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br Next we explored the SAR
2022-08-04

Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic actin inhibitor sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo
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In the present study recipient oestradiol serum levels
2022-08-04

In the present study, recipient oestradiol serum levels on the day of donor oocyte retrieval or warming were found to be significantly higher in the antagonist group and higher than 100 pg/ml in all cases. Serum oestradiol level has been reported to have no effect on endometrial receptiveness in ooc
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Herein we report the discovery of AM AM maintains
2022-08-03

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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droperidol Natural products have been always
2022-08-03

Natural products have been always the most important and productive sources of lead compounds for the development of drugs [[15], [16], [17]]. A variety of potent α-glucosidase inhibitors have been identified from natural products, such as quercetin, resveratrol, isorhamnetin, calein C and curcumin
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In order to consolidate our genetic
2022-08-03

In order to consolidate our genetic funding, we performed several in silico analysis regarding the p.R85W mutation. The high conservation of R85 residue in all species suggests that it has an important role in glucokinase function. Pathogenic effect of the p.R85W is supported by in silico prediction
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Glucagon regulates the transition from
2022-08-03

Glucagon regulates the transition from hepatic glucose utilisation in the absorptive state to glucagon production in the post-absorptive state by acute stimulation of glycogenolysis and inhibition of glycolysis [1]. An important component of this response is the phosphorylation of liver PFK2/FBPase2
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br Methods br Results br Discussion In this
2022-08-03

Methods Results Discussion In this series of studies we hypothesized that FHH-GHSRm1/Mcwi rats would, relative to their WT counterparts, exhibit a metabolic and behavioral phenotype reminiscent of GHSR−/− mice. Through the use of the GHSR−/− mouse, a great deal about the role of ghrelin sig
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The most ubiquitous serine threonine phosphatases such as PP
2022-08-03

The most ubiquitous serine/threonine phosphatases, such as PP1, PP2A, and PP2B are known to contribute to the majority of phosphatase activity in the heart [4]. Dysregulation of these and other PPs have been found in numerous CVDs, including heart failure (HF), and may play a critical role in reduce
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br FPRs regulate anti microbial
2022-08-03

FPRs regulate anti-microbial responses The classic evidence supporting FPR as an anti-microbial receptor is that bacteria are the major biological source of chemotactic formyl peptides, fMLF binds to FPR and fMLF activates chemotactic and anti-microbial responses in neutrophils 2., 3.. Recently,
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uPAR promotes cell associated proteolysis by binding to uPA
2022-08-03

uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot
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br Materials and methods br Results br Discussion The distri
2022-08-03

Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta A-740003 synthesis [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract, a
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br Introduction GPR also known as free fatty
2022-08-03

Introduction GPR40 (also known as free fatty Phos-tag Biotin receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium- and long-
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br Introduction GPR also known as free fatty
2022-08-03

Introduction GPR40 (also known as free fatty Clozapine receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium- and long-chain s
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br Acknowledgements The authors have no ethical conflicts to
2022-08-03

Acknowledgements The authors have no ethical conflicts to disclose. The authors have no conflicts of interest to declare. This work was funded by the Research Council of Lithuania. Introduction This paper studies whether there is a causal influence of the risk-taking incentives provided by op
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In spite of decades of research the mechanisms of
2022-08-03

In spite of decades of research the mechanisms of SV endocytosis and recycling remain controversial. Accumulating evidence suggests that SV endocytosis occurs by more than one mechanism (e.g. clathrin-independent endocytosis, clathrin-mediated endocytosis, bulk endocytosis; reviewed in (Dittman and
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