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To investigate the potential molecular mechanism of
2021-10-27

To investigate the potential molecular mechanism of FXR-mediated regulation of liver cancer cell proliferation, gene expression profiles were determined using Agilent arrays in SK-Hep-1-FXR and NC after treatment with the FXR agonist GW4064. The results indicate that mTOR and S6k are involved in di
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The binding of DHAP to aldolase resulted
2021-10-27

The binding of DHAP to aldolase resulted in a dramatic decrease of aldolase affinity to FBPase – KAapp was reduced more than 100 times. The dependence of the complex activity versus increasing DHAP concentration was biphasic (Fig. 3a). Supposedly, the first phase of the curve represents the state in
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In this review we focus on the
2021-10-27

In this review, we focus on the structure and function of the KDM4A protein, its role in cancer development, and the importance of this enzyme as a therapeutic target. For further review of the KDM4 family, see Shi et al., Whetstine et al., and Berry et al. , , . KDM4A protein structure and enzymol
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To efficiently develop bioactive ligands even if the structu
2021-10-27

To efficiently develop bioactive ligands even if the structural information of the target protein is unknown, we have presented a three-dimensional structural diversity-oriented strategy based on structural properties of a chiral cyclopropane. Our strategy has allowed us to design and synthesize a s
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In prostate cancer PCa glucose
2021-10-26

In prostate cancer (PCa), glucose metabolism plays a major role in progression [14]. Androgens can activate the metabolic regulator AMP-activated kinase (AMPK), promoting oxidative phosphorylation (OXPHOS) [15]. Besides, androgens increase GLUT1 [16], which overproduction has been described in the m
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br Materials and methods br Conflicts of
2021-10-26

Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He
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br Introduction The term autophagy
2021-10-25

Introduction The term “autophagy” was coined by Christian de Duve in 1963 to describe the process of removing and degrading intracellular components such as unused proteins and damaged organelles through lysosomes [1,2]. Autophagy has been divided into three main types, namely, macroautophagy, mi
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Fatty acid amide hydrolase FAAH is a membrane
2021-10-25

Fatty ripasudil amide hydrolase (FAAH) is a membrane-bound enzyme which releases arachidonic acid and ethanolamine by breaking amide bond of AEA. It also controls the cellular uptake of AEA, by creating and maintaining an inward concentration gradient leading to AEA-facilitated diffusion via a speci
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At the molecular level AZ
2021-10-25

At the molecular level AZ scaffold proteins including piccolo and bassoon have been shown to directly or indirectly associate with endocytic and actin-binding proteins such as ABP1 (Fenster et al., 2003), profilin, and GIT (Podufall et al., 2014) (Fig. 2B). ABP1 and profilin, via regulating F-actin,
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br Experimental procedures br Conflicts of interests br
2021-10-25

Experimental procedures Conflicts of interests Introduction Here we investigate differences in growth properties and short-term morphological changes in response to ET-1 in Chinese hamster ovary (CHO) cells stably and separately expressing ETA or ETB receptors. A stably transfected CHO syst
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The H R antagonist JNJ developed by
2021-10-25

The H3R antagonist JNJ-17216498, developed by Johnson & Johnson, has entered clinical trial studies, but no information regarding its structure has been publicized to date. A phase II study of JNJ-17216498 monotherapy has been completed for patients with narcolepsy, but the results are not publicall
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A recent novel and important finding is that
2021-10-25

A recent novel and important finding is that YAP connects cellular growth with anabolism; YAP suppresses the transcriptional induction of genes which importantly regulate gluconeogenesis in the liver; namely glucose-6-phosphatase catalytic subunit (G6PC) and phosphoenolpyruvate carboxykinase 1 (PCK1
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The PAS and CC domains of sGC have been studied
2021-10-25

The PAS and CC domains of sGC have been studied less by comparison, though their function in sGC signal transduction is likely important. PAS domains are versatile as they can play varied roles in different proteins, such as quaternary structure organization, cofactor binding, and signal transductio
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Originally identified as a GPCR upregulated on Burkitt
2021-10-25

Originally identified as a GPCR upregulated on Burkitt lymphoma cells upon Epstein-Barr virus infection (Birkenbach et al., 1993), Ebi2 was later found to play critical roles in immunity by regulating the migration of activated GW1929 to extrafollicular sites for early plasmablast responses (Gatto e
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Wasting syndrome is a common complication of
2021-10-25

Wasting syndrome is a common complication of HIV infection and is marked by progressive weight loss and weakness, often associated with fever (Weinroth et al., 1995). Fever is a highly complex process initiated by the action on the INCB3344 thermosensitive cells of a number of endogenous pyrogens,
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