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In conclusion this is the first description of
2022-09-16
In conclusion, this is the first description of a GPR81 agonist with an ability to exert in vivo efficacy without causing flushing. These results demonstrate that GPR81 small-molecule agonists may be effective for treating dyslipidemia. In addition, targeting GPR81 could prevent the unwanted side ef
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Finally our data found that the
2022-09-16
Finally, our data found that the EBV dUTPase protein modulates tryptophan, serotonin, and DA metabolism and use in vitro and in vivo. The EBV dUTPase may alter kynurenine catabolism in microglia in vitro, suggesting that there is an increase synthesis of quinolinic acid. Quinolinic acid, an agonist
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Obestatin synthetized mainly in the gastrointestinal tract p
2022-09-16
Obestatin, synthetized mainly in the gastrointestinal tract, participates in the regulation of metabolic functioning at both central and peripheral levels (food intake, pancreatic activity or/and adipocytes proliferation) (Granata et al., 2008; Li et al., 2011). It is involved in the complex gut-bra
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The amyloid precursor protein APP is a membrane protein
2022-09-16
The amyloid precursor protein (APP) is a membrane protein thought to be involved in plasticity, synapse formation and repair, and export of metal ions [68]. The APP present in the brain can be cleaved by three different secretases [73], [74]. Cleavage of APP first by alpha secretase and then gamma-s
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PF-04449913 Studies of human and mouse GPR as ascertained
2022-09-16
Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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Yeast two hybrid screening studies have provided the foundat
2022-09-16
Yeast two-hybrid screening studies have provided the foundation for countless investigations of protein-protein interactions [[141], [142], [143]]. To identify additional hepatic proteins similar to GKRP that are implicated in GCK regulation, a group of researchers conducted a two-hybrid study using
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In the present study we set
2022-09-16
In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmacop
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While CART increased circulating levels of GIP
2022-09-16
While CART increased circulating levels of GIP and GLP-1 in vivo, we were unable to detect any effect of exogenous CART on GIP and GLP-1 mRNA expression or GLP-1 secretion in vitro. There is no ready explanation for this discrepancy. The CART doses used (both in vivo and in vitro) have been shown to
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Considering together the conformational docking and SAR
2022-09-15
Considering together the conformational, docking and SAR results of this and of previously published papers, a three points pharmacophore model can be developed considering the indispensable residues of SRSRY derived antagonists, namely Arg89, Arg91 and Tyr92. This model is shown in Fig. 10, and req
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Till date the first line treatment of T
2022-09-15
Till date, the first line treatment of T2DM is oral metformin followed by oral sulfonylureas, dipeptidyl peptidase-IV-inhibitors, and TZDs. As the disease progresses, injectable glucagon-like peptide-I analogues or ultimately insulin become necessary to maintain glycaemic control. Despite the establ
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The deduced amino acid sequences of
2022-09-15
The deduced amino adenylate cyclase sequences of all scIPPSs display high similarity, and sequence alignments reveal seven conserved regions [2]. Regions II and VI contain the substrate-binding regions, with two characteristic aspartate-rich motifs (DDx(xx)xD; where x represents any amino acid resid
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Despite these multiple mechanisms of
2022-09-15
Despite these multiple mechanisms of viral persistence, one patient has been reportedly cured from HIV-1 infection . Timothy Brown, also known as the 'Berlin patient', was diagnosed with HIV-1 infection in 1995. After controlling viremia for several years via cART, he was diagnosed with acute myeloi
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Despite these multiple mechanisms of
2022-09-15
Despite these multiple mechanisms of viral persistence, one patient has been reportedly cured from HIV-1 infection . Timothy Brown, also known as the 'Berlin patient', was diagnosed with HIV-1 infection in 1995. After controlling viremia for several years via cART, he was diagnosed with acute myeloi
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The even bigger surprise was the second
2022-09-15
The even bigger surprise was the second feature of both structures. Interestingly, binding of the MRG domain hardly altered the conformation of the SET domain compared with its apo state (An et al., 2011). What did change, however, is the conformation of the ASH1L auto-inhibitory loop (Figure 1). De
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br Disp Mediated Hh Membrane Recycling Due to its cholestero
2022-09-14
Disp-Mediated Hh Membrane Recycling Due to its cholesterol modification, Drosophila Hh enriches on sphingolipid-rich apical membranes of polarized epithelial LDC000067 33., 38., 39.. Genetic studies examining Hh release from wing imaginal disc epithelia suggest that Hh must be endocytosed from t
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