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br Conclusions This report describes the discovery of a new
2021-07-19

Conclusions This report describes the discovery of a new class of host-directed antiviral agents characterized by a 1-aryl-4,6-diamino-1,2-dihydrotriazine scaffold, responsible for a host (human) DHFR inhibition mechanism. Host-targeting antivirals represent an alternative and emerging strategy t
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Studies of Jelski and Szmitkowski show
2021-07-19

Studies of Jelski and Szmitkowski show that differences of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) activity between chpg receptor of many cancers and healthy tissue may be one of the factors intensifying carcinogenesis [7]. Moreover, changes of ADH and ALDH activity in cancer
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Recent pharmaceutical research in the field of respiratory d
2021-07-19

Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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Boc-D-FMK From the general synthetic route we
2021-07-19

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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We have previously disclosed the
2021-07-19

We have previously disclosed the discovery of a 7-azaindole-3-acetic Prostaglandin E2 CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that
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neuronal nitric oxide synthase br Materials and methods br R
2021-07-19

Materials and methods Results Discussion Consistent with previous reports (Barr et al., 2010, Vuong et al., 2010), the current study demonstrates that rats treated with amphetamine exhibit heightened anxiety states during withdrawal. Furthermore, icv. infusion of a CRF2 receptor antagonist
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Among the various neurotransmitter systems pointed out to
2021-07-19

Among the various neurotransmitter systems pointed out to play a role in the mediation of defensive and antinociceptive responses elicited by environmentally aversive stimuli, the neuropeptide corticotropin-releasing factor or hormone (CRF or CRH) has attracted the interest of many researchers inves
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Meanwhile high levels of extraversion have been
2021-07-19

Meanwhile, high levels of extraversion have been associated with weaker conditioning and faster sch772984 learning (Eysenck, 1970). Similar to neuroticism/anxiety, the role of extraversion for fear conditioning and extinction has found only limited empirical support (Rauch et al., 2005) with severa
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It would be very useful if
2021-07-19

It would be very useful if unphosphorylated CK1s could be prepared using an E. coli expression system without the troublesome in vitro phosphatase treatment. So far, it has been shown that coexpressed λPPase, a Mn2+-dependent protein phosphatase that can dephosphorylate phospho-Ser/Thr/Tyr [20,21],
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Our earlier experimental studies showed neutral i e non prol
2021-07-19

Our earlier experimental studies showed "neutral", i.e. non-proliferative, effects of progesterone but a large increase in proliferation using certain progestins; however, this was only in the presence of PGRMC1 [[13], [14], [15], [16], [17], [18], [19]]. The next step was to investigate whether thi
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One possibility to differentiate between the two failure
2021-07-19

One possibility to differentiate between the two failure modes, and also to identify the corresponding characteristics of the resulting fracture surface, is a series of FNCT measurements with varying nominal (initial) stress. The dependence of the observed time to failure tf on the actual stress cha
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Although several genomic technologies including the generati
2021-07-19

Although several genomic technologies, including the generation of ERRγ-specific knockout mice, have revealed that ERRγ plays a pivotal role in cellular bioenergetics [1], its involvement in other metabolic pathways has been appreciated only recently. Therefore, we highlight recent findings on the r
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In the horse oviduct the EP receptor was most
2021-07-19

In the horse oviduct, the EP2 receptor was most strongly expressed in epithelial Cy3 carboxylic acid (non-sulfonated) particularly in nonciliated (secretory) epithelial cells as evidenced by IHC. Furthermore, relative amount of EP2 mRNA was greater in the ampulla than in the isthmus, although this l
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br Halogenases Enzymatic C H
2021-07-19

Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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Long stretches of ssDNA have also been
2021-07-17

Long stretches of ssDNA have also been observed in rad53-1 mutant Arctigenin under replication stress using EM images (Sogo et al., 2002). Deletion of EXO1, a 5′-to-3′ exonuclease, can suppress the generation of ssDNA detected in rad53-1 mutant cells (Cotta-Ramusino et al., 2005). It was thus propos
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