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The balance and composition of
2022-07-28
The balance and composition of the gut microflora can be altered by the use of antibiotics or by colonization of the intestine by pathogens. This change may also induce, or be induced by, modifications in the body’s immune response, ultimately leading to disease. Thus, when intestinal homeostasis is
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br Conflict of interest statement br Acknowledgments The aut
2022-07-27
Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). GPR35 is an orphan G protein-coupled receptor (GPCR) implicat
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The combination of niacin with a selective PGD receptor
2022-07-27
The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data su
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br TGR agonists current developments and future landscape
2022-07-27
TGR5 agonists: current developments and future landscape The amphipathic nature of bile acids is crucial in aiding the digestion and dopamine hydrochloride of vitamins and fats. With the emerging roles of bile acids in the regulation of energy and glucose homeostasis through TGR5, the pharmaceut
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The precise mechanisms of action of PBA
2022-07-27
The precise mechanisms of action of 4-PBA are as yet ambiguous. Its capacity as a chemical chaperone has been thoroughly documented for the ABC transporter family in particular (Prulière-Escabasse et al., 2007; Iram and Cole, 2014; Gordo-Gilart et al., 2016; Pomozi et al., 2017). 4-PBA has been clas
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br Results and discussion A diverse set of compounds
2022-07-27
Results and discussion A diverse set of compounds were synthesized to improve the PK and physicochemical properties of 2. Compounds' agonist effects on hGPR40 were assessed by calcium mobilization assay using hGPR40-HEK293 cell line which stably expressed human GPR40. Preliminary explorations fo
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In the present study compared
2022-07-27
In the present study, compared to diabetic control rats, hepatic glucose-6-phosphatase activity was significantly decreased in both SE and METF treated diabetic animals, with the latter producing greater reduction in glucose-6-phosphatase activity. This observation is consistent with the claim of Ta
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CVT 10216 GCK MODY is the most common form of MODY
2022-07-27
GCK-MODY is the most common form of MODY diabetes in many populations (Chevre et al., 1998; Massa et al., 2001; Barrio et al., 2002; Estalella et al., 2007; Pruhova et al., 2010; Capuano et al., 2012; Giuffrida et al., 2017). However, data about GCK-MODY among North African populations are very rare
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In the course of our synthetic studies
2022-07-27
In the course of our synthetic studies, we also discovered an unprecedented application of Burgess reagent. Instead of generating an olefin by an intramolecular syn-elimination, the product resulting from the treatment of spirocyclic alcohols 11 and 12 with Burgess reagent led to the expansion of th
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It is widely acknowledged that CpG methylation of the promot
2022-07-27
It is widely acknowledged that CpG methylation of the promoter regions of some genes plays an important regulatory role in transcriptional regulation and in the establishment and maintenance of cell type-specific gene expression (Li, 2002, Jaenisch and Bird, 2003). This study obtained multiple lines
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As ghrelin effects are suspected to
2022-07-27
As ghrelin effects are suspected to be mediated by a heterogeneous population of G-protein-coupled-receptors [2], [21], other so far unknown subtypes of ghrelin receptors differing from the classical GHSR-1a may additionally exist that might also mediate ghrelin effects on the heart. Thus, the real
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Based on the collective experience to date it is
2022-07-27
Based on the collective experience to date, it is likely that a much more comprehensive assessment of GSI selectivity for inhibition of multiple substrates, as well as biomarkers to track inhibition of non-APP substrates in vivo will be needed to support future efforts to develop substrate selective
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The C terminal regions in both
2022-07-27
The C-terminal regions in both FGF19 and FGF21 define their KLB interaction [15], [16], [23], [25]. However, less than 40% identity in comparative alignment of C-terminal sequences for these two proteins (Table 1) suggests that their interaction with KLB may require higher-order association with oth
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br FGF FGFR pathway as
2022-07-27
FGF/FGFR pathway as predictive factor Several studies have identified FGFR1 amplification as the major predictive factor of response to FGFR inhibitors [26], [27]. However, in a recent study on lung cancer cell lines with ponatinib, FGFR1 mRNA and protein expression, together with FGF2 and FGF9
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However the clinical development of
2022-07-27
However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this rece
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