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G quadruplex DNA structures may
2022-07-25
G-quadruplex DNA structures may exist in either positive or negative strand of a promoter to regulate gene expression. The positive strand of the HOXC10 promoter is overall C-rich in the 1000 bp upstream of the TSS (36.6% of C versus 24.1% of G) and contains many C-runs; thus, G-quadruplex structure
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Ligand selectivity may directly be
2022-07-22
Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This
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The typical pharmacophore for GPR agonists
2022-07-22
The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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535 2 Our previous study had shown that silencing FFAR expre
2022-07-22
Our previous study had shown that silencing FFAR1 expression weakened the action of PIO in increasing insulin secretion in lipotoxic β 535 2 [6]. Resent research found that PIO promoted insulin secretion by upregulating FFAR1 [17]. Therefore, we presumed that FFAR1 may be involved in the anti-lipoa
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Conformational analysis provides further insight into the SA
2022-07-22
Conformational analysis provides further insight into the SAR trends apparent in . Acyclic precursors – are 25–50-fold less active than their macrocyclic counterparts – against Pyk2. The global minima for – are conformations in which the –NHCH– linker between the pyrimidine and pyridine rings is sta
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br Materials and methods br
2022-07-22
Materials and methods Results Discussion In general, we have demonstrated that the CRISPR/dCas9-based system, fused with 2 × PP7 and PCP-EZH2, could stably and precisely methylate the H3K27 at specific locus of C/ebpα to silence gene expression and inhibit adipogenic differentiation in 3T3
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The most abundant form of Hat p in the
2022-07-22
The most abundant form of Hat1p in the nucleus is apt to be in the form of the NuB4 complex [96]. In the context of SGI-1776 sale assembly, the function of the NuB4 complex may be similar to that ascribed for the cytoplasmic HAT1 complex. That is, the NuB4 complex may be involved in directing newly
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In this study there is
2022-07-22
In this study, there is a limitation in the study of sex differences. Only female rats were used in our study. This is because the rats cannot urinate autonomously after SCI. Manual Cy3 NHS ester (non-sulfonated) emptying was needed until reflex bladder emptying was established (Lu et al., 2008, Ma
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The increased levels of proinflammatory cytokines in BALF ar
2022-07-22
The increased levels of proinflammatory cytokines in BALF are noted during ALI/ARDS, and the persistent elevation of these mediators may exaggerate systemic or focal inflammatory reaction with a worse outcome. These cytokines, particularly TNF-α and IL-6, play essential roles in ALI [16,17]. The ove
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HDAC enzymes oppose the effects of HATs
2022-07-22
HDAC enzymes oppose the effects of HATs by reversing lysine acetylation, an action that restores the positive charge of the lysine thus stabilizing the local chromatin structure. By removing acetyl groups from ε-amino lysines of proteins, HDACs not only alter transcription, but also promote either t
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br Conflict of interest br Acknowledgements br
2022-07-22
Conflict of interest Acknowledgements A Class of Unconventional, Dimerization-Activated GTPases GTP-binding proteins, or GTPases, are a superfamily of proteins that regulate numerous cellular pathways 1, 2, 3, 4. Pioneering work on the extended Ras subfamily of GTPases, exemplified by Ras,
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br Experimental br Acknowledgments The authors are grateful
2022-07-21
Experimental Acknowledgments The authors are grateful to Fundamental Scientific Research Fund of Chinese Academy of Medical Sciences (No. 2016ZX350030) for financial support. Introduction 2-Lysophosphatidylcholines (1-acyl-glycero-3-phosphocholines, 2-LPC) are blood derived factors involve
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br Results br Discussion The twin cysteine motif is an
2022-07-21
Results Discussion The twin-cysteine motif is an evolutionary conserved motif in all primate lentiviruses except HIV-1 and some strains of SIVcpz according to sequence analysis (Bohl et al., 2013). It is assumed that only those SIVcpz which have lost the twin-cysteines successfully evolved to
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Trypanosomatid GLO enzymes are monomeric and contain
2022-07-21
Trypanosomatid GLO2 enzymes are monomeric and contain a zinc–iron binuclear metal center (Irsch and Krauth-Siegel, 2004, Silva et al., 2008), similar to all other glyoxalases II. As mentioned, in T. brucei there are two GLO2 genes but only one encodes an enzyme with glyoxalase II activity (Irsch and
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Herein we report the discovery of AM AM maintains the
2022-07-21
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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