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We first investigated the influence of
2022-05-06

We first investigated the influence of the -acyl group of the glycine amide side chain and found that shorter linkers lead to better activities (–); simple -benzoyl substituents were always superior to the 3-arylpropanoyl group present in the high-throughput hit (). Electron withdrawing substituents
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Boc-D-Asp(OtBu)-OH.DCHA mg Glycogen synthase kinase GSK is c
2022-05-06

Glycogen synthase kinase 3 (GSK3) is currently considered to be a multifunctional serine/threonine kinase involved in a wide spectrum of cellular processes such as glycogen metabolism, cell proliferation, neuronal function, oncogenesis or embryonic development (for recent reviews see: Rayasam et al.
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SB 431542 In insects structural cuticular proteins CPs play
2022-05-06

In insects, structural cuticular proteins (CPs) play important roles in determining the diverse physical properties of the cuticle, depending on developmental stages, as well as different body regions, as a result of interactions with other CPs and the structural biopolymer chitin [4]. Many studies
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To maintain low Glu concentrations in the synaptic cleft
2022-05-05

To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino bun hot is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and in to
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The plasma levels of glucose and amino acids at day
2022-05-05

The plasma levels of glucose and amino acids at day 0 likely represent the function in utero since the blood was collected within 2h after birth. To elucidate the roles of intestinal transporters as determinants of plasma levels of glucose and amino acids, we analyzed the correlation between the exp
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Next the effects of a phenyl group
2022-05-05

Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-positio
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The presented results speak for the direct
2022-05-05

The presented results speak for the direct effects of ghrelin on rat spermatozoa, which are accomplished by the activation of the GHSR-1a receptor. Thus, the results seem to be of physiological significance in vivo since ghrelin, the natural ligand of GHSR-1a, was found to be present in the seminal
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In the last years a plethora of studies
2022-05-05

In the last years, a plethora of studies overstepped the classic concept of the ENS as purely modulator of GI secretion and motility, focusing on its potential as source of substances acting on immune cells and consequently involved in the control of local inflammatory events, as in the Inflammatory
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DNAzymes a series of nucleotide sequences with
2022-05-05

DNAzymes, a series of nucleotide sequences with specific catalytic activity, have been reported frequently applied in detection assays for such as ions and amino acids, due to the advantage in stability, high cost-effectiveness and modification convenience, by comparison with protein enzymes. The DN
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No G C pattern managed to capture all GQ
2022-05-05

No G4C pattern managed to capture all GQ forming sequences of the reference dataset. The sequences that were missed by even the most flexible models were AGATGGAGTGGAGAGG, AGGAGATGCAGGAG, AGAGGGTAGATGG and TTTTTAAAAGAAGGGGAGGAATAGGGGATATGA. In fact, the former three are not expected to form any unim
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br Medium to long chain
2022-05-05

Medium- to long-chain fatty acids Medium- to long-chain fatty acids impart a wide range of physiological effects. Medium-chain and long-chain fatty acids have 6–12 carbons and >12 carbons, respectively. As the energy source, these fatty acids are supplied primarily by food intake, biosynthesis, a
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Natural product based drug discovery can be enhanced with
2022-05-05

Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in isoprenaline binding assays, we used molecular modeling to predict how well these compound
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SBHA br Material and methods br
2022-05-05

Material and methods Results Discussion In the present study, we attempted to unravel the mechanism underlying the statin-mediated inhibition of FGFR3 signaling in chondrocytes, reported earlier by Yamashita and colleagues. We evaluated the role of statins in four different experimental sys
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br Materials and methods Patients
2022-05-05

Materials and methods Patients’ charts were reviewed retrospectively, and 165 consecutive patients (82 with cancer and 83 without cancer) who either started edoxaban (Lixiana®, Daiichi-Sankyo, Tokyo, Japan) therapy for the treatment of VTE or were switched from other oral anticoagulants to edoxab
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thz1 The structures of KDM A revealed
2022-05-05

The structures of KDM4A revealed a Cys-His Zn(II) binding site that is close to the substrate binding spot, which bioinformatic analyses indicated was not present in any other histone demethylase subfamily. Therefore, an alternative method to inhibit the KDM4 family (95) would be to use compounds th
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