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dnmt br Histamine H R The cloning of the H R
2022-02-28

Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other dnmt receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et al., 2009, Liu et a
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The H autoreceptors distributed mainly in the CNS
2022-02-28

The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co
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Over recent decades there were three
2022-02-28

Over recent decades, there were three breakthroughs of high intensity heavy-ion acceleration [6]. The first is the invention of radio frequency quadrupole (RFQ) type accelerator, which could accelerate more than dozens of milli-ampere ion beams and is a good solution to space-charge-effect of heavy-
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br Materials and Methods A human
2022-02-28

Materials and Methods A431 (human skin SCC) and HT-297.T (human AK) cell lines were purchased from ATCC (Manassas, VA) and were maintained in DMEM supplemented with 10% fetal calf serum, 4 mM L-Gln, 1 mM sodium pyruvate, 100 U/mL penicillin, and 1 μg/mL streptomycin. Human HK1 and HK2 plasmids we
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br Chemistry The methylsulfanyl dihydro H thieno g
2022-02-28

Chemistry The 8-methylsulfanyl-4,5-dihydro-1H-thieno[3,4-g]isothiadizaole scaffold was synthesized from commercially available 1,3-dioxolane-2,1′-cyclohexane-4-one 17 (Scheme 1). The isothiadizaole ring was formed with SOCl2 from N-carboxamide hydrazine imine 19, which was prepared from 17 and hy
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Introduction Glycogen synthase kinase GSK is an
2022-02-26

Introduction Glycogen synthase kinase-3 (GSK-3) is an enzyme playing multiple roles in animal tissues and organs, and Vacuolin-1 is not an exception. Apart from involvement in regulation of apoptosis and survival GSK-3 influences neuronal morphology, synapse formation, memory reconsolidation in ad
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In summary we have designed and optimized a
2022-02-26

In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstra
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Disrupting the dialog between microbiota and
2022-02-26

Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated
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br Conflict of interest statement br Acknowledgements We
2022-02-26

Conflict of interest statement Acknowledgements We acknowledge the support of Zoetis Animal Health, Estrotect, Select Sires and Texas A&M AgriLife Research. The assistance of Randle Franke and Ernest Soto is also gratefully acknowledged. Background Luteal phase deficiency (LPD) is caused b
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br Acknowledgements This work was supported by the
2022-02-26

Acknowledgements This work was supported by the grants from National key Basic Research Program of China (2012CB124702), 948 Program (2015-Z33), National Natural Science Foundation of China (31172093, 31301947), the National Science Foundation for Fostering Talents in Basic Research (J1103510), S
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Psoriasis is an inflammatory skin disease characterized by e
2022-02-26

Psoriasis is an inflammatory skin disease characterized by epidermal hyperplasia; micro-abscesses; neo-angiogenesis; a proinflammatory cytokine environment involving alterations of IL-17A, IL-23, and TNF-α; and activation of and infiltration by macrophages, mast cells, neutrophils, CD11c+ dendritic
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LY 294002 The molecular mechanism of gliotransmitter release
2022-02-26

The molecular mechanism of gliotransmitter release is not fully understood until now, and previous studies have emphasized that the elevation of [Ca2+]i triggers vesicular LY 294002 of glutamate. Parpura et al. reported that the essential role of Ca2+ release from internal stores in glutamate releas
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Silicristin br Acknowledgments br Introduction Histone deace
2022-02-25

Acknowledgments Introduction Histone deacetylases (HDACs) related to tumor suppressor genes have become promising targets for the treatment of cancer [1,2]. Under the normal physiological conditions, Histone acetyltransferases (HATs) and histone deacetylases (HDACs) together regulate the acety
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br Acknowledgments We thank Dr Kathleen Sullivan of Merck
2022-02-25

Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 norepinephrine bitartrate expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistan
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Our synthetic approach to GPR antagonists was designed
2022-02-25

Our synthetic approach to GPR55 antagonists was designed so that many different structures could be accessed to rapidly explore initial SAR, along with validating or modifying our current model (). The synthesis begins with the coupling of a carboxylic ornidazole to 4-piperidone by first forming th
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