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Lastly haspin inhibitor was assessed against a panel of
2022-05-24

Lastly, haspin inhibitor was assessed against a panel of 292 kinases at 10μM. At this high concentration, the fostamatinib inhibited thirteen kinases, in addition to haspin, ⩾90%., These kinases were CaMK2b, CaMK2d, CDK7-CycH-Mat1, cGK2, CK1d, CLK1, CLK2, DYRK1A, DYRK1B, DYRK3, PASK, PIM1 and PKD
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ZM 306416 synthesis br Author contributions br Acknowledgeme
2022-05-24

Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa
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In contrast to short term effects long term exposure
2022-05-23

In contrast to short-term effects, long-term exposure of beta cells to FFAs impairs insulin secretion and triggers apoptosis [13]. The deleterious effects of FFAs have been linked to altered glucose/fatty Ac-YVAD-CHO mg oxidation cycle [13], decreased NADPH content [14], endoplasmic reticulum (ER)
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br Dysregulation of glutamate transporter expression and fun
2022-05-23

Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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Human GS is a multi subunit complex consisting of four
2022-05-23

Human GS is a multi-subunit complex consisting of four components: presenilin 1 (PS1), presenilin enhancer 2 (PEN-2), anterior pharynx-defective 1A (APH-1A) and nicastrin (NCT) (Fig. 1a) [5,6]. PS1 comprise nine transmembrane helices (TM 1–9) and contains the catalytic aspartate residues in its TM6
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Nicastrin is heavily glycosylated contributing
2022-05-23

Nicastrin is heavily glycosylated, contributing 40–70KDa to the molecular weight of human γ-secretase. Among the 16 predicted N-linked glycosylation sites in the ECD, 11 have been unambiguously identified. The glycans appear to mostly stabilize the local structure, thus contributing to the folding a
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br Introduction Alzheimer s disease AD affects ca
2022-05-23

Introduction Alzheimer's disease (AD) affects ca. 46 million people worldwide [1] and it is expected that the number will double or triple by 2030 or 2050, respectively, while no significant progress has been made in research for early diagnosis and new efficient therapies. Currently available me
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GPR which is also known as FFA receptor FFAR or
2022-05-23

GPR40, which is also known as FFA receptor 1 (FFAR1 or FFA1), was identified as an orphan receptor in the search for novel human galanin receptor (GALR) subtypes in 1997. Using reverse pharmacology approaches measuring calcium transients, GPR40 were deorphanized and characterized as being activated
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br Redox cancer therapy The understandin http
2022-05-23

Redox cancer therapy The understanding of ROS mechanisms supported the development of two parallel anticancer strategies based on ROS modulation, the use of antioxidants for cancer prevention and the use of ROS inducers to exacerbate oxidative stress to lead cancer plx4720 synthesis to death [27
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br Formation of secretory vesicles and trafficking toward pl
2022-05-23

Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for gap junction off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013). Bin/A
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br Materials and methods br Results
2022-05-23

Materials and methods Results Discussion In this study, we demonstrated that, at the level of hREECs, blockade of the ETA receptor partially inhibited the effect of NPY on the secretion of ET-1. This suggests that the secreted ET-1 by NPY contributes, in part, to its own secretion via activ
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br Introduction Currently HIV infection treatment guidelines
2022-05-23

Introduction Currently, HIV-1 infection treatment guidelines adopted in USA and EU provide for the simultaneous administration of three antiretroviral drugs (HAART “Highly Active Anti-Retroviral Therapy”) in severely compromised patients [[1], [2], [3]]. Coupling at least two different mechanisms
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In various models histamine has been shown
2022-05-23

In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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In recent years the Hippo signaling pathway has emerged
2022-05-23

In recent years, the Hippo signaling pathway has emerged as an important regulator balancing cell proliferation and differentiation [[5], [6], [7]]. The pathway components, first described in the fruit fly Drosophila melanogaster, are highly conserved across different phyla [6]. The signaling pathwa
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br Discussion In this study we show
2022-05-23

Discussion In this study, we show that conditional loss of Yap/Taz in the endocardium results in a thin compact myocardium and early postnatal lethality. We also report that loss of Yap/Taz in the endocardium leads to diminished expression of Nrg1, which is a crucial endocardial-derived factor t
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