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The current gold standard for diagnosing BAM or BAD
2022-03-25

The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) CRT 0066101 (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugated taurocholic acid an
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We next determined the selectivity profile of the most
2022-03-25

We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty Rosiglitazone maleate receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affinit
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br Fenton reaction based nanomaterials for ferroptosis In
2022-03-24

Fenton reaction-based nanomaterials for ferroptosis In Fenton reaction, H2O2 is converted by Fe2+ or Fe3+ to highly oxidative ROS (Eqs. (1) and (2)), which is commonly used to catalyze the degradation of refractory organics [34]. Since the tumor microenvironment is characterized by low acidity an
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Taken together the four HRs couple with several different si
2022-03-24

Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc
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As an inflammatory mediator histamine plays a pivotal
2022-03-24

As an inflammatory mediator, histamine plays a pivotal role in nociceptive processes in both the central and peripheral nervous systems (Gemkow et al., 2009; Hough & Rice, 2011; Tiligada et al., 2009). In this respect, the participation of H3Rs in modulating pain, especially neuropathic pain, has at
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Arena Pharmaceutical introduced a biaryl sulfone derivative
2022-03-24

Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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br Surrogate ligands for GPR Although identification of
2022-03-24

Surrogate ligands for GPR35 Although identification of endogenously produced chemicals with agonist action at GPR35 is of considerable importance, the ligands described above are far from ideal to probe the roles of GPR35. Surrogate ligands are therefore required. Until recently, the key GPR35 ag
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To facilitate the development of
2022-03-24

To facilitate the development of novel diagnostic and therapeutic interventions in NASH, a plethora of animal models have been used to identify molecular targets that are involved in the onset and progression of NASH. In view of recent advances in the understanding of the pathogenesis of NASH and pr
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br Materials and methods br Results br Discussion To
2022-03-24

Materials and methods Results Discussion To fulfill its role in tissue homeostasis, repair and immunoregulation, MSCs must be able to (i) renew themselves by cell division and proliferation, (ii) migrate to its target end-site in response to chemotaxis signals and (iii) undergo appropriate
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br Conflict of interest br
2022-03-24

Conflict of interest CRediT authorship contribution statement Magdalena Olga Ciechanowska: Conceptualization, Data curation, Investigation, Methodology, Project administration, Writing - original draft. Magdalena Łapot: Formal analysis, Investigation, Methodology. Marek Kowalczyk: Writing - re
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Reports of hyperlocomotion after administration of ALX
2022-03-24

Reports of hyperlocomotion after administration of ALX-5407 [27] coupled with the lack of hyperlocomotion after administration of SSR504734, a non-sarcosine, long-residence time, competitive inhibitor [19], suggested that the GlyT1 inhibitor chemotype may impact OP. Furthermore, a compound with a co
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Our inhibitor studies revealed the presence of
2022-03-24

Our inhibitor studies revealed the presence of a signaling network triggered by dicarbonyl stress. Nevertheless, p38-MAPK activation was clearly necessary for NADPH-oxidase mediated production of ROS. This is consistent with data from other groups using different cell culture systems [37], [38], [39
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br Methods and materials br Results and discussion
2022-03-24

Methods and materials Results and discussion Conclusions This is the first study that attempted to isolate, purify and identify the characteristics of Salmeterol xinafoate from ginseng. In vitro studies have demonstrated that PGL-1 efficiently suppressed SH-SY5Y cell apoptosis induced by A
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br Conclusion br Experimental procedures br Introduction The
2022-03-24

Conclusion Experimental procedures Introduction The glycine receptor (GlyR) is a member of the Cys-loop family of ligand-gated ion channels. It is the primary inhibitory receptor in the brainstem and spinal cord but also plays important roles in higher Chymostatin synthesis regions, includ
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Natural products have been always
2022-03-24

Natural products have been always the most important and productive sources of lead compounds for the development of drugs [[15], [16], [17]]. A variety of potent α-glucosidase inhibitors have been identified from natural products, such as quercetin, resveratrol, isorhamnetin, calein C and curcumin
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