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The ghrelin receptor is expressed in a number
2021-11-29
The ghrelin receptor is expressed in a number of human malignancies including prostatic carcinoma cell lines [18,19] and tissues [20], breast carcinoma tumours and cell lines [21], testicular tumours [22], and malignant ovarian cysts and tumours [23]. In addition, it has an elevated level of express
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br Results br Discussion In this study we investigated the
2021-11-29
Results Discussion In this study, we investigated the role of galanin and GAL2 receptors on anxiety-like behaviours mediated by the dorsal hippocampus of rats. We showed that locally administered galanin (1 nmol) decreased exploration of the open arms in the EPM, suggesting an anxiogenic-like
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Many neutral and acidophilic galactosidases have been purifi
2021-11-29
Many neutral and acidophilic β-galactosidases have been purified from microorganisms [14], while only a few alkalophilic β-galactosidases have been reported [19]. An alkalophilic β-galactosidase, BGal_375, was obtained and researched for the characterization of its hydrolytic activity. BGal_375 show
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Due to the presence of all FGFRs in the epithelium
2021-11-29
Due to the presence of all FGFRs in the epithelium, there are several FGFs ligands that could be binding to these FGF receptors, namely FGFs 1–4, 8–10, 16 and 18–20. By evaluating the known roles of FGFs in epithelial-mesenchymal interactions and in bone development, this list can be reduced. For ex
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Tetrazole is one of the most commonly
2021-11-29
1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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FBPase deficiency is a very rare
2021-11-29
FBPase deficiency is a very rare inborn error of fructose Repaglinide of autosomal recessive inheritance. This disorder usually occurs in the first year of life through ketotic hypoglycemia and lactic acidosis triggered by catabolic episodes such as prolonged fasting or febrile infections (Steinman
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In the present study VTE recurrence occurred in a
2021-11-29
In the present study, VTE recurrence occurred in a non-cancer patient during edoxaban administration, representing recurrence rates of 1.7% in non-cancer patients and 0.8% in all patients. In a sub-analysis of cancer patients [27] and the main analysis [19] in the HOKUSAI-VTE trial, recurrent VTE oc
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br Challenges and open questions Deepening
2021-11-29
Challenges and open questions Deepening our understanding of PKC’s role in GSIS will require harnessing recently developed techniques and developing new tools. Here we describe three challenges remaining in the field and offer suggestions on experimental approaches to address them. PKC plays an
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br Results br Discussion br STAR
2021-11-29
Results Discussion STAR★Methods Acknowledgments The authors thank Drs. Michael Wegner, Ron Waclaw, and Ed Hurlock for critical comments. We thank Drs. Lihui Tsai and Jiang Wu for CHD8 and ASH2L-expressing vectors, respectively, Dr. Yueh-Chiang Hu for generating transgenic lines, and Jing
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Myriocin The H R couples to G i o proteins and
2021-11-29
The H3R couples to Gαi/o proteins, and hence its stimulation leads to inhibition of adenyalate cyclases, diminishing the level of cyclic AMP (cAMP) with the subsequent reduction in downstream signaling pathways such as protein kinase A (PKA) activation and cAMP-responsive element binding protein (CR
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br Acknowledgments br Introduction Lung cancer is a common b
2021-11-29
Acknowledgments Introduction Lung cancer is a common but extremely perilous cancer, with approximately 733,000 new incidences reported annually in China [1]. Lung cancer ranks highest in the causes of tumor-related mortality, accounting for approximately one quarter of all cancer deaths [2]. N
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Introduction Epigenetic mechanisms modulate heritable phenot
2021-11-29
Introduction Epigenetic mechanisms modulate heritable phenotypic changes that are not dictated by changes in DNA sequences. The link between epigenetic modifications and cancer development has been established [1], [2]. Histone modifications represent an important class of epigenetic mechanisms tha
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PPM-18 Another interesting approach is to use partial
2021-11-29
Another interesting approach is to use partial agonists as starting point to develop specific antagonists like done in earlier decades [64], [65]. Possible indications for an attenuation of the NO/sGC signalling pathway might be specific neuronal disorders: an involvement in the aetiology of migrain
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GKRP binds to the inactive super
2021-11-26
GKRP binds to the inactive, super-open conformation of GCK, acting as a competitive inhibitor of glucose association with the enzyme (Fig. 3) [45]. Upon formation of the inhibitory complex with GKRP, GCK is sequestered into the hepatocyte nucleus [48]. The detailed mechanism by which GKRP mediates t
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However the clinical development of
2021-11-26
However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this recep
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