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From the general synthetic route we first synthesized a
2021-01-11

From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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br Objectives br Study design Thirty
2021-01-11

Objectives Study design Thirty KTx recipients were enrolled in this pilot study from December 2015 to May 2016. Patient demographics are presented in Table 1. The inclusion criteria were: age ≥ 18 years and CMV-IgG serostatus (D+/R−, D+/R+, D−/R+) pre-Tx. All patients were enrolled during the
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br Discussion Of the age related
2021-01-11

Discussion Of the age-related differences in serum non-cholesterol sterols, we first deal with the cholesterol precursors. After birth, the markedly elevated serum desmosterol values decreased during the first year of life, and after 1 year of age they were similar between the other age groups. S
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Berner et al used a meta analysis to show
2021-01-11

Berner et al used a meta-analysis to show that sildenafil resulted in an effect of 9.65-point improvement. Tadalafil could be pooled into an effect of 8.52-point improvement, and vardenafil showed an effect of 7.50-point improvement. In our present studies, 200 mg udenafil resulted in an effect of 8
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crotaline br Introduction Oral contraceptives OCs are the
2021-01-11

Introduction Oral contraceptives (OCs) are the most commonly used medication for contraception all over the world and are also used in the treatment of menstrual disturbances and hyperandrogenism in women with polycystic ovary syndrome [1]. The impact of OC steroids on cardiovascular pathophysiol
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Defactinib br Results br Discussion The
2021-01-11

Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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To explore the mechanism behind
2021-01-09

To explore the mechanism behind differential activation kinetics, Marcott et al. (2018) manipulate local dopamine dynamics. They show that differences in dopamine concentrations are not responsible for different D2R activation kinetics, since D2-IPSCs reach similar amplitudes at different rates in N
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C PHNO has been described
2021-01-09

[11C]-(+)-PHNO has been described as a full agonist at both D2 and D3 receptors [54,55]. [11C]-(+)-PHNO was initially developed as a PET radiotracer for imaging the high affinity state of the D2 receptor (i.e., highD2) as a means of measuring synaptic dopamine changes in response to pharmacologic ch
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Drug drug interactions are frequently attributed to function
2021-01-09

Drug-drug interactions are frequently attributed to functional alterations in CYP enzymes, including inhibition and induction (Chen et al., 2014, Wang et al., 2013). Mechanism-based inhibition is an irreversible form of enzyme inhibition and could form a stable inhibitor-enzyme complex, which is tho
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E3330 br Results Table shows demographics and
2021-01-09

Results Table 1 shows demographics and clinical features of subjects with obesity and controls. Before surgery five obese were diabetic, only one on glucose-lowering therapy; three obese were dyslipidemic and assumed lipid lowering medications. Lathosterol levels were significantly higher in pati
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Plant uptake of P from OA could also be affected
2021-01-09

Plant uptake of P from OA could also be affected by arbuscular mycorrhizal fungi (AMF). Approximately 80% of terrestrial plant species form symbiotic associations with AMF (Smith and Read, 2010) which can enhance plant P uptake (Facelli and Facelli, 2002, Pearson and Jakobsen, 1993, Tibbett, 2000).
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br Loss of Chk sensitizes
2021-01-09

Loss of Chk 1 sensitizes WZ4003 to hypoxia/reoxygenation In contrast to Chk 2, studies have identified Chk 1 as being phosphorylated in an ATR-dependent manner at residue serine 345 during hypoxia [18]. More recently, siRNA mediated inhibition of Chk 1 signaling was found to sensitize cells expo
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br Conclusions br Acknowledgement Grant
2021-01-09

Conclusions Acknowledgement Grant support: Ministry of Health (n. of grant: RBAP10447J_004 to N. Baldini), Italian Association for Cancer Research (n. of grant: 11426 to N. Baldini). Introduction Ewing sarcomas (ES) and primitive neuroectodermal tumors (PNET) are related childhood tumors.
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EC barrier dysfunction triggered by inflammatory mediators i
2021-01-09

EC barrier dysfunction triggered by inflammatory mediators involves more than one mechanism, explaining the partial attenuation of EC barrier compromise obtained with PKA and Epac activators. PKA-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) has been shown to make a posit
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EP is the major receptor to mediate PGE induced
2021-01-09

EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by RP 67580 in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3], [16], [26]. However,
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