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Finally worth of mention are few papers that
2021-10-12

Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a STO-609 acetate library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first ser
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br Heme oxygenase inhibitors Historically the first class of
2021-10-12

Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron CEP-32496 of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme for binding to the e
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br GC C and cGMP
2021-10-12

GC-C and cGMP: of mice and men As is usually the case for many genes, most of the studies that relate to GC-C have to date been carried out in mouse models, or in cell lines derived from human colorectal cancer tissue. What appeared to be a lacuna was any report of a human disorder that resulted
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GLP is an intestinal peptide hormone that
2021-10-12

GLP-1 is an intestinal peptide hormone that is released by the gut following ingestion of food, particularly Donitriptan hydrochloride australia and fats. Following its release, GLP-1 stimulates pancreatic β-cells to secrete insulin (Hirasawa et al., 2005, Covington et al., 2006). Originally, GLP-1
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The atherosclerosis development requires additional pro infl
2021-10-12

The atherosclerosis development requires additional pro-inflammatory response in the vascular tissue, promoting increased levels of adhesion molecules such as VCAM-1 (vascular cell adhesion molecule-1) and ICAM-1 (intercellular adhesion molecule-1). Cytokines such as TNF-α and IL-1β are able to upre
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We suggest that the FRET enhancement
2021-10-12

We suggest that the FRET enhancement observed when the modified mD1 protein containing Acd at position 28 was excited at 260nm (), may differ from the diminution in fluorescence observed following excitation at 280nm due to the excitation of different transitions in Trp (i.e., the L and L transition
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Introduction Substantial body of evidence supports the notio
2021-10-12

Introduction Substantial body of evidence supports the notion that GABA, the dominant inhibitory neurotransmitter in the hypothalamus of mammals, affects GnRH release by two classes of membrane receptors: GABAA (GABAAR) [1] and GABAB (GABAB R) [2]. Studies in rodents and sheep have documented that
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vorapaxar EAATs can transport glutamate aspartate cysteic ac
2021-10-12

EAATs can transport glutamate, aspartate, cysteic acid, and serine-o-sulfate (Bjorn-Yoshimoto and Underhill, 2016). All EAATs work as symporters co-transporting 2 or 3 molecules of Na+ and a proton with each molecule of glutamate (or aspartate). In addition, a K+ ion is counter-transported ending in
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br Vesicular glutamate transporters VGLUTs br
2021-10-12

Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,
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In summary this study shows that compound d
2021-10-11

In summary, this study shows that compound 4d has strong clinical potential as an efficient GLP-1/GCGR agonist exhibits weight-lowering, lipid-regulation and diabetes-protective effects and plays an important role in the prevention and therapy of diet induced obesity and dyslipidemia. The present st
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In the light of the above mentioned
2021-10-11

In the light of the above-mentioned considerations, it is interesting to note that the FPR-related research with regards to bias agonism did not prosper during considerably during the last decade (possible exceptions are [[8], [9], [10], [11]]. However, with new insights in receptor chemistry and fu
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br ABT aR aR methyl hexahydropyrrolo
2021-10-11

ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo
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br Tissue Specific Roles for HIF
2021-10-11

Tissue-Specific Roles for HIF/PHD Isoforms Hypoxia signaling pathways are active in almost all mammalian cells, including immune 5 03 synthesis and tissues such as the epithelium and endothelium. This is of crucial importance when considering the influence of environmental hypoxia in inflammatory
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Glucagon (19-29), human mg Over the last few years experimen
2021-10-11

Over the last few years, experimental evidence for the involvement of Epac1 in cancer progression is beginning to emerge (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). For example in melanoma cells, silencing of Epac1 attenuates
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Concerning the molecular mechanisms underlying transcription
2021-10-11

Concerning the molecular mechanisms underlying transcriptional regulation of the GSTP1-1 gene expression we and others have characterized structural and functional properties of the human GSTP1-1 promoter. GSTP1-1 gene promoter activity is driven by a TATA-box [16] as well as Spl [16], [17], AP-1 [1
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