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Compared with the tetrazole derivative the potency of analog
2021-12-08

Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su
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dizocilpine In human platelets only and isoforms
2021-12-08

In human platelets, only α1 and β1 isoforms of sGC are expressed in equimolar concentrations (3700 copies for β1, and 3500 copies for α1 per platelet) [57] [62]. sGC, is usually a heterodimer and contains heme as cofactor which is required for high-affinity NO binding and stimulation of its activity
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br Acknowledgments This research was supported
2021-12-08

Acknowledgments This research was supported by the Czech Ministry of Education, Youth and Sports by grants MSM LH11013 and Czech Grant Agency (501/12/0590). David Kopečný and Martina Kopečná were supported by the grant LO1204 from the National Program of Sustainability I by the Ministry of Educat
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GLP is an intestinal peptide hormone that
2021-12-08

GLP-1 is an intestinal peptide hormone that is released by the gut following ingestion of food, particularly CGP 3466B maleate synthesis 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 acted in
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As part of their ongoing effort in the field
2021-12-08

As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile Kartogenin derivatives as TG
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br Results and discussion br Conclusion
2021-12-08

Results and discussion Conclusion In this study the first binding assays based on a nonlabelled reporter ligand addressing GlyT1 are described. Following the concept of MS Binding Assays recently introduced in our group, binding of the well-known GlyT1 inhibitor Org24598 employed as reporter l
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Abnormal expression and higher activity of GLO I have been
2021-12-08

Abnormal expression and higher activity of GLO I have been detected more in various tumor pexidartinib sale than in normal cell samples., , , , , , , Among cancer cell lines, lung carcinoma cells frequently showed higher GLO1 activity. Human NSCLC cell line NCI-H522 cells possess high activity and
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br Membrane transporters as a novel therapeutic
2021-12-08

Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS
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Conessine synthesis br Some Gardos channel perplexities
2021-12-08

Some Gardos channel perplexities While much is known about the Gardos channel (inside Ca2+-activated K+ channel) and it's characteristics in human red blood Conessine synthesis (e.g. [18,19]), there are a number of intriguing and unexplained phenomena that are in much need of study. One is that
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How changes in APP processing
2021-12-08

How changes in APP processing by γ-secretase lead to AD is still not well understood. Deposition of amyloid beta (Aβ) peptide fragments of the amyloid precursor protein (APP) in amyloid plaques and hyperphosphorylated tau in neurofibrillary tangles are the cellular hallmarks of AD (O’Brien and Wong,
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UCB 35625 The role of cell to cell
2021-12-08

The role of cell-to-cell interactions in coordinating the cells’ behaviour to ensure an appropriate anterior pituitary hormone response is receiving increasing attention. Anterior pituitary UCB 35625 interact with neighbouring cells through junctional complexes. As their name implies, the complexed
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Furthermore our results are the first to demonstrate that
2021-12-08

Furthermore, our results are the first to demonstrate that the stimulating effect of GALP on AVP release in rats is independent of galanin receptors. The same stimulatory GALP influence on AVP secretion has been also observed in the presence of galantide, an antagonist of Gal receptors in the incuba
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br Acknowledgments This study was
2021-12-08

Acknowledgments This study was supported by a Conquer Cancer Foundation (American Society for Clinical Oncology) Drug Development Research Professorship Grant (AAA). Introduction Gastric cancer (GC) is one of difficult cancers to treat in terms of its poor prognosis and limited applicability
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LPCs have been previously described
2021-12-08

LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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Therefore the histomorphology and the comprehensive analysis
2021-12-08

Therefore, the histomorphology and the comprehensive analysis of TMJ-RA pathogenesis need to be completed although clinical findings in TMJ-RA are similar to RA in other joints [41]. Especially for the dentist, the difficulties associated with diagnosing TMJ-RA patients [49] posing challenges to dia
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