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We have expressed the ECDs of the human and
2023-03-01

We have expressed the ECDs of the human α1, β1, γ and ɛ AChR subunits in the past using the methylotropic yeast Pichia pastoris as soluble glycosylated proteins [15], [16]. Further work with the γ subunit ECD revealed a marked improvement of the solubility and yield following the mutation of hydroph
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In the previous study we demonstrated the importance of the
2023-03-01

In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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hydroxydopamine OHDA is a selective catecholaminergic neurot
2023-03-01

6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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From our in vivo studies and previously reported findings
2023-03-01

From our in vivo studies and previously reported findings [25], we have found that orteronel possesses excellent oral BA. Indeed, single oral dosing of orteronel at doses of 0.3–10.0mg/kg decreased serum DHEA levels in a dose-dependent manner. Of interest, DHEA levels did not return to levels compar
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br Research perspective In vitro and in vivo studies have
2023-03-01

Research perspective In vitro and in vivo studies have demonstrated that increased LPA/ATX signaling contributes to cancer initiation and progression. Recent findings on the role of non-tumoral ATX in cancer progression and metastasis highlighted a new functional contribution for the microenviron
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Imatinib is a well known anticancer
2023-03-01

Imatinib is a well-known anticancer drug used in Chronic Myeloid Leukemia (CML) against the altered expression/activity of tyrosine kinase resulting from the fusion of BCR-ABL in leukemic blasts. It has been demonstrated that Imatinib can induce autophagy in BCR-ABL expressing EW-7197 receptor (K562
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i am g br Implementation of sacubitril valsartan into clinic
2023-02-25

Implementation of sacubitril/valsartan into clinical practice Following on from the results of PARADIGM-HF, sacubitril/valsartan was given regulatory approval for use in patients who conform to the main inclusion criteria of the trial; NYHA functional class II–IV, reduced left ventricular ejectio
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Consistent with the in vitro results memantine
2023-02-25

Consistent with the in vitro results, memantine ameliorated Aβ-induced cytotoxicity in rat primary cortical cultures. Studies reported that memantine protected neurons against the damage caused by aggregated Aβ40 or Aβ42 oligomers in vivo[26], [27]. These results suggest that, in addition to its ne
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AAT enzyme activity was readily detected in crude cell
2023-02-25

AAT enzyme activity was readily detected in crude cell-free extracts obtained from berry tissues of all accessions but displayed different substrate selectivities (Fig. 2). Cell-free extracts derived from ‘Muscat Hamburg’ berries showed the highest AAT activity with all alcoholic substrates tested,
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Ketogenic diets are more effective in promoting weight loss
2023-02-25

Ketogenic diets are more effective in promoting weight loss than conventional caloric restriction [26] however, their effect on hepatic glucose and lipid metabolism remains inconclusive. Blood glucose homeostasis is tightly regulated. In both mice and humans consuming KD, baseline blood glucose decr
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Extracellular adenosine acts as a local modulator of
2023-02-25

Extracellular adenosine acts as a local modulator of cell function via four adenosine receptor subtypes (A1Rs A2AR, A2BR, and A3R) that are involved in numerous physiological and pathophysiological processes [31]. Each is encoded by a separate gene and has different functions, although with some ove
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Encouraged by this observation a
2023-02-25

Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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Introduction Mammalian cells express the seven STAT family m
2023-02-25

Introduction Mammalian Liproxstatin-1 express the seven STAT family members STAT1, −2, −3, −4, −5A, −5B, and −6 [1], [2]. All STATs exert physiologically important roles as homo- and heterodimers [2], [3], [4]. Cytokines and growth factors activate STATs through the activation of kinases that phos
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To reconstruct the amino acid sequence
2023-02-25

To reconstruct the amino CGRP (rat) sequence of an ancestral β subunit a molecular phylogeny is required, which is inferred from a β subunit sequence alignment. To build this alignment we searched the NCBI database for proteins similar in sequence to the human muscle-type β subunit precursor protei
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Indanone and its analogues are useful intermediates for the
2023-02-25

1-Indanone and its analogues are useful intermediates for the synthesis of compounds some of which have applications as pharmaceuticals, especially as analgesic and antihypertensive as well as tobacco flavoring agents. Indanones are commonly used as starting agent for the synthesis of ninhydrin whic
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