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Tetrazole is one of the most commonly used bioisosteres for
2022-02-11

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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To assess whether this coupling mechanisms
2022-02-11

To assess whether this coupling mechanisms might operate also in a native system of untransfected cells, we select a cell line SH-SY5Y neuroblastoma that is known to express both the dopamine transporter and the M-currents (Jiang et al., 2004; Wickenden et al., 2008). These experiments were performe
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A high fat maternal diet during the pregestation period and
2022-02-11

A high-fat maternal diet during the pregestation period and extending throughout gestation (including the period of conception) has the propensity of affecting early embryonic development and placentation. Previous investigations have revealed that the preimplantation embryos are generally exposed t
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br Conflict of interest statement br Acknowledgements This
2022-02-11

Conflict of interest statement Acknowledgements This work was supported by the National Health and Medical Research Council of Australia (NHMRC) (project grants [1061044], [1065410] and [1126857], and NHMRC program grant [1055134]); P.M.S. and A.C. are NHMRC Principal and Senior Principal Rese
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br Conclusions br Introduction Bioinformatics analysis shows
2022-02-10

Conclusions Introduction Bioinformatics analysis shows that there are about 300,000 G-rich sequences in human genome if searching with the consensus sequence (G3+N1-7G3+N1-7G3+N1-7G3+) [1], and their localizations are non-random. These G-rich sequences always localize in functional regions, su
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Another lever to efficiently eradicate tumors including ovar
2022-02-10

Another lever to efficiently eradicate tumors including ovarian cancer might rely on their high addiction to iron [34]. In fact, ultrasmall silica-based nanoparticles, functionalized with melanoma-targeting peptide, efficiently triggered ferroptosis not only in cell culture but also in tumor bearing
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Trifluoromethyl ketones and fluorophosphates were the first
2022-02-10

Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated h
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Dysregulation of catecholaminergic neurotransmission particu
2022-02-10

Dysregulation of catecholaminergic neurotransmission, particularly the dopaminergic system, has long been correlated with the development of neuroinflammation and HAND. Studies specifically examining role of catecholamines in HIV pathogenesis, particularly focused on NeuroHIV, are relatively few. Ho
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br STAR Methods br Acknowledgments We
2022-02-10

STAR★Methods Acknowledgments We thank Emeritus Professor Chikashi Shimoda and Professor Taro Nakamura of the National BioResource Project/Yeast Genetic Resource Center (NBRP/YGRC) at Osaka City University (Osaka, Japan) for Schizosaccharomyces pombe meiotic cDNA library, yeast plasmids, yeast
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The finding that a peptide
2022-02-10

The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino etifoxine sale ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1 an
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Several named antagonist ligands have figured noticeably
2022-02-10

Several named antagonist ligands have figured noticeably in preclinical studies, with proved clear ability to release neurotransmitters and having efficacy in preclinical animal models. Consequently, this has encouraged ongoing research on improved agents with potency, selectivity, and better drug-l
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br STAR Methods br Acknowledgments
2022-02-10

STAR★Methods Acknowledgments We thank P. Adler, V. Riechmann, N. Tapon, E. Knust, the Vienna Drosophila RNAi Center, the Australian Drosophila Research Support Facility (www.ozdros.com), the Bloomington Drosophila Stock Center, and the Developmental Studies Hybridoma Bank for D. melanogaster s
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br Regulation of HO expression under conditions
2022-02-10

Regulation of HO-1 expression under conditions of ischemic cardiac damage Heart is a vital organ with high metabolic demand, rich in mitochondria and it is very vulnerable to oxidative damage [85]. Disruption in coronary blood flow following MI leads to hypoxia (a reduction in the amount of avail
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Cut proteins have five evolutionarily
2022-02-10

Cut proteins have five evolutionarily conserved domains. These include a homeodomain, three Cut repeats, and a coiled coil structure. The cut repeats, called CR1, CR2, and CR3, are composed of 70 amino acids, and, along with the homeodomain, are each capable of binding DNA. Mammalian cut proteins fu
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Activation of sGC induces the generation of
2022-02-10

Activation of sGC induces the generation of cyclic guanosine monophosphate (cGMP), phosphorylation of protein kinase G (PKG) and changes in activity of effector proteins such as phosphodiesterases (PDE), ion channels and ion pumps [43]. This pathway eventually leads to dilation of Beauvericin (bronc
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