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Recently a receptor for nicotinic
2022-04-11

Recently, a receptor for nicotinic acid, named GPR109A (also known as HM74a in man or PUMA-G in the mouse) has been identified (Lorenzen et al., 2001, Lorenzen et al., 2002, Soga et al., 2003, Tunaru et al., 2003, Wise et al., 2003). This receptor, a member of the 7 transmembrane G-protein coupled f
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The rat model was validated with another agonist of
2022-04-11

The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L
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SAR around amino derivative revealed a number of interesting
2022-04-11

SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-p
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Autophagy as an important cellular process has drawn attenti
2022-04-11

Autophagy as an important cellular process has drawn attentions to its role in cardiovascular systems [16]. Autophagy is a self-digestion and degradation process that recycles the contents of the cytosol, including macromolecules and cellular organelles, resulting in self-repair and conservation for
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The results of our study indicate
2022-04-11

The results of our study indicate the general importance of the gp120 V3 loop Marizomib patch in the subunit association of primate immunodeficiency virus Env trimers. Our observation that the stem insertion mutants and hydrophobic patch mutants exhibit similar phenotypes with respect to gp120 shed
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Ginger derived glycoproteins contain a
2022-04-11

Ginger-derived flavopiridol australia contain a variety of functional components, including specific phenolic compounds, purine compounds, and bioactive polysaccharides. Moreover, glycoproteins belong to the glycoconjugates, which combine some of the properties of polysaccharides and proteins. It h
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In teleosts GR is expressed in almost
2022-04-09

In teleosts, GR is expressed in almost every cell and regulates genes controlling development, metabolism, and immune response [17,18]. Several teleosts contain two GR genes, GR1 and GR2 [8]. Other groups have found only one GR in some species thus far, such as the Japanese flounder, brown trout, an
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Our data suggest that Slc
2022-04-09

Our data suggest that Slc38a5 is important for amino-acid-induced α cell proliferation and expansion of α cell mass following GCGR inhibition, but not for formation and maintenance of α cell mass. This is supported by the finding that Slc38a5−/− mice have normal α cell mass. This is interesting sinc
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As early as glucagon was shown
2022-04-09

As early as 1957, glucagon was shown to increase phorbol 12 myristate 13 acetate expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [2
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Decoquinate synthesis Recently unimolecular multi functional
2022-04-09

Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with Decoquinate synthesis and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose contro
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br Conflict of interest br Introduction Since its
2022-04-09

Conflict of interest Introduction Since its discovery in 1958 [1]the Ca2+-dependent K+ efflux in human red blood full text(pdf) (RBC) (further referred to as the Gárdos effect) has been extensively studied (see 2, 3for review) and has been helpful in understanding the role of the Ca2+-activat
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br Chemistry Analog has been previously reported by our grou
2022-04-09

Chemistry Analog 12 has been previously reported by our group. Experimental procedures for the synthesis and characterization of 13–32 are available in Scheme 1, Schemes S1–S9 and Table S1 in Supplementary data. Preparation of 30 and 31 is depicted in Scheme 1 as the representative example. Commo
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br Introduction Farnesoid X receptor FXR
2022-04-09

Introduction Farnesoid X receptor (FXR) is a bile p2x7 receptor regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporter α (OSTα) that
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The effects of FFAR and FFAR activation in different
2022-04-09

The effects of FFAR1 and FFAR2 activation in different tissues have been reported in several species (Hara et al., 2014). Herein, we report the first evidence for differential expression of FFAR1 and FFAR2 during the peripartal period in the liver of dairy cows that differ in liver metabolism, based
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NVP-BGJ398 The typical pharmacophore for GPR agonists contai
2022-04-09

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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