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Elimination of the Q R
2022-06-13
Elimination of the Q234–R244 bridge significantly affected the protein omecamtiv synthesis but had little effect on its activity at a permissive temperature, which may seem contrary to the known functional importance of this motif in Fpg. However, since the mutants fully or partially retained the b
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br Material and methods br Results
2022-06-13
Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a
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Moreover intestinal chronic inflammation is a promoting fact
2022-06-10
Moreover, intestinal chronic inflammation is a promoting factor in the development of CRC in patients affected by inflammatory bowel disease (IBD), such as Crohn's disease and ulcerative colitis. We have previously shown that pharmacological FXR activation via its ligand obeticolic A-1331852 counte
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br Short Communication Free fatty acid receptors FFAR play s
2022-06-10
Short Communication Free fatty Z-Ligustilide synthesis receptors (FFAR) play significant roles in energy metabolism (Brown et al., 2005; Ichimura et al., 2009). The receptor FFAR1 is involved in insulin secretion in humans (Meidute Abaraviciene et al., 2013). Activation of the receptor FFAR2 incr
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The PK and the tissue distribution profiles of k j
2022-06-10
The PK and the tissue distribution profiles of 15k, 15j, 14d and 2 (Table 8) in male ICR mice were assessed. 15k, 15j, 14d all exhibited prolonged half-lives and improved plasma exposure. 15k achieved the highest concentration (15.45 μg/mL) in plasma among four compounds. The observation that 15j (S
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br Author contributions statement P N Y designed
2022-06-10
Author contributions statement P.N.Y. designed the study, analyzed the data and prepared the draft of the manuscript. C.S performed the experiments, analyzed the data and generated Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5, Fig. 6, Fig. 7, Fig. 8. A.K. and S.D. made Supplementary Figs. S1 and S2. D.
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For our test subjects we used established high fat
2022-06-10
For our test subjects, we used established high fat diet–induced obese (eDIO) male mices T2DM models. The establishment of eDIO mice was accomplished with a 60% high fat diet ad libitum over a 14 week period (initiated at 6 weeks of age). Compared with regularly-dieted mice, the eDIO ones weigh sign
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br Site of expression FASTK is expressed
2022-06-10
Site of expression FASTK is expressed in various parts of human body including heart, skeletal muscle, brain, placenta, lung, liver, kidney pancreas (Ota et al., 2004) and many other organs (Fig. 1). It has been reported that FASTK is highly expressed in pancreatic tumors, where it is involved in
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The inhibitory activities of the compounds with the
2022-06-10
The inhibitory activities of the compounds with the modification of the amino group against human liver FBPase are summarized in . Replacement of the amino group of with hydrophobic substituent such as a methyl group () led to a substantial loss of activity (IC=995nM). Similarly, replacement with h
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Telotristat The zinc dependent HDACs are classified into fou
2022-06-10
The zinc-dependent HDACs are classified into four groups based on their structure, complex formation, and expression pattern: class I (HDAC1, HDAC2, HDAC3, and HDAC8), class IIa (HDAC4, HDAC5, HDAC7, and HDAC9), class IIb (HDAC6 and HDAC10), and class IV (HDAC11) [16]. We recently reported on a cyto
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br All platelet agonists acting
2022-06-10
All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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br Rho family GTPases are molecular switches
2022-06-10
Rho-family GTPases are molecular switches; most which cycle from an ‘on’ GTP bound state to an ‘off’ GDP bound state, driven by GEFs (guanine nucleotide exchange factors) and GAPs (GTPase-activating proteins) respectively. Association with lipid membranes through a lipid (farnesyl or geranylgerany
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By combining the results of the melting curve
2022-06-10
By combining the results of the melting curve analysis of exon 5 and exon 6, the allelic setup of our 250 subjects was determined; the four allelic variants are shown in Table 1. However, GSTP1-1 *A/*C and GSTP1-1 *B/*D could not be distinguished from one another because both genotypes are character
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br S NO signalling during the
2022-06-10
(S)NO signalling during the plant immune response Redox signalling molecules must exhibit specificity for their target substrate. Moreover, a given redox-based modification must be reversible to ensure transient signalling. Oxidative cysteine (Cys) modifications are integral to a variety of redox
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Ning et al showed that LPC appeared to increase
2022-06-10
Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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