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Recently a lot of synthetic FFA agonists
2022-04-15

Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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Tetrazole is one of the most commonly used bioisosteres
2022-04-15

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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DAMPs are endogenous danger signals
2022-04-15

DAMPs are endogenous danger signals that can initiate and perpetuate a noninfectious ω-Agatoxin TK during cell death [23]. HMGB1 is a well-studied nuclear DAMP in various types of regulated necrosis and has been implicated in the pathogenesis of infection and sterile inflammation. Our current data
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The physicochemical properties of the
2022-04-15

The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-ala
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Pomalidomide receptor Factor Xa FXa has emerged as a particu
2022-04-15

Factor Xa (FXa) has emerged as a particularly promising target for the development of effective anticoagulant drugs because FXa acts at the convergence point of the extrinsic and intrinsic coagulation pathways. It efficiently catalyzes the conversion of prothrombin to thrombin with one molecule of F
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The eel and perhaps other euryhaline teleost
2022-04-14

The eel, and perhaps other euryhaline teleost fish, have the additional peptide, renoguanylin that exhibits high levels of expression within the kidney as well as the intestine. In terms of overall sequence, pre-prorenoguanylin is more homologous to pre-proguanylin than pre-prouroguanylin and a phen
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In addition for the function of GSNOR in brain since
2022-04-14

In addition, for the function of GSNOR in brain, since GSNOR is the sole alcohol dehydrogenase isozyme in brain, the failure to detect ethanol dehydrogenase activity poses a problem if it is assumed that this enzyme has evolved and developed as a protective mechanism for ethanol detoxification in th
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br Introduction Nicotinic acid has been used clinically
2022-04-14

Introduction Nicotinic Fluorescein-12-dUTP mg has been used clinically for more than 50 years [1] since it has anti-atherogenic effects, including the ability to reduce triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C), and elevate high-density lipoprotein cholesterol (HDL-C) [2]
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The hypothesis that genes involved in type diabetes evolved
2022-04-14

The hypothesis that genes involved in type 2 diabetes evolved under changing selective pressures and may carry the signature of natural selection motivated us to describe patterns of sequence variation at CAPN10 and GPR35 in human populations. An initial population genetics study reported an unusual
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In addition researchers studying GPR agonists
2022-04-14

In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it AT-406 is unclear why Sanofi-Aventis chose to terminate collaboration with Metabolex (no
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Initial evidence that cell contact mediated transmission of
2022-04-14

Initial evidence that cell-contact-mediated transmission of HIV-1 is relevant for the generation of latently infected SB743921 was suggested in the context of transmission from dendritic cells to resting CD4+ T cells (Evans et al., 2013, Kumar et al., 2015). As dendritic cells probe for antigens, t
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The activation of the ERK pathway may participate
2022-04-14

The activation of the ERK pathway may participate in the sensitization of primary afferents in pain transmission (Ji et al., 2009, Lai et al., 2011); the blockade of ERK activation in the DRG can decrease mechanical and heat hypersensitivity in inflammatory pain. IL-10 can inhibit phosphorylation of
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The average pregnancy rate in this work
2022-04-14

The average pregnancy rate in this work was 60.1%; similar results have been reported with the same estrus synchronization treatment (58% pregnancy rate) [26]. Later studies also showed that the pregnancy rate was 56.9 and 51.1%, with FTAI and estrous detection, respectively [34,35]. Although that t
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br Expression of GlyT in the spinal
2022-04-14

Expression of GlyT in the spinal cord in response to neuropathic pain Twelve days after sham injury or CCI, GlyT1 and GlyT2 mRNA expression in rat spinal cord was analyzed using qPCR. Here, no significant changes in expression of the transporters in our CCI model of neuropathic pain compared with
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However the GPR R H polymorphism was reported to affect
2022-04-14

However, the GPR40 R211H polymorphism was reported to affect the variation of insulin secretory capacity in other ethnic groups. The allele frequency of H211 in Japanese was 78.4%.102, 103 By comparing clinical and metabolic parameters among Japanese men, Ogawa et al. found that histidine homozygote
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