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br TGR agonists current developments and future
2021-10-25

TGR5 agonists: current developments and future landscape The amphipathic nature of bile acids is crucial in aiding the digestion and Fenretinide of vitamins and fats. With the emerging roles of bile acids in the regulation of energy and glucose homeostasis through TGR5, the pharmaceutical industr
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br Materials and methods br Results br
2021-10-25

Materials and methods Results Discussion Chronic neuroinflammation underlies the pathogenesis of HAND (Saylor et al., 2016, Sodhi et al., 2004). Infected immune cells release viral proteins and inflammatory factors which act on microglia, astrocytes, and neurons to produce the synaptodendri
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The general synthetic routes leading to aspartate and
2021-10-25

The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic y15 analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid. It is worth mentioning that st
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We observed the reduced expression
2021-10-25

We observed the reduced expression of the GluN2a subunit in the temporal and entorhinal cortexes and ventral hippocampus, which may result in the predominance of GluN2b-containing NMDA receptors during the latent period. Previously, using the same model, we revealed the reduction of the GluN2a/GluN2
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1347 The role of the ER EK variant which
2021-10-25

The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of 1347 levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism might protect from the devel
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br Role of ghrelin in reward and addiction In
2021-10-25

Role of ghrelin in reward and addiction In addition to its well-known effects on PFTα homeostasis regulation at the hypothalamic level [reviews in (Al Massadi et al., 2017, Muller et al., 2015)], ghrelin also has the ability to increase food motivation acting on hypothalamic and extra-hypothalam
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In general substrates that undergo regulated
2021-10-25

In general substrates that undergo regulated intramembrane proteolysis are initially cleaved in the extracellular domain by sheddases such as TACE (TNFα converting enzyme) or ADAM (a disintegrin and metalloproteinase domain)/α-secretase, or by aspartyl proteases, such as BACE/β-secretase, before cle
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palovarotene receptor br Prospects The prospects for GABAerg
2021-10-25

Prospects The prospects for GABAergic palovarotene receptor can be projected from the rate at which new compounds have been introduced (Fig. 1) and the amounts used. More than three billion pounds of NCA-IA insecticides were used in the past seven decades. There was no target site cross-resistanc
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We show here that FXR is a point of
2021-10-23

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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One of the main mechanisms enabling recycling of intracellul
2021-10-23

One of the main mechanisms enabling recycling of intracellular redox-active iron is lysosomal degradation of ferritin in the process of autophagy, often referred to as ‘ferritinophagy’ [128]. Autophagy was suggested to contribute to ferroptotic cell death by promoting the degradation of iron storage
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Preadipocytes are capable of differentiating into lipid lade
2021-10-23

Preadipocytes are capable of differentiating into lipid-laden mature adipocytes. Lipid droplets are a prominent morphological feature of mature adipocytes, which is accumulated and maintained during adipocytes differentiation [26]. In this study, rHhip treatment increased lipid accumulation, as well
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Recent evidence suggests that HCA can
2021-10-23

Recent evidence suggests that HCA2 can also mediate antineuroinflammatory effects [63]. Studies in this field were initiated when monomethyl fumarate, the metabolite of DMF, was shown to be an agonist of HCA2[5]. DMF at the same time was shown to not only have beneficial effects in the treatment of
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GPR detection by reverse transcription polymerase chain
2021-10-23

GPR35 detection by reverse transcription-polymerase chain reaction (RT-PCR). Total RNA of cultured DRG neurons was extracted using the RNAqueous kit (Ambion). Complementary DNA (cDNA) was synthesized from 1μg of isolated total RNA with SuperScript III reverse transcriptase (Invitrogen). An aliquot o
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br Experimental br Acknowledgments This research
2021-10-23

Experimental Acknowledgments This research was supported by the Korea Research Foundation (2013R1A1A2007509). The authors thank to Dr. Moon Ho Son (Dong-A Pharm. Co. Ltd) for hGPR119 agonist activity assay. We also thank to Pharmacal Research Institute and Central Laboratory of Kangwon Nationa
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Tetrazole is one of the most
2021-10-23

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive a
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