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Two pathways have emerged to
2021-11-06

Two pathways have emerged to explain the beneficial metabolic effect of Roux-en-Y bypass [Fig. 3]. Firstly, the rapid delivery of nutrients to the distal small intestine and bowel might up-regulate secretion of a physiological stimulus that improves glucose homeostasis. As such, GLP-1 represents an
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The sexual dimorphism in dlGALR a and dlGALR
2021-11-06

The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that
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In addition several other considerations were
2021-11-06

In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty Zoniporide hydrochloride receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization ef
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Pharmacological inhibition of PKR seems to be an interesting
2021-11-06

Pharmacological inhibition of PKR seems to be an interesting strategy for revealing the role of PKR in oxytosis and ferroptosis. The oxindole/imidazole derivative C16 was identified by screening a library of 26 different ATP-binding site-directed inhibitors of varying structure that is more selectiv
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br Introduction Thrombosis is one of
2021-11-06

Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable rilpivirine and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 million (1–2
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Here we show in contrast to previous work that several
2021-11-06

Here we show, in contrast to previous work, that several phenotypes associated with Orb6 inactivation, including increased cell width, are independent of Gef1. We further find that Orb6 positively regulates exocytosis, also independently of Gef1. To identify novel targets of Orb6, we performed quant
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br Discussion Our results showed that the histamine H recept
2021-11-06

Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation
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DDD107498 In conclusion while class I HDAC inhibitors isofor
2021-11-06

In conclusion, while class I HDAC inhibitors, isoform-specific HDAC3 and HDAC6 inhibitors may represent novel therapeutic targets for prevention of clinical AF onset and progression, the specific HDAC3 and HDAC6 inhibitors may be more appropriate because of their limited off-targets effects. Besides
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Whereas binding of activated RhoA to the PH domains of
2021-11-05

Whereas binding of activated RhoA to the PH domains of the RhoGEFs is proposed to mediate positive feedback regulation (Chen et al., 2010b, Medina et al., 2013), the sequestration of p190RhoGEF by activated Rac1 reveals a novel putative physiological role, that is to utilize Rac1 to directly drive r
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br Funding M I is supported
2021-11-05

Funding M.I. is supported by European Research Council (ERC) Consolidator Grant 725038, Italian Association for Cancer Research (AIRC) Grant 19891, Italian Ministry of Health (MoH) Grant GR-2011-02347925, Lombardy Foundation for Biomedical Research (FRRB) Grant 2015-0010, the European Molecular B
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Besides its established insulinotropic actions GIP has been
2021-11-05

Besides its established insulinotropic actions, GIP has been shown to possess other direct beneficial effects on the beta cell, including stimulation of growth, differentiation, proliferation and survival.21, 22, 23 It has also been shown to stimulate proinsulin gene transcription and translation. M
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Besides the described effects on gross locomotor function
2021-11-05

Besides the described effects on gross locomotor function, impairment of visuo-motor coordination and fine-motor skills like resting tremors, bradykinesia and rigidity were also investigated, reflecting on the symptomatology of Parkinson's disease in humans (Inzelberg et al., 2008). Preclinically, t
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ETV plays an important role in tumorigenesis and
2021-11-05

ETV5 plays an important role in tumorigenesis and metastasis. For example, chromosomal rearrangement of ETV5 which results in increased ETV5 level is believed as a common event driving human prostate cancer (Helgeson et al., 2008; Huang and Waknitz, 2009). Ghrelin/acyl-ghrelin also plays an importan
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Because of its role in
2021-11-05

Because of its role in the cleavage of Aβ and the fact that many genetic forms of AD are caused by mutations in the enzyme, GS has long been a target for drug development, though previous clinical trials of Semagacestat, a GS inhibitor, have failed due to an increase in skin cancer, and a decrease i
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Photoincorporation of pTFDBzox AP occurred
2021-11-05

Photoincorporation of 21-pTFDBzox-AP occurred predominantly in the β3 subunit, very modestly in the α1 subunit and not at all in the γ2 subunit. These observations taken together with the sensitivity of 21-pTFDBzox-AP enhancement of GABA currents to the α1 M1 mutation Q242 W4 suggest that the 21-pTF
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