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Our study has strengths and limitations We
2021-10-22

Our study has strengths and limitations. We believe we are the 1st to report a novel model of secondary hypogonadism. Several animal models for hypogonadotropic hypogonadism (kisspeptin and the kisspeptin receptor knockout) exist but we are unaware of animal models of secondary hypogonadism with di
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In the present study we conducted a search
2021-10-22

In the present study, we conducted a search for other possible endogenous ligands for GPR35. We focused on lysophospholipids because of the homology (30%) between GPR35 and GPR55 whose endogenous ligand is lysophosphatidylinositol (LPI) [9], especially 2-arachidonoyl LPI [10]. Notably, the GPR35 gen
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br Conclusions br Introduction G protein coupled receptors
2021-10-22

Conclusions Introduction G protein-coupled receptors (GPRs) share common structural motifs, including seven transmembrane helices, and the ability to activate heterotrimeric G proteins such as Gs, Gi, Gq and G12/13. A variety of GPR cellular functions are mediated by second messengers such as
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Next we designed substituents of the position Edge to
2021-10-22

Next, we designed substituents of the 6-position. Edge-to-face aromatic interaction between aromatic ring of ligand and Phe162B needed to be retained because the interaction seems to be important for tight binding. 3′-Position of the 6-phenyl group of directs to a hydrophilic space where W1 exists.
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Recognition and Repair of DNA Damage
2021-10-22

Recognition and Repair of DNA Damage DNA is a reactive molecule that is continually challenged by both endogenous and exogenous insults 1., 2.. Cellular metabolites and their byproducts, environmental toxins, and radiation alter the chemical structure of DNA, producing a wide spectrum of DNA damage
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Through the analysis of various synthetic GPR agonists
2021-10-22

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic glycosylase motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering
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Regulation of pancreatic and cell mass has been extensively
2021-10-22

Regulation of pancreatic α and β cell mass has been extensively studied and hotly debated, due to potential therapeutic implications. Early claims of Angptl8 as “betatrophin” and Angptl4 as a regulator of glucagon secretion and α cell proliferation (Yi et al., 2013, Ben-Zvi et al., 2015) have not st
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Despite the potential promise of both of these peptides
2021-10-22

Despite the potential promise of both of these peptides, such compounds are still susceptible to efficient renal filtration (Emmanouel et al., 1978, Holst, 1991, Deacon et al., 1996). However, numerous studies have demonstrated that fatty monobenzone dervatisation of related regulatory peptides res
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After the successful development of molecular targeted
2021-10-21

After the successful development of molecular targeted drugs in lung adenocarcinoma, substantial efforts have been made to provide similar targeted drugs in lung squamous-cell carcinoma. Because FGFR gene alteration is the most frequent occurrence in squamous-cell carcinoma, targeted therapies for F
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Among the isoforms of heme oxygenases HO
2021-10-21

Among the 3 isoforms of heme oxygenases (HO-1, HO-2, and HO-3), HO-1 expression is inducible, and it catalyzes the degradation of heme to biliverdin, carbon monoxide (CO) and free Fe. The Fe is then stored in ferritin, limiting its ability to participate as a catalyst through the Fenton reaction and
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br Results br Discussion Our
2021-10-21

Results Discussion Our cardiomyocyte-specific GR knockout mice did not show spontaneous cardiac hypertrophy unless pressure overload was given to the heart. This finding is somewhat different from previous work of a cardiomyocyte-specific GR Manumycin A australia mouse model using GR-floxed m
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br Results br Discussion Immune mediated chronic inflammator
2021-10-21

Results Discussion Immune-mediated chronic inflammatory diseases (e.g. rheumatoid arthritis, psoriasis, multiple sclerosis, and inflammatory bowel disease) are characterized by a dysregulated migration of leukocytes from blood vessels into inflamed tissues. To date, several new targets and inh
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To identify structurally novel autophagy inhibitors a medium
2021-10-21

To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 ZCL278 stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by automated flu
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Aspartame l aspartyl l phenylalanine
2021-10-21

Aspartame (l-aspartyl l-phenylalanine methylester) is a dipeptide artificial sweetener that is widely used as a non-nutritive sweetener in various food products [1]. The increased market of dietary products and the development of new synthetic sweetening compounds have not been sufficiently explored
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Considering the fact that OCL induced depletion
2021-10-20

Considering the fact that OCL induced depletion of T CP-673451 sale in non-stimulated cultures, the only possible explanation of this effect is the elevated mortality of these cells. It was found that OCL at the higher concentration induced the apoptosis of CD4+ and CD8+ T cells. These results stro
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