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Within the Class II receptors the Type
2020-09-15
Within the Class II receptors, the Type I IFN receptor subunit, IFNAR-1, is exceptional in having four tandem FNIII domains, denoted here D1–D4. This structure appears to have arisen as a tandem mg to mol of the basic D1/D2 structure; thus, D1 and D3 of IFNAR-1 are more closely related, as are D2 an
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It should also be noted that remarkable individual differenc
2020-09-15
It should also be noted that remarkable individual differences in extinguished fear bradycardia (i.e., CS+E vs. CS−E) during initial Day 2 recall test were observed, particularly within Met carriers. Exploratory analyses revealed that these individual differences were partly driven by the level of r
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br Materials and methods br
2020-09-15
Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen
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The first mammalian mutation linked
2020-09-15
The first mammalian mutation linked to CR was identified in golden hamsters (Mesocricetus auratus). The mutation was an autosomal allele first described in the late 1980s [8] and was identified using positional cloning [9]. These animals displayed a shortened period length (20h in homozygous animals
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The repeat sequence TTAGGG of
2020-09-15
The repeat sequence “TTAGGG” of telomere could be directly recognized by TERF1. TERF1 is indispensable for the maintenance of telomere 3-bromo-5-phenyl Salicylic Acid structure and integrity (Tan et al., 2017). Trf1 genetic depletion in vivo induces a persistent DNA damage response and telomere unc
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Selective inhibitor of phosphodiesterase type PDE I is
2020-09-15
Selective inhibitor of phosphodiesterase type 5 (PDE5I) is commonly used for ED treatment. PDE5I exhibits its vasodilatory effect by inhibiting the degradation of cyclic guanosine monophosphate (cGMP), which relaxes the smooth muscle and allows increased blood flow for penile tumescence. Udenafil (D
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br Conclusion br Declaration of interest br Introduction Gly
2020-09-15
Conclusion Declaration of interest Introduction Glyphosate [N-(phosphonomethyl)glycine] is the main active ingredient in one of the most widely used herbicides in the world. The commercially used concentrations of glyphosate range from 1% for domestic use to 41% for conventional agricultura
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br Methods br Discussion In a recent survey among high
2020-09-15
Methods Discussion In a recent survey among 2625 high risk patients on atorvastatin, 10.5% of patients achieved an LDL-target of glycogen synthase kinase level for improvement of acceptance and adherence to effective lipid lowering therapy are warranted to maximize the benefits of standard tr
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br STAR Methods br Acknowledgments We are grateful
2020-09-15
STAR★Methods Acknowledgments We are grateful to Amaia Lujambio, James Fagin, and Ramon Parsons for providing cell lines and Evripidis Gavathiotis for critical reading of the manuscript. We would like to thank Saboor Hekmaty for providing expertise with RNA-seq analysis. P.I.P. would like to ac
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Further modifications on the position of compound
2020-09-15
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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Furan analogs and N methylpyrrole analogs had completely dif
2020-09-15
Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 PF-5274857 mg affinity and an increased antagonist activity, while the corresponding chemical modi
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A wealth of studies support the key role of
2020-09-15
A wealth of studies support the key role of high NO in promoting higher blood flow and thus greater O2 delivery to working tissues in healthy Tibetans and thus partly compensate hypoxia induced low arterial O2 content [7,9,27]. We observed high eNOS mRNA, protein and enzyme activity in Ladakhi women
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Our study revealed elevated basal Akt phosphorylation in
2020-09-15
Our study revealed elevated basal Akt phosphorylation in diet-induced obesity, the effect of which was reversed by ETAKO. Activation of Akt promotes cardiac hypertrophy via a number of cellular mechanisms including activation of its downstream targets such as mTOR and GSK3β [45, 46]. Short-term acti
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br Conflicts of interest br Financial support NZ is
2020-09-14
Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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Currently much effort has been made to design and synthesize
2020-09-14
Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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