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Subsequently BAs are secreted in the
2021-10-01
Subsequently, BAs are secreted in the portal vein by the heterodimeric organic solute transporter OSTα/β [15]. At this level, BAs are transported back to the liver, where the great majority is reabsorbed by the sodium (Na)-Taurocholate Cotransporter Protein (NTCP) and organic anion transporting poly
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Accumulating evidence suggests that the NGF
2021-10-01
Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, fccp derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37]. BDNF knockout mice d
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br STAR Methods br Author Contributions br Introduction
2021-10-01
STAR★Methods Author Contributions Introduction Hyaluronan, a major constituent of the extracellular matrix (ECM), is produced by hyaluronan synthases (HASs) and degraded by hyaluronidases (HYALs) (Vigetti et al., 2014). Physiologically, hyaluronan exists in a form with a molecular weight of
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Free fatty acid receptor FFAR also known as GPR
2021-10-01
Free fatty S63845 receptor 1 (FFAR1, also known as GPR40) belongs to the family of G protein-coupled receptors (GPCRs) and was de-orphanized in 2003 as a receptor for medium-to long-chain free fatty acids (FFAs) [9,10]. Mainly expressed in beta cells of pancreatic islets, GPR40 can be activated by
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Although the ramifications of non additive
2021-10-01
Although the ramifications of non-additive SAR are context-dependent, the knowledge that perturbations in one region of a chemical series are not synergistic with perturbations in another region of the same chemical series is clearly pertinent to any medicinal chemistry effort. In our experience, no
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br Conclusion and future directions
2021-10-01
Conclusion and future directions GS is an important therapeutic target for the treatment of Alzheimer's disease. Its structure and function have been studied during the last years to understand the substrate cleavage mechanism to modulate the Aβ42 peptide production. The recent elucidation of GS
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In our study the changes in
2021-10-01
In our study, the changes in the α4 and δ subunit expression were accompanied by a significant increase in γ2 subunit expression in almost all analysed hippocampal structures in the fully kindled animals. In contrast, an acute injection of PTZ at a convulsive dose (55mg/kg) evoked a potent decrease
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In addition to the type
2021-10-01
In addition to the type of food consumed, also the effect of calorie restriction (CR), i.e. an intermittent fasting and re-feeding cycles with concomitant fluctuations in the level of glucose and insulin, can affect the course of IBS through the modulation of the BA homeostasis. This type of nutriti
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We show here that FXR is a point of convergence
2021-10-01
We show here that FXR is a point of convergence of heredity (H) and environmental (E) risk factors for CRC (re the Tomasetti and Vogelstein model). Our studies demonstrate that the APC mutation and high-fat diet independently and cooperatively increase the BA pool that results in the repression of F
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The improved glucose tolerance of Ffar R W R
2021-09-30
The improved glucose tolerance of Ffar1R258W/R258W mice on HFD was unexpected. In combination with similar fasting blood glucose levels, the significant lower fasting plasma insulin of mutant mice compared to wild-type mice is indicative of improved insulin sensitivity. However, peripheral insulin r
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In the course of an internal FAAH program many very
2021-09-30
In the course of an internal FAAH, program,, , , , , , , , , , , , , many very similar compounds were profiled in vivo with particular interest paid to their ability to penetrate the BBB. The compounds profiled were heteroaryl piperazinyl and piperadinyl ureas; a class of compounds, reported on pre
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Compared to the other histamine receptor subtypes the H
2021-09-30
Compared to the other MDV3100 receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (2005) and Bon
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One of the possibilities of HO targeting
2021-09-30
One of the possibilities of HO-1 targeting is gene therapy. So far, the majority of preclinical studies have focused on recombinant adeno-associated viral (rAAV) vectors as DNA carriers. They not only provide stable, long-term transgene expression in non-dividing NU 1025 but also have very limited i
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GPR belongs to the G protein coupled receptor family and
2021-09-30
GPR84 belongs to the G protein-coupled receptor family, and it was first identified from human peripheral blood neutrophils [,]. GPR84 is now considered to be a member of receptor for medium chain fatty SB431542 (MCFA) with carbon chain lengths of 9–14 []. GPR84 is mainly expressed in bone marrow,
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The difference in the expression of
2021-09-30
The difference in the expression of functional FFARs between neutrophils and monocytes/macrophages suggests that the role of FFA2R may be restricted to the very early phase of acute inflammation where neutrophils are dominating players called into action, whereas GPR84 may have a broader functional
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