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The typical pharmacophore for GPR agonists
2021-10-20

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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In order to consolidate our genetic funding we
2021-10-19

In order to consolidate our genetic funding, we performed several in silico analysis regarding the p.R85W mutation. The high conservation of R85 residue in all species suggests that it has an important role in glucokinase function. Pathogenic effect of the p.R85W is supported by in silico prediction
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7-Ethoxyresorufin Andexanet alfa works as a decoy for
2021-10-19

Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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Among the isoforms of heme oxygenases HO HO and HO
2021-10-19

Among the 3 isoforms of heme oxygenases (HO-1, HO-2, and HO-3), HO-1 expression is inducible, and it catalyzes the degradation of heme to biliverdin, carbon monoxide (CO) and free Fe. The Fe is then stored in ferritin, limiting its ability to participate as a catalyst through the Fenton reaction and
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The dramatically reduced expression of CFTR in human colorec
2021-10-19

The dramatically reduced expression of CFTR in human colorectal cancer tissues identified herein is consistent with our previous findings using human breast cancer tissues, prostate cancer tissues, and colon cancer tissues, and suggests that the loss of CFTR is likely a general phenomenon in epithel
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The molecular mechanisms underlying spindle orientation are
2021-10-19

The molecular mechanisms underlying spindle orientation are still largely unknown. Budding yeast has been used to study spindle positioning and asymmetric cell division. Indeed, after cytokinesis, daughter cells have different sizes. The cell division plane is established early in the cell cycle and
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Following our initial observation of
2021-10-19

Following our initial observation of an unexpected increase in the maximal rates of cGMP formation by NO-stimulated sGC in the presence of cytosolic PCA preparations [15], we attempted to purify, identify and characterize the responsible protein(s). The purification protocol described in the present
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Angiotensin Fragment 1-7 acetate br Experimental br Acknowle
2021-10-19

Experimental Acknowledgments The authors are grateful to Fundamental Scientific Research Fund of Chinese Academy of Medical Sciences (No. 2016ZX350030) for financial support. Introduction 2-Lysophosphatidylcholines (1-acyl-glycero-3-phosphocholines, 2-LPC) are blood derived factors involve
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We found that most antigenic regions in GlyT C
2021-10-19

We found that most antigenic regions in GlyT1C are located in the second half of the GlyT1C-terminus, which is in concert with previously published results (Olivares et al., 1994). We however further show that in contrast to epitopes 554–625 which are affected by calcium only minimally, the epitopes
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In summary we discovered azaindole
2021-10-19

In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that
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Free d glutamate also has been found in
2021-10-19

Free d-glutamate also has been found in various tissues of invertebrates and vertebrates including mammals (Han et al., 2011; Ariyoshi et al., 2017), fish (Kera et al., 2001) amphibians (Kera et al., 2001), birds (Kera et al., 2001), mollusks (Tarui et al., 2003; Patel et al., 2017) and arthropods (
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His brother individual B II is months
2021-10-19

His brother, individual B.II-4, is 11 months old. He was born at term with intrauterine growth retardation. His birth weight was 2.2 kg ( can smile but does not seem to recognize his mother. He has not had any seizures. On his most recent examination (age 11 months), his weight was 7.5 kg (T (p. Arg
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Autophagy plays a multifaceted role in regulating
2021-10-18

Autophagy plays a multifaceted role in regulating both the quality and quantity of protein (e.g., protein half-life and activity) and organelles (e.g., mitochondrial number and function), thus determining cell fate [15]. The induction of autophagy has been generally considered a programmed cell surv
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Interestingly the subcellular localization of FBPase in hepa
2021-10-18

Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule Rufinamide reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the abil
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br Regulation of HO expression under conditions of ischemic
2021-10-18

Regulation of HO-1 expression under conditions of ischemic cardiac damage Heart is a vital organ with high metabolic demand, rich in mitochondria and it is very vulnerable to oxidative damage [85]. Disruption in coronary blood flow following MI leads to hypoxia (a reduction in the amount of avail
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