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PKC potentiates insulin release in
2021-12-23

PKC potentiates insulin release in beta cells; however, it is currently not clear how this is mechanistically accomplished in living fccp [15]. First, we discuss PKC structure, regulation, and activation in beta cells. Then, we address two fundamental questions: (1) what is the specific effect of PK
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Taken together the four HRs
2021-12-23

Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc
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Based on pharmacophore modeling a good
2021-12-23

Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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br Material and methods br Results br Discussion
2021-12-23

Material and methods Results Discussion The inhibitory action of a GABA agonist, muscimol, on the level of mRNA encoding GnRH in the POA-hypothalamus [25] of follicular-phase sheep has suggested that at the hypothalamic level GABA may exert a suppressive effect on subsequent steps of the Gn
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Among the compounds prepared at
2021-12-23

Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with moderat
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As GLO is the major detoxification
2021-12-23

As GLO1 is the major detoxification system of reactive dicarbonyls, it is plausible that differences in production and activity of the enzyme influences AGE production and the development and/or modulation of diabetic neuropathy. Glo1 exists as a copy number variant (CNV) in many inbred strains mice
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Limitations of our study are the
2021-12-23

Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we
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Ghsr may have therapeutic value
2021-12-23

Ghsr may have therapeutic value in disorders associated with impairments in AHN. As anxiety disorders and enhanced fear responses observed in PTSD are linked with overgeneralization of similar but distinct memories (i.e poor discrimination), we suggest that acyl-ghrelin’s anti-anxiety effect (Lutter
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Sensitivity to EphB TKI was also demonstrated
2021-12-22

Sensitivity to EphB3 TKI was also demonstrated in a colon cancer cell line, COLO 205, with high expression of EphB3. We found not only exogenous but also endogenous EphB3 protein was expressed in the COLO 205 Phenformin after transient transfection of pCMV6-AC-GFP/EphB3, and both were demonstrated t
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Thirteen multiparous German Holstein cows in their
2021-12-22

Thirteen multiparous German Holstein cows, in their second to fourth lactation, were selected from a previous study (Schäff et al., 2012) based on their individual peak in plasma BHB concentrations in wk 2 or 3 postpartum: high BHB (H-BHB; 1.05 to 2.57 mmol/L, mean 1.59 mmol/L; n = 8) and low BHB (L
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We have presented evidence that
2021-12-22

We have presented evidence that only muscle FBPase is detectable within HL-1 cells. This is consistent with past findings of the Eschrich's group, which showed that in rat heart Pergolide mesylate expression of FBPase is almost exclusively limited to the muscle isozyme [3]. Results of our prelimin
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Several observations about structure activity relationships
2021-12-22

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic JSH-23 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage of
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The site of paracetamol action remains controversial Some
2021-12-22

The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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GSK dimethylpiperidin yl butoxy phenyl piperidine carbonyl n
2021-12-22

GSK-835726 (3-[4-[4-[4-[4-(3,3-dimethylpiperidin-1-yl)butoxy]phenyl]piperidine-1-carbonyl]naphthalen-1-yl]propanoic acid) is a dual H1/H3 receptor antagonist with the potential to be used in allergic rhinitis. Likewise GSK-1004723, the drug-likeness criteria have not been passed by this drug candida
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Studies of early cell fate specification in the mouse
2021-12-22

Studies of early cell fate specification in the mouse embryo have identified a role for differential Motin localization in controlling Hippo signaling [88]. At the 32-cell stage, mouse blastomeres are subdivided into inner cells, which form the inner cell mass (ICM), and outer cells, which form the
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