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Malotilate Structurally the termini of FGF are
2021-11-06

Structurally, the termini of FGF21 are critical for effective signaling. Progressive amino Malotilate truncation at either end of the protein sequentially impairs FGF21 bioactivity, but via different mechanisms. Shortening at the N-terminus weakens its ability to activate the FGFR/KLB-complex but d
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Together the epigenetic interplay revealed in this study ena
2021-11-06

Together, the epigenetic interplay revealed in this study enabled us to expand the therapeutic potential of EZH2is from hematological malignances to solid tumors. In solid tumors, EZH2i-driven transcriptional changes are shown to be dispensable of H3K27me-regulated transcriptional network. Instead,
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SCH is a H R receptor
2021-11-06

SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obese
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A number of studies have reported
2021-11-06

A number of studies have reported that lncRNA may function as sponge to interact with miRNAs at posttranscriptional level, thereby regulating miRNA targeted genes (Tang et al., 2015, Han et al., 2015). For example, lncRNA Malat1 induces autophagy by regulating ULK2 via sponging miR-26b (Li et al., 2
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br Materials and Methods A human skin
2021-11-06

Materials and Methods A431 (human skin SCC) and HT-297.T (human AK) cell lines were purchased from ATCC (Manassas, VA) and were maintained in DMEM supplemented with 10% fetal calf serum, 4 mM L-Gln, 1 mM sodium pyruvate, 100 U/mL penicillin, and 1 μg/mL streptomycin. Human HK1 and HK2 plasmids we
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A more quantitative view of kinase specificity suggests
2021-11-05

A more quantitative view of kinase specificity suggests a continuum of phosphorylation rates for the various substrates of a particular kinase (Figure 4A). Such differences in ‘substrate quality’ can arise from variations in phosphorylation site or docking sequences and may explain why the timing or
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In summary we obtained and type
2021-11-05

In summary, we obtained - and -type of linaclotide by protein chemical synthesis and acquired the X-ray crystal structure of linaclotide for the first time through racemic crystallization technique. The structure of linaclotide forms a compact spatial structure containing three- turns through three
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The ketone body receptor HCA is most
2021-11-05

The ketone body receptor HCA2 is most likely not active under normal conditions, since local levels and plasma levels of ketone bodies such as β-HB are too low to activate the receptor. However, overnight fasting or prolonged starvation results in plasma levels of the ketone body in the millimolar r
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So far GnRH receptors have been detected in
2021-11-05

So far, GnRH receptors have been detected in the human ovary, but their physiological importance is still unclear (). In particular, GnRH receptors as well as GnRH types I and II have been localized in the granulosa Kif15-IN-1 of pre-ovulatory follicles, but not of follicles from the primordial to
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DNA repair is essential for cell survival and for
2021-11-05

DNA repair is essential for cell survival and for tissue homeostasis given that cellular DNA is constantly challenged by various endogenous and exogenous genotoxic factors that generate DNA damage: structural and chemical modifications of a primary DNA sequence. Various organisms have evolved multi
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br Materials and methods br Results
2021-11-05

Materials and methods Results Discussion l-glutamate is the major excitatory neurotransmitter in the brain, and is functionally involved in many processes of the nervous system which have been connected with several neurological diseases [4]. These conditions are characterized by the time-d
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br Acknowledgements br Introduction Aminoacyl tRNA synthetas
2021-11-05

Acknowledgements Introduction Aminoacyl-tRNA synthetases catalyze the formation of an ester bond between an amino Chlorogenic acid synthesis and the 3′ end of a tRNA in a two-step reaction. First, the amino acid is activated and an enzyme-bound adenylate intermediate is formed. Then, the amin
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The mechanism underlying the anorectic effect of OXM is
2021-11-05

The mechanism underlying the anorectic effect of OXM is well established. It is centrally mediated via GLP-1 receptor activation, confirmed by both pharmacological blockade of the GLP-1 receptor, and using GLP-1 receptor knock-out mice [2], [11], [12]. However, the mechanism by which it increases en
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Different responses in feed intake have been noticed followi
2021-11-05

Different responses in feed intake have been noticed following administration of exogenous GHRL (peripherally or centrally) depending on animal species. In mammals, injection of GHRL stimulates food intake (orexigenic effect) (reviewed in Kaiya et al., 2013b). In contrast, in domestic birds, exogeno
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br Experimental br Results and discussion br
2021-11-05

Experimental Results and discussion Conclusion In conclusion, four bisnaphthalimides have been investigated for their potential G-quadruplex binding. The compounds 3a, 3b and 5b display high affinity for telomeric and oncogenic G-quadruplexes. On the other hand, 5a only show high affinity f
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