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In T cells whereas SETDB
2021-10-25

In T cells, whereas SETDB1 is implicated in OX40-dependent repression of the Il17a locus in Th17 cells (Xiao et al., 2016), SUV39H1 controls Th2 cell stability by depositing H3K9me3 at the Ifng promoter (Allan et al., 2012). However, the deregulation of the Ifng locus observed in Suv39h1−/− cells ca
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In this study we demonstrate that HHcy upregulated the
2021-10-25

In this study, we demonstrate that HHcy upregulated the expression of GSNOR in T cells. As a result, GSNOR induced denitrosylation of Akt in Hcy-activated T protein phosphatase in vivo and in vitro, which contributed to vascular inflammation and susceptibility to atherosclerosis in GSNOR-/-ApoE-/-
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Gefitinib hydrochloride synthesis In addition to the role of
2021-10-25

In addition to the role of TGR5, the FXR-FGF15/19 axis has been implicated in other aspects of glucose metabolism and metabolic disorders. In humans, both obesity and type 2 diabetes mellitus (T2DM) are associated with lower plasma FGF19 levels [67,68]. A derivative of the naturally occurring FXR ag
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So far GnRH receptors have been detected in the human
2021-10-25

So far, GnRH receptors have been detected in the human ovary, but their physiological importance is still unclear (). In particular, GnRH receptors as well as GnRH types I and II have been localized in the granulosa KN-92 of pre-ovulatory follicles, but not of follicles from the primordial to the e
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br The glycine transporter GlyT was
2021-10-25

The glycine transporter 1 (GlyT1) was originally identified as a member of the solute carrier family 6 of sodium- and chloride-dependent neurotransmitter transporters . GlyT1 is expressed in the central nervous system and in peripheral tissues; mainly in erythroid cells, from erythroblasts in the
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Ghrelin is mostly known for
2021-10-25

Ghrelin is mostly known for its orexigenic properties, whereas the role of DAG on feeding is controversial with studies claiming an orexigenic, anorexigenic or no effect (Inhoff et al, 2009, Toshinai et al, 2006). One of these studies was that of Toshinai and colleagues, who found a link between the
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NSC228155 receptor Introduction Parkinson s Disease PD is a
2021-10-25

Introduction Parkinson's Disease (PD) is a neurodegenerative disease affecting approximately 5–6 million individuals worldwide [1]. This number is expected to escalate to ∼10 million by the year 2030 as the world's population rapidly ages [2]. In the United States, more than 1 million individuals h
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Primarily because secretase was a therapeutic target
2021-10-25

Primarily because γ-secretase was a therapeutic target in AD, a plethora of γ-secretase inhibitors (GSIs) have been developed that effectively inhibit γ-secretase cleavage in humans [16]. Indeed, “druggability” of γ-secretase has not been an issue even when the identity of the target was unknown in
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Considering the fact that NADPH oxidase is
2021-10-23

Considering the fact that NADPH oxidase is the main source for paraquat and maneb-induced oxidative stress, we hypothesized that NADPH oxidase activation might contribute to dopaminergic neurodegeneration induced by paraquat and maneb through ferroptosis. To test our hypothesis, we investigated the
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FXa is a vitamin K
2021-10-23

FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 Dapoxetine HCl and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The
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DZNep is a PRC inhibitor that inhibits S
2021-10-23

DZNep is a PRC2 inhibitor that inhibits S-adenosylhomocysteine hydrolase, resulting in cellular accumulation of S-adenosylhomocysteine. S-adenosylhomocysteine is a competitive inhibitor of methyl donor for methyltransferases [38]. DZNep targets EZH2 by reduction in the level of the enzyme H3K27me3 a
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PBI is an agonist of GPR and
2021-10-23

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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br GPR is a class A GPCR expressed
2021-10-23

GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine 5-fu which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell signali
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GPR agonistic activity was evaluated for the human
2021-10-23

GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin
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Up to now many UDG assays have
2021-10-23

Up to now, many UDG assays have been reported based on the design of dU-containing substrate DNA, which can be roughly divided into two categories according to the sensing mechanisms. One type of UDG assays are simply based on the physical or chemical property changes of the substrate accompanied wi
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