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In summary activated A AR exacerbated
2021-10-13

In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which
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Gastric inhibitory polypeptide a hormone belonging to the
2021-10-13

Gastric inhibitory polypeptide, a hormone belonging to the glucagon-secretin family of peptides, exhibits protection against the neurodegeneration and also stimulates neurogenesis in adult rats in a paracrine manner (Gault and Holscher, 2008, Nyberg et al., 2005, Usdin et al., 1993). The expression
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The development of metabolic stable
2021-10-13

The development of metabolic stable, non-peptidergic galanin agonists could be the basis to clinical diagnosis and treatment of tumors with high levels of galanin receptor expression like gliomas and pituitary tumors. As for gliomas, penetration of the blood brain barrier by the compounds might be p
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The objective of this study is to design and
2021-10-12

The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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EZH can also interact with Ten
2021-10-12

EZH2 can also interact with Ten-Eleven Translocation gene family members (TET1, TET2, and TET3), which convert 5-methylcytosine (5 mC) to 5-hydroxymethylcytosine (5hmC), to cause changes in patterns of histone methylation and DNA methylation [52]. Huang et al. found that the expression levels of all
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In this study it was demonstrated that also in
2021-10-12

In this study it was demonstrated that also in mice chronically exposed to CS, lung inflammation persists after SC and is associated with a progressive alveolar loss and remodeling of respiratory tract, characterized by the onset of bronchial and bronchiolar GCM and peribronchiolar fibrosis. Persist
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The synthesis of substituted pyrimidinone carboxamides
2021-10-12

The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of bromocriptine mesylate australia provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxy
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br Significance Cellular heterogeneity for phenotypic featur
2021-10-12

Significance Cellular heterogeneity for phenotypic features is a key mechanism underlying disease progression and therapeutic resistance, yet its regulation is poorly understood at the molecular level. Our findings demonstrate that endocrine resistance is associated with higher transcriptomic het
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Mice with GSTP knock out show
2021-10-12

Mice with GSTP1 knock out show increased risk of skin cancer when exposed to carcinogens like polycyclic aromatic hydrocarbons [23]. Most of the genetic association studies have focused on GSTP1 c.313G > A variant which results in isoleucine to valine substitution at amino adenosine receptor antagon
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A number of synthetic GPR agonists
2021-10-12

A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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A localization of GK to both a cytoplasmic and perinuclear
2021-10-12

A localization of GK to both a cytoplasmic and perinuclear area of normal rat pancreatic beta-cells was reported in 1996 (Noma et al., 1996), which changed on acute hyperglycemia to a more diffuse staining throughout the cytoplasm. The localization of GK within the nucleus was first reported by Mura
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Herein in consider of the high similarity between GR HBP
2021-10-11

Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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br Electron crystallographic structures of connexins The str
2021-10-11

Electron crystallographic structures of connexins The structures of gap junctions are good targets for electron microscopy because they exhibit the characteristic features of self-assembly. Early studies examined the three-dimensional (3D) structures of native gap junction Uridine from rodents u
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To investigate an involvement of GPR
2021-10-11

To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) Rp-8-Br-PET-cGMPS mg were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-63 cells
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Two typical properties of Gi o
2021-10-11

Two typical properties of Gi/o protein-coupled receptors, namely an increase in 35S-GTPγS binding (Strange, 2010) and an inhibition of exocytotic noradrenaline release (Schlicker and Göthert, 1998), were not shared by H4 receptor activation on cortical membranes (guinea-pig and mouse) and cortical s
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