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Similar to GPR A activation of G protein coupled receptor
2022-04-11
Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic Adenosine 5-monophosphate receptor receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 200
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Chlorogenic acid mg In conclusion we provided the first evid
2022-04-09
In conclusion, we provided the first evidence of a modification and regulation of GCK by O-GlcNAc modification that until now was not explored. This discovery provides important clues in the prevention of hyperglycemia and development of novel therapeutic drugs to treat type 2 diabetes. Acknowled
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The vast majority of clinical studies have shown that chroni
2022-04-09
The vast majority of clinical studies have shown that chronic administration of GLP-1R agonists frequently lowers SBP/DBP in diabetic humans, which is consistent with preclinical studies, though the reported reductions are not as potent as those observed in their animal counterparts. In contrast, ac
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It has also been demonstrated
2022-04-09
It has also been demonstrated that PS1 is ubiquitinated by Caenorhabditis elegans SEL-10 [52], Fbw7 the mammalian homologue of SEL-10 [38], and more recently by tumour necrosis factor dfmo associated factor 6 (TRAF6), which facilitates Lysine-63 (K63)-linked polyubiquitination of PS1 [50], [51]. The
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In order to facilitate the
2022-04-09
In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to
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Doxorubicin HCl Gal is a amino acid residue peptide comprisi
2022-04-09
Gal is a 29-amino Doxorubicin HCl residue peptide, comprising 30 amino acids in humans, isolated from the porcine intestine 30 years ago (Tatemoto et al., 1983). It has been shown to be involved in the regulation of numerous processes, including neuroendocrine control of systems such as the hypothal
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br Materials and methods br Results
2022-04-09
Materials and methods Results Discussion G-quadruplex structures are extensively studied for its role in central dogma of molecular biology viz. replication problems leading to chromosomal translocations [20], [21], transcriptional inhibition [32] and alternative splicing and translational
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Activation of FXR or TGR inhibits
2022-04-09
Activation of FXR or TGR5 inhibits inflammatory response via repressing NF-κB activity [1]. FXR is not expressed or expressed at a very low level in macrophages [45] (data not shown), but highly expressed in hepatocytes. In contrast, TGR5 is expressed in macrophages but not in hepatocytes. Our data
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Leupeptin br Results and discussion The synthesis of core
2022-04-09
Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou
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It has been reported that aberrant GPR
2022-04-09
It has been reported that aberrant GPR120 expressions were detected in colorectal carcinomas, compared with normal tissues. In addition, GPR120 stimulated cell motile activity and angiogenic property in colon cancer cells [10]. Recently, we indicated that GPR40 suppressed cell motile and invasive ac
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On the contrary the benzhydrol
2022-04-09
On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the bruton's tyrosine kinase tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compar
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br Acknowledgments This research was supported by the Nation
2022-04-09
Acknowledgments This research was supported by the National Institutes of Health Grants GM58442 and GM084152, as well as the National Institutes of Health Predoctoral Training Grant 5T32GM008700-13. We thank Eric Oldfield (University of Illinois, Urbana-Champaign) for providing the FDPS inhibitor
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A large body of literature
2022-04-09
A large body of literature have reported that various cellular pathways are dysregulated in NPC [19]. Among these pathways, Akt is frequently hyperactivated in NPC and regulates diverse cellular processes including tumor cell growth, proliferation, metabolism, survival and invasion, as well as angio
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One limitation of our study
2022-04-09
One limitation of our study was that all control dogs had histologic evidence of mild GI inflammation according to established WSAVA guidelines (Washabau et al., 2010), despite being apparently healthy purpose-bred research dogs housed in a controlled environment with no history of vomiting, diarrhe
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br Materials and methods br Results br
2022-04-09
Materials and methods Results Discussion Numerous studies have identified important roles for HIF-1α in cellular function and dysfunction through its transcriptional activity [4]. A few studies have reported that HIF-1α is translocated to the mitochondria in human and mouse cancer cell line
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