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br Discussion This study dedicated to histamine H and
2022-03-14
Discussion This study, dedicated to JNJ-38877605 H3 and H4 receptors, was carried out on superfused tissues preincubated with 3H-choline or 3H-noradrenaline; electrical stimulation was used to elicit quasi-physiological exocytotic release of the respective transmitter. Since inhibition of transm
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The H R couples to
2022-03-14
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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RS testing has been extensively
2022-03-14
RS testing has been extensively validated in patients with early stage, ER+, HER2− patients. TAILORx, a randomized controlled trial to evaluate the role of adjuvant chemotherapy by RS, found no recurrence or survival benefit to the addition of chemotherapy to endocrine therapy in patients with inter
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Stability of DBS over the day
2022-03-14
Stability of DBS over the 60-day time points was encouraging, with a maximum of 0.1 log10 IU/mL degradation from the day 1 value (Supplementary Fig. 1 and Supplementary Table 3). Discussion This study evaluated the sensitivity and specificity of the Aptima HCV Dx assay for HCV RNA detection from
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GSTP is a class Glutathione S transferase GST enzyme
2022-03-12
GSTP1 is a π-class Glutathione S-transferase (GST-π) enzyme involved in tumor suppression by protecting Taxifolin against genomic damage mediated by various oxidants. Although the loss of GSTP1 function by hypermethylation has been reported as a common epigenetic alteration in prostate carcinogenes
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br GPR is a class A GPCR expressed on
2022-03-12
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine Estradiol Benzoate which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated
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br Animal models of NASH The human NAS system
2022-03-12
Animal models of NASH The human NAS system (see above) is largely reproducible in NAFLD mouse models [37] and, therefore, has been increasingly applied in the preclinical assessment of liver histological responses to test compounds. In general, the NAS system is well suited for this purpose, alth
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Restless running behavior was first described in mice after
2022-03-12
‘Restless running behavior’ was first described in mice after administration of 30mg/kg i.p. ALX-5407 and was thought to be due to an augmentation of NMDA-induced dopamine activity [27]. The motor impairments caused by ALX-5407 were confirmed by Perry et al. [10] and extended to another sarcosine-de
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Milnacipran HCl Finally we investigated if calpain
2022-03-12
Finally, we investigated if calpain truncation affects GlyT1 turnover and trafficking. To simulate calpain cleavage at the T602/T603 and G626/S627 sites we constructed GlyT1 transporters missing the last 12 and 36 amino acids. Since the 36 amino Milnacipran HCl truncation also removes all C-termina
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br Transporter based brain targeting nano DDS
2022-03-12
Transporter-based brain-targeting nano-DDS Drug delivery to the central nervous system (CNS) is still challenging due to the bloodbrain barrier (BBB)53., 54.. The BBB is a natural defense barrier protecting the Nivolumab mg from harmful substances. Since only selected, neutral, lipophilic small
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br Acknowledgments The financial support from the National N
2022-03-12
Acknowledgments The financial support from the National Natural Science Foundation of China (Nos. 31460422 and 31060210), the Natural Science Foundation of Jiangxi Province, China (20171BAB204029 and 20143ACB20006), the Project of Science and Technology of Jiangxi Provincial Education Department,
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In the present study we set out
2022-03-12
In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmaco
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Regulation of pancreatic and cell mass
2022-03-12
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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In the gastrointestinal GI tract CART
2022-03-12
In the gastrointestinal (GI) tract CART expression has been described in the enteric nervous system in rats (Ekblad et al., 2003), pigs (Wierup et al., 2007), sheep (Arciszewski et al., 2009), guinea pigs (Ellis and Mawe, 2003) and humans (Kasacka et al., 2012). Less is known about CART expression i
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br Acknowledgements We thank the following individuals
2022-03-12
Acknowledgements We thank the following individuals for notable contributions to this work: Dr. Ruth Wood, Dr. Alan Watts, Dr. Casey Donovan, Andrea Suarez, Emily Nakamoto, Allison Apfel, April Banayan, and Jonathan Cheung. This study was supported by the National Institute of Health grants, DK10
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