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br Introduction Maintaining blood glucose within an appropri
2021-12-29
Introduction Maintaining blood glucose within an appropriate range is crucial for survival. In diabetes, those who suffer episodes of severe hypoglycemia have an increased risk of death [1], [2]. The AI-10-49 receptor is especially dependent on an adequate, continuous supply of circulating gluco
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MRcKO mice showed a comparable degree of cardiac
2021-12-29
MRcKO mice showed a comparable degree of cardiac remodeling compared to control (MRf/f) mice. Moreover, the worse cardiac remodeling in pressure-overloaded GRcKO mice is not due to compensatory activation of cardiomyocyte MR, because GRMRdcKO mice displayed cardiac remodeling to the same extent as G
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543 On the other hand histone deacetylase
2021-12-28
On the other hand, histone deacetylase inhibitors can accelerate inflammation resolution by promoting the externalization of AnxA1, a main ALX/FPR2 agonist, with concomitant inhibition of cytokine gene expression in mouse macrophages [30]. Thus, our present results provide an additional mechanism, i
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Indeed another recent study found that the HR
2021-12-28
Indeed, another recent study found that the HR-like cell death triggered in rice epidermal cells by an avirulent or incompatible isolate of the fungal pathogen , which causes blast disease, is a ferroptotic cell death phenomenon (). Similar to the heat shock example given above, elevated levels of
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br Conflict of interest br
2021-12-28
Conflict of interest Introduction Colorectal cancer (CRC), characterized by high prevalence in elderly people, is one of the most common cancers of digestive tract. CRC severely affects human health and causes enormous social and economic burdens [[1], [2], [3]]. Although public health awaren
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br Introduction Ovarian cancer patients have the highest mor
2021-12-28
Introduction Ovarian cancer patients have the highest mortality rate amongst patients with gynecologic cancers. The 10-year survival rate of ovarian cancer patients is beta lactamase inhibitor with BRCA1/2 mutation [2]. Several studies have indicated the role of dysregulation of histone methylat
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Introduction Hepatitis C virus HCV is a small nm
2021-12-28
Introduction Hepatitis C virus (HCV) is a small (50–80 nm in size) enveloped RNA virus belonging to the Hepacivirus genus of the Flaviviridae family [1]. The HCV particle consists of a nucleocapsid, which contains the positive single-stranded RNA genome covered by a host cell-derived lipid envelope
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In contrast to RhoA Rac and Rap which are
2021-12-28
In contrast to RhoA, Rac1 and Rap1 which are stimulated by platelet activators and inhibited by NO/PKG, the GTPase ADP-ribosylation factor 6 (Arf6) is regulated in the reverse way. Platelet agonists like thrombin, collagen, or ADP, reduce Arf6-GTP levels, whereas NO and PGI2 oppose this reduction [1
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Main Text There are over small GTPases that play critical
2021-12-28
Main Text There are over 200 small GTPases that play critical roles in diverse fundamental cellular processes such as signal transduction, Marimastat dynamics, and intracellular trafficking. Most of the GTPases act as switch-like molecules by cycling between the guanosine triphosphate (GTP)-bound
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GPR shares a amino acid sequence identity in
2021-12-28
GPR81 shares a 52% amino Amodiaquine dihydrochloride dihydrate australia sequence identity in humans to GPR109A [1], [2], [3]. In addition, GPR81 is localized more specifically to the adipose tissue [3]. In 2008, lactate was discovered to be the endogenous ligand for GPR81 [9], [10]. Plasma lactate
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br Potential endogenous agonists of
2021-12-28
Potential endogenous agonists of GPR35 The first endogenously produced chemical that was shown to be able to activate GPR35 was the tryptophan metabolite kynurenic Papain synthesis [8]. When human GPR35 was expressed along with a mixture of promiscuous and chimeric G proteins 9, 10 (Box 1) in CHO
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SAR around amino derivative revealed
2021-12-28
SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-po
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br FXR Agonists Azepinol b
2021-12-28
FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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On the other hand it is quite
2021-12-28
On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th
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Our overall goal is to develop selective compounds for low
2021-12-28
Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and
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