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Based on work from our labs with mGlu NAMs
2022-06-13
Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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Several studies have found decreased astroglial and neuronal
2022-06-13
Several studies have found decreased astroglial and neuronal cell numbers and G-1 damage after OP exposure. Neuronal loss and brain lesions increase proportionally to the severity and duration of OP-induced seizures (Albuquerque et al., 2006, Carpentier et al., 2000, Gullapalli et al., 2010, Myhrer
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In vitro studies have shown that some
2022-06-13
In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found t
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The glucokinase protein sequence is most closely related to
2022-06-13
The glucokinase protein sequence is most closely related to the C-terminal domain of 100kD hexokinases, thus for glucokinase to evolve from a larger hexokinase ancestor it must have lost its N-terminal kinase domain. The genetic mechanism by which this occurred is currently unknown. Here we propose
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br Materials and methods br Results br
2022-06-13
Materials and methods Results Discussion Present study demonstrated the ability of a GIP agonist, D-Ala2GIP, to protect against the QA-induced neurobehavioral phenotype of HD in rats, for the first time. D-Ala2GIP treatment significantly improved the behavioral deficits, biochemical and neu
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br Some Gardos channel perplexities While much
2022-06-13
Some Gardos channel perplexities While much is known about the Gardos channel (inside Ca2+-activated K+ channel) and it's characteristics in human red blood PRX-08066 mg (e.g. [18,19]), there are a number of intriguing and unexplained phenomena that are in much need of study. One is that activat
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br GSMs Secretase cleavage of APP generates a number
2022-06-10
GSMs γ-Secretase cleavage of APP generates a number of Aβ peptides [32], [137]. In most cells Aβ1–37, 38, 39, and 42 are produced at low levels (typically each represents 5–20% of total Aβ detected) and the major species generated is Aβ1–40 (typically over 50% of total Aβ). Other Aβ peptides can
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In the intestine ethanol exposure
2022-06-10
In the intestine, ethanol exposure can change the composition of gut microbiota and promotes the growth of intestinal gram-negative bacteria, which results in the accumulation of endotoxins such as, LPS. Ethanol also impacts the integrity of the gastrointestinal mucosal barrier, increasing intestina
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br Chronic obstructive pulmonary disease COPD is characteriz
2022-06-10
Chronic obstructive pulmonary disease (COPD) is characterized by progressive obstruction of airflow, not fully reversible, which is accompanied by a chronic inflammatory response, induced by deleterious particles or gases, in airways and lung parenchyma. The most important risk factor for COPD is
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Previous research has suggested that differences in spatiote
2022-06-10
Previous research has suggested that differences in spatiotemporal regulation of intracellular signaling pathways can confer specificity to cellular responses (Marshall, 1995). Conventional approaches based on gain- or loss-of-function genetic manipulations or small-molecule inhibitors, however, lac
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BDNF is intricately implicated in
2022-06-10
BDNF is intricately implicated in energy homeostasis (Hamdouchi et al., 2016; Schwartz and Mobbs, 2012), regulation of mood (Sartorius et al., 2015) and adult neurogenesis (Taliaz et al., 2010; Waterhouse et al., 2012), our primary focus was to evaluate the effects of GPR40 stimulation on BDNF expre
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Introduction Type diabetes T D has been seriously
2022-06-10
Introduction Type 2 diabetes (T2D) has been seriously affecting the health life of 415 million people and 193 million undiagnosed people [1]. Importantly, this disease was found to cause death at least 1.5 million annually, and has brought about an extensive health concern throughout the world [2,3
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Consistent with our gene profiling analyses
2022-06-10
Consistent with our gene-profiling analyses showing that genes involved in mutual compensation of EGFR or integrin/FAK were significantly downregulated by Tinagl1 overexpression, treatment with r-Tinagl1 inhibited the activation of EGFR and FAK in vitro, and phenocopied the combined inhibition of in
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The above mentioned studies are especially important since t
2022-06-10
The above-mentioned studies are especially important since the structural alterations of the peritoneum during peritoneal dialysis are very similar to vascular and tissue alteration seen in diabetes. The tissue alterations during long-term peritoneal dialysis include a thickening and replication of
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To date the crystal structures of HIV
2022-06-10
To date, the crystal structures of HIV-1 IN complexed with ligands and related proteins could help us in studying the interactions between the inhibitors and IN. Until now, 114 co-crystal structures of HIV-1 IN with small molecular ligands 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34,
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