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Our recent discovery M P H R
2021-03-18

Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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Despite the significant associations between TNF and TRAIL
2021-03-18

Despite the significant associations between TNF-α and TRAIL in our results, the use of a single top cytokine in predicting sPTB is limited, and the previous study using the specific candidate cytokines failed to accurately predict the risk for sPTB in asymptomatic women, with AUC ranged from 0.48 t
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The intricate roles and neural
2021-03-18

The intricate roles and neural systems and mechanisms involved in the CRF1 and CRF2 mediation of spontaneous and stress-induced anxiety behavior remain to be defined. Of particular relevance are studies evaluating the behavioral actions of CRF1 and CRF2 receptors separately as well as together. For
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Our results also showed that
2021-03-18

Our results also showed that the highest dose of Astressin2-B increased the rewarding effects of cocaine, since non-defeated animals treated with this dose developed CPP with a sub-threshold dose. We monitored the acute effects of 30 µg/kg of Astressin2-B and found an increase of anxiety in the open
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flavopiridol Currently approved anti obesity drugs for long
2021-03-18

Currently approved anti-obesity drugs for long term use such as orlistat, lorcaserin and liraglutide are efficient in reduction of weight gain but are limited in usage due to their adverse effect profile and higher cost (Krentz et al., 2016; Mopuri and Islam, 2017). In flavopiridol to this, plant de
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Apicidin Though limited to a large cohort of
2021-03-18

Though limited to a large cohort of self-reported healthy individuals, associations between individual Apicidin have been identified which may be clinically significant. Though slight, there is a relationship between the CYP2D6-inferred metabolizer phenotype and the diplotype-predicted activities o
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br Acetylcholinesterase and cholinergic signaling
2021-03-18

Acetylcholinesterase and cholinergic signaling The concept of a synapse between a neuron and an innervated cell, and the receptors that mediated their interaction, was developed by Bernard, Ehrlich, Sherrington, Langley and others (see [7], [8], [9]. It was long debated whether transmission of ne
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br Conclusions br Declaration of interest br Acknowledgment
2021-03-17

Conclusions Declaration of interest Acknowledgment This work was supported by an AIRC (Associazione Italiana Ricerca Cancro-Milan) Grant KFR062-2 to A.G.L, by Ricerca Funds by Fondazione IRCCS Ca’ Granda Ospedale Maggiore Policlinico (Grant No. 180/01) and by the ERA-NET “ERare” (Grant G
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Irsogladine Introduction Pain is frequently the
2021-03-17

Introduction Pain is frequently the first clinical symptom of head and neck carcinoma. Indeed, pain is the initial reason leading ∼70% of cancer patients to seek professional assistance (Lam & Schmidt, 2011; Rettig & D’Souza, 2015; Schmidt, 2014). Clinically, cancer-induced facial pain can be evoke
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Silvestrol The totality of evidence from randomized clinical
2021-03-17

The totality of evidence from randomized clinical trials supports the premise that worsening Silvestrol failure is a class effect of DPP-4 inhibitors. A meta-analysis by Verma et al. (54) of 100 randomized controlled clinical trials reported that the use of DPP-4 inhibitors was accompanied a signif
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Extracellular uridine can be transported across the cell
2021-03-17

Extracellular uridine can be transported across the cell membrane to enter the nucleotide salvage pathway. A colon cancer cell line supplemented with uridine was capable of growing normally in the presence of 1 μM brequinar (Peters et al., 1992). The supplemented uridine may be transported into the
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A An optimized BEI SEIscore
2021-03-17

(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compar
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Cytokines are small secreted proteins that mediate and regul
2021-03-17

Cytokines are small secreted proteins that mediate and regulate immunity, inflammation, and hematopoiesis. They are produced in response to an immune stimulus. Cytokines regulate the intensity and duration of the immune response by stimulating or inhibiting the activation, proliferation, and/or diff
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For LAU extracted ion chromatograms
2021-03-17

For LAU 399, extracted 71 5 chromatograms of the blank, t0, and t120 samples for the diagnostic product ion m/z 163.0216 are provided in Fig. S11, and extracted ion chromatograms of the t120 sample for m/z 163.0216 (diagnostic product ion), and m/z 308.1677 and 306.1522 (metabolites) are shown in Fi
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Unexpectedly CRF receptor agonist and antagonist evoked simi
2021-03-17

Unexpectedly, CRF2 receptor agonist and antagonist evoked similar effects in the fall in tail skin temperature caused by restraint. However, Ucn3 reduced basal values of tail skin temperature, thus indicating that some degree of basal vasoconstriction caused by BNST treatment with Ucn3 may have cont
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