the activation of A1R [16], and cordycepin increases theta waves power density via nonspecific
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NLX a k a F or befiradol exhibits
2024-12-26

NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in leukotriene to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it ha
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The molecular mechanisms involved in the pathogenesis of cho
2024-12-26

The molecular mechanisms involved in the pathogenesis of cholestatic pruritus remain unknown [45], [46]. Indeed, there has been an enormous effort at understanding the etiology of PBC-related pruritus, including work at the cellular and molecular level, but such efforts have not been translated into
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Crohn s disease an inflammatory bowel disease that affects t
2024-12-26

Crohn’s disease, an inflammatory bowel disease that affects the gastrointestinal (GI) tract, is characterized by a polymorphism in ULK1 autophagy gene due to the presence of single nucleotide polymorphisms (SNPs). Thus, the autophagic process is impaired during the disease. The mutations in the leuc
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In liver the essential organ
2024-12-26

In liver, the essential organ of lipoprotein synthesis, ACL plays a fundamental role in lipogenesis and steroidogenesis by supplying cytosolic cox 2 inhibitor to both pathways. By using a tricarboxylic acid cycle intermediate (citrate) to produce acetyl CoA, ACL can be seen as an important bridge b
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The Type A series contains of the confirmed hits
2024-12-26

The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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br ACL A Metabolic Checkpoint for
2024-12-26

ACL: A Metabolic Checkpoint for Sensing Excess Nutrients? During normal transitions between fasting and feeding, cells maintain energy homeostasis by integrating energy and nutrient status signals at key metabolic nodes, coordinating multiple processes. For example, the AMP-activated protein kina
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Transient transfection with ATR kinase dead D
2024-12-26

Transient transfection with ATR kinase-dead (D2475→A) [30] and ATM kinase-dead (D2870→Ala and N2875→K) [31] constructs was performed using Fugene 6 (Roche Applied Science, Indianapolis). Three microliters of fugene 6+1μg plasmid was used in transfections using 6-well plates at 2×105 cells/well and a
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Although the exact mechanisms are not fully understood
2024-12-26

Although the exact mechanisms are not fully understood, IGF-1 is tightly linked with ER and estrogen actions and a crosstalk occurs between these two systems in breast cancer. To illustrate this close relationship, studies have identified a synergy between IGF-1 and estrogen in gap27 expressing bot
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APJ is mainly coupled to
2024-12-26

APJ is mainly coupled to PTX-sensitive Gi/o proteins [33], and thus, it is associated with the inhibition of adenylyl cyclase and the activations of PI3K/Akt signaling and MAPKs signaling pathways [23], [54], [55], [56]. In a previous study, apelin stimulations of the PI3K/Akt and/or the MAPK pathwa
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Furthermore because most of foods
2024-12-26

Furthermore, because most of foods and beverages have been consumed after processing, researchers have focused on the effects of processing (e.g. blanching, cooking, drying, cooling, freezing, high-pressure treatment, pulsed electric field) on total antioxidant capacity of foods. In general, there w
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