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Through a large scale phylogenetic analysis of UDG superfami
2022-07-29

Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 Sulforhodamine 101 can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are present in
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br Acknowledgement This work was supported in part by
2022-07-29

Acknowledgement This work was supported in part by grants from the Ministerio de Economía y Competitividad from Spain (BFU2011-23034). Introduction The glutamate hypothesis of schizophrenia emerged from observations in the 1960s that phencyclidine and similar psychotomimetic agents produce sc
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br Experimental br Results br
2022-07-29

Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,
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br Xenobiotics and the Glucocorticoid
2022-07-29

Xenobiotics and the Glucocorticoid Receptor Conclusion Transparency document Acknowledgements The author wishes to thank Professor Wilhelm Engström from the Swedish University of Agricultural Sciences (Department of Biomedical Sciences and Veterinary Public Health) for his proof reading
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Various strategies have been pursued in the
2022-07-29

Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino Y 134 substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such as e.g. Pro3(GI
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The observed increase in macroscopic conductance could be du
2022-07-29

The observed increase in macroscopic conductance could be due to a left shift in the open state probability vs. voltage curve for the high-activity state causing an increase in the open state probability at all potentials. However, an increase of the apparent single channel conductance cannot be ent
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FXR agonists represent an attractive
2022-07-29

FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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Recently they reported an enyne chemotype agonist Fig with l
2022-07-29

Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral Busulfan (tmax=15min) and a decent pharmacokinetic profile, a sa
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br Introduction The nature of chemotherapies is to relieve
2022-07-29

Introduction The nature of chemotherapies is to relieve the tumor burden of the patients by eliminating cancer estrone via inducing cell death, mostly regulated cell death represented by apoptosis [1,2]. Dozens of anticancer agents including clinically used ones kill cancer cells by promoting ap
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The results of our analysis of
2022-07-29

The results of our analysis of Fas alleles, Fas 670 A>G, FasL alleles, and FasL IVS2nt 124 A>G for cases and controls are shown in Table 2. For Fas 670, we found statistically significant differences between the two groups regarding the AA Fmoc-Gln(Trt)-OPfp (P=0.040) and GG/AG (P=0.040) as well as
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br Materials and methods br Results br Discussion In
2022-07-29

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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br Visualizing single synaptic vesicle
2022-07-29

Visualizing single synaptic vesicle PF-562271 at CNS synapses We visualized the dynamics of individual synaptic vesicles as they fuse and immediately before fusion at the mammalian conventional synapses for the first time (Midorikawa and Sakaba, 2015). We use a calyx of Held terminal, a large pr
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Here we report the kinetics of
2022-07-28

Here, we report the kinetics of inhibition of the MYST HAT family member KAT8 by MG149, and a calculation of the inhibitory constant Ki of MG149 for KAT8. The inhibition of HATs by MG149 could be correlated to inhibition of histone acetylation in murine PCLS upon MG149 treatment, as determined by a
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Anti apoptotic Bcl proteins have become attractive targets
2022-07-28

Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients w
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br Introduction Coat colors are determined by both genetics
2022-07-27

Introduction Coat colors are determined by both genetics and environment, especially genetics. The phenotype of coat color of animals depends on two types of melanin, black to brown eumelanin and yellow to reddish brown pheomelanin produced in mammalian melanocyte (Ito et al., 2000; Ito and Wakam
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