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br Introduction The amino acid glycine
2022-05-13

Introduction The amino Lck Inhibitor glycine functions as a neurotransmitter in the vertebrate central nervous system: as an inhibitory neurotransmitter and as a co-agonist of the NMDA-subtype of excitatory glutamatergic receptors (Eulenburg et al., 2005). Under a current hypothesis that schizop
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As GLO is the major detoxification system of reactive dicarb
2022-05-13

As GLO1 is the major detoxification system of reactive dicarbonyls, it is plausible that differences in production and activity of the enzyme influences AGE production and the development and/or modulation of diabetic neuropathy. Glo1 exists as a copy number variant (CNV) in many inbred strains mice
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Introduction The brain contains abundant fatty
2022-05-13

Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in dev
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The simple carrier model for
2022-05-13

The simple carrier model for GLUT1 transport activity proposes that the transporter alternates between an outward facing glucose binding site and an inward, cytoplasmic, facing glucose binding site. Cytochalasin B is an endofacial inhibitor and appears to preferentially bind to the open, inward faci
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Moreover we examined inhibition of GLI
2022-05-13

Moreover, we examined inhibition of GLI-mediated mRNA expression by 1. Colubrinic Capecitabine (1) inhibited the mRNA production of PTCH in PANC1 cells in the dose-dependent manner. This result clearly shows 1 inhibits GLI-mediated transcription (Fig. 6). Discussion In this study, we identified
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br Materials and methods br Chemical synthesis
2022-05-12

Materials and methods Chemical synthesis Declaration of interest Acknowledgements This research was supported by a grant from the National Institute for General Medicine to K.W.M. (GM 58448) and by the Department of Anesthesia, Critical Care & Pain Medicine at Massachusetts General Hospi
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Despite their undisputed importance however FPR receptors ar
2022-05-12

Despite their undisputed importance, however, FPR receptors are not in the limelight of GPCR-related research (for review [12] and references therein). We, therefore, draw attention to this GPCR receptor family, in order to re-initiate FPR-related research, particularly in the light of biased agonis
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Methods Very briefly PLA polymeric
2022-05-12

Methods Very briefly: PLA polymeric nanoparticles as well as liposomes were synthesized and loaded with three different FGFR inhibitors. The encapsulation efficiency, average size, PDI, zeta potential, stability and release kinetics were investigated. The most promising formulations were biological
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While earlier reports on ferroptosis did not clarify mitocho
2022-05-12

While earlier reports on ferroptosis did not clarify mitochondrial damage and consequent death signaling in this paradigm of oxidative death, evidence from recent studies in neuronal systems strongly suggested a mechanistic link between enhanced lipid peroxide formation and loss of mitochondrial int
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By measuring the accumulation of unprenylated Rap a
2022-05-12

By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult
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In addition to indoles two additional structural
2022-05-12

In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic hbv side chain to prepare compound (). The extension of the chain was expected
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Numerous strategies of cardiomyocyte protection are effectiv
2022-05-12

Numerous strategies of cardiomyocyte protection are effective in preclinical, animal models and in small clinical trials. However, most have disappointed in large clinical trials [4,5]. Failures of cyclosporine and post-conditioning to mitigate reperfusion injury are recent examples [[6], [7], [8]].
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Currently the computational chemical biology has been
2022-05-12

Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug
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Our results show that deletion of the
2022-05-12

Our results show that deletion of the first loop of Obg does not abolish the augmentation of the GTPase activity of CgtAvc, revealing that the first loop is mainly responsible for the anchoring of the protein in the 50S and the transient interaction with ribosome is enough for augmentation of GTPase
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We first investigated the influence of the
2022-05-11

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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