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Levofloxacin receptor The membrane metalloendopeptidase MME
2021-12-13

The membrane metalloendopeptidase (MME) gene is located at human chromosome 3q21-27. It encodes a 100-kD type II transmembrane glycoprotein, a widely expressed membrane metalloendopeptidase that degrades a number of substrates. The active site of the enzyme faces the extracellular space. MME is wide
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In C elegans KDM A appears to be involved in
2021-12-13

In C. elegans, KDM4A appears to be involved in H3K36me3 reduction on the X chromosome, suggesting that this protein has a relevant role in germ cell development (Figure 2A) (47). In addition, in HeLa cells, KDM4A is associated with the repression of the achaete-scute complex homologue 2 (ASCL2) gene
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Reduction of the hydrolysis of ATP
2021-12-13

Reduction of the hydrolysis of ATP is an important strategy to reduce ischemia/reperfusion injury. Increased intracellular concentrations of solutes secondary to ATP depletion are known to result in osmotic swelling that may be sufficient to cause sarcolemmal rupture. Cinaciguat activates sGC direct
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Screening of the compounds allowed
2021-12-13

Screening of the compounds allowed for a number of interesting SAR observations. First of all, pyridyl analogue demonstrated that a pyridine ring would be beneficial for both log as well as increasing the potency (entry 2 versus entry 1). Electron-poor aryl groups next to the oxadiazolone were detr
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The occurrence of MDR in cancer
2021-12-13

The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer Epiberberine in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the
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br Results and discussion br Conclusions TZDs represent
2021-12-13

Results and discussion Conclusions TZDs represent a well-studied group of antidiabetic agents. Based on previous observations of the ability of some TZDs to activate FFAR1, we designed five scaffolds consisting of the TZD head, a linker, and a carefully selected privileged structure. For the p
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br Introduction Most organisms require glucose as a key
2021-12-13

Introduction Most organisms require glucose as a key metabolite, and it is critical that mammalian cells regulate glucose levels properly to maintain bioenergetic homeostasis. The major transporters responsible for the uptake of glucose from systemic circulation into cells are the GLUTs, members
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Fig A demonstrates the body weight gain of the
2021-12-13

Fig. 2A demonstrates the body weight gain of the pregestational females. High-fat diet in wild-type mice increased body weight in 2 weeks and sustained this increase over 8 weeks. A similar effect was noted in glut3 mice in response to a high-fat diet. Fig. 2B depicts fat and muscle mass as assessed
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Rare mutations can impair the molecular function
2021-12-13

Rare mutations can impair the molecular function of GR and alter tissue sensitivity to GCs in humans, resulting in primary generalized GC resistance (PGGR) and hypersensitivity (PGGH) [14]. Familial and sporadic PGGR, or Chrousos Syndrome, is characterized by general and partial insensitivity of tis
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According to the implication of the
2021-12-13

According to the implication of the endocannabinoid system in IBD, we decided in our laboratory to develop selective CB agonists and FAAH inhibitors to treat these diseases. Recently, we described 3-carboxamido-5-aryl-isoxazoles as selective CB agonists. This series of isoxazoles possesses a 2-subst
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Our observation of LPS induced increase in
2021-12-13

Our observation of LPS-induced increase in the sensitivity of cultured endothelium-intact coronary MG 262 towards stimulation with selective ETB receptor agonist (S6c) could be explained by activation of TLRs receptors located on the endothelium of rat coronary arteries. However, the possible recru
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Two typical properties of Gi o
2021-12-13

Two typical properties of Gi/o protein-coupled receptors, namely an increase in 35S-GTPγS binding (Strange, 2010) and an inhibition of exocytotic noradrenaline release (Schlicker and Göthert, 1998), were not shared by H4 receptor activation on cortical membranes (guinea-pig and mouse) and cortical s
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br Author contributions br Declaration
2021-12-10

Author contributions Declaration of conflict of interest Acknowledgements We are grateful to the Director, National Institute of Immunology for his support. The work was partially supported by J.C. Bose Fellowship to SSM. We acknowledge the help from staff of Small Animal Facility of Nation
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br Experimental br Results and discussion br Conclusion In t
2021-12-10

Experimental Results and discussion Conclusion In the current work, a novel method for separation and preparation of flavonoid glycosides from L. chinensis was successfully developed using a 2 D-HILIC × RPLC system based on a zwitterionic Click XIon column and a polar-modified Atlantis T3 c
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Here we demonstrate an anti inflammatory and anticancer
2021-12-10

Here we demonstrate an anti-inflammatory and anticancer function for Gpr109a in colon. Gpr109a signaling imposed anti-inflammatory properties in colonic antigen-presenting cells, which in turn induced differentiation of Treg GDC-0994 synthesis and IL-10-producing T cells. Gpr109a was also required f
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