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fauc sale br Surrogate ligands for GPR Although identificati
2022-09-16

Surrogate ligands for GPR35 Although identification of endogenously produced chemicals with agonist action at GPR35 is of considerable importance, the ligands described above are far from ideal to probe the roles of GPR35. Surrogate ligands are therefore required. Until recently, the key GPR35 ag
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It is well known that
2022-09-16

It is well known that 12-O-tetradecanoylphorbol-13-acetate (TPA) is a tumor promoting agent of skin carcinogenesis in rodents [12]. TPA stimulates a variety of cellular functions in cancer cells, including cell motile activity [13], [14]. In our recent study, when liver epithelial cells were treated
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It appears that not all GPR agonists require a
2022-09-16

It appears that not all GPR119 agonists require a high dose to elicit acceptable 1,2-Dilauroyl-sn-glycerol control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved
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br Experimental br Acknowledgments The authors are grateful
2022-09-16

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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Recently a G protein coupled
2022-09-16

Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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Estrus expression after removal of P insert and
2022-09-16

Estrus 1 25-dihydroxyvitamin d3 after removal of P4 insert and before TAI is a clear predictor of greater P/AI in protocols that use GnRH [6,8], EB, or ECP [10,18] as ovulation inducers. Therefore, our third hypothesis was that heifers showing estrus behavior would have greater P/AI, which was supp
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We compared the age BMI and relevant laboratory variables be
2022-09-16

We compared the age, BMI and relevant laboratory variables between the two groups of risk factor multiplicity. The results are presented in Table 7 for the women and in Table 8 for the men. The individuals with an increased erythrocyte adhesiveness/aggregation can clearly be seen to be older, more o
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In a previous study M ykkynen et al
2022-09-16

In a previous study (Möykkynen et al., 2003), we reported that ethanol lengthens the time needed for the AMPA receptors to recovery from desensitization in isolated hippocampal neurons. Here, we did not observe any effect of ethanol on recovery from desensitization in recombinant homomeric GluR-D re
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Transmembrane AMPA receptor regulatory proteins TARPs are
2022-09-16

Transmembrane AMPA receptor regulatory proteins (TARPs) are a relatively newly discovered protein family. Prototypic TARP, stargazin, was found by a spontaneous mutation in ataxic stargazer mouse line as a homologous protein to γ1 calcium channel subunit (Letts et al., 1998). The role of stargazin i
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Although encoded by a single gene GR displays considerable h
2022-09-16

Although encoded by a single gene, GR displays considerable heterogeneity through the combined effects of alternative mRNA splicing, alternative translation initiation, and complex post-translational modification. Differential expression of the various GR isoforms may contribute to tissue-specific f
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C steroids and their glycosylation products distribute widel
2022-09-16

C21 steroids and their glycosylation products distribute widely in Asclepiadaceae plants. Their anticancer activities have been shown in different human cell lines and in vivo animal experiments [[27], [28], [29], [30], [31], [32]]. However, the mechanisms of their anticancer activities are still un
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mth1 pathway One effective approach to fine tuning the lipop
2022-09-15

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic mth1 pathway scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as A
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The G protein coupled receptor GPR also called FFAR
2022-09-15

The G protein-coupled receptor, GPR40 (also called FFAR1) responds to medium and long chain unsaturated fatty acids, resulting in increase of insulin secretion during elevated glucose levels. The glucose dependency of insulin secretion makes this receptor a very good target for developing therapies
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br The potential of EPA Ffar signaling as a
2022-09-15

The potential of EPA-Ffar4 signaling as a novel intervention for HFpEF Conclusions and future directions Optimization of ω3-PUFA/EPA-therapy based upon titration to achieve therapeutic levels: A pressing clinical challenge is to continue to define the benefit of ω3-PUFA/EPA-therapy. Recent ana
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growth hormone secretagogue receptor As a part of our
2022-09-15

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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