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br Material and methods br Results and discussion Unlike
2021-12-27

Material and methods Results and discussion Unlike many fruits such as bananas and tomatoes, known as climacteric fruits, in which ripening is regulated by a burst of Brassinolide biosynthesis and an increase in respiration, pepper fruits, which do not follow this pattern, are called non-clima
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br Acknowledgements br Introduction Type diabetes is a
2021-12-27

Acknowledgements Introduction Type 2 diabetes is a progressive metabolic disorder which is characterised by chronic hyperglycaemia due to relative insulin deficiency, insulin resistance and increased hepatic glucose production [1]. The metabolism of glucose by glycolysis increases the ATP:ADP
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br Materials and methods br
2021-12-27

Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 GW-1100 has been identified within discrete regions of the nervous sy
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GPR A a G protein coupled receptor
2021-12-27

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic vasopressin receptor antagonists [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR10
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Even though for almost years GnRH was considered the main
2021-12-27

Even though for almost 30 years GnRH was considered the main neuropeptide regulating gonadotropin release in vertebrates, Tsutsui et al. (2000) discovered, in the Japanese quail, Coturnix japonica, a hypothalamic neuropeptide that directly inhibits gonadotropin release, and thus named as gonadotropi
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Oxidative stress results from the disequilibrium
2021-12-27

Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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Herein in consider of the high similarity between
2021-12-27

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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With rare exceptions the biological role of secretase
2021-12-24

With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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A common feature of ferroptosis is the
2021-12-24

A common feature of ferroptosis is the iron-dependent accumulation of lipid-ROS and the subsequent depletion of polyunsaturated fatty Cephalexin phospholipids (PUFA-PLs) [118]. The PUFA chains of membrane lipids are more susceptible to both enzymatic and non-enzymatic oxidation, which results in PUF
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In the previous paper we described the design and synthesis
2021-12-24

In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In
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The present study was designed to clarify the
2021-12-24

The present study was designed to clarify the distribution and the function of the endothelin receptors in the guinea-pig urinary bladder. We found that endothelin-1 produced a clear tonic contraction via both dpni subtypes, the endothelin ETA and ETB receptor, and that sarafotoxin S6c also induced
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The development of immobilization techniques
2021-12-24

The development of immobilization techniques for β-glucosidase offers a potential way to enable its reuse several times [13]. The aim of immobilization is to trap the enzyme within or on the surface of an insoluble material with retention of its catalytic activity [14]. The immobilization strategy a
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MRcKO mice showed a comparable degree of cardiac
2021-12-24

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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br Conclusions br Conflicts of Interest br Acknowledgments T
2021-12-24

Conclusions Conflicts of Interest Acknowledgments The Section of Endocrinology and Investigative Medicine is funded by grants from the Medical Research Council (MRC), Biotechnology & Biological Sciences Research Council (BBSRC), National Institute for Health Research (NIHR), an Integrative
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Genetic disruption or pharmacologic inhibition of the hepati
2021-12-24

Genetic disruption or pharmacologic inhibition of the hepatic glucagon pathway has invariably been shown to increase pancreatic α cell mass. This has been observed in glucagon receptor (GCGR) knockout (Gcgr−/−) mice (Gelling et al., 2003), glucagon knockout mice (Hayashi et al., 2009), prohormone co
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