• The present study chose the fdh gene the homolog of

  2022-01-21

  

  The present study chose the fdh gene, the homolog of mammalian GSNOR, to generate UAS-fdh and fdh double-stranded RNA interference (ds-RNAi) transgenic Drosophila. These transgenic models were used to study the effect of GSNOR activity modulation on visual learning and memory and to explore the poss

• We first set out to identify the minimum pharmacophore

  2022-01-20

  

  We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc

• Based on work from our labs with mGlu

  2022-01-20

  

  Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]

• Uracil DNA glycosylase UDG is a highly conserved damage

  2022-01-20

  

  Uracil-DNA glycosylase (UDG) is a highly conserved damage repair enzyme which can specifically recognize and excise uracil residue within the DNA sequences and actuate the DNA Bezafibrate excision repair (BER) pathway which keeps the maintenance of genomic integrity and stability [[21], [22], [23]]

• br Regulation of Glu transporters The pivotal role

  2022-01-20

  

  Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino Bikinin synthesis calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include tr

• The biological actions of ghrelin are mainly due to

  2022-01-20

  

  The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept

• br Secretase in inflammatory diseases Secretase appears to

  2022-01-20

  

  γ-Secretase in inflammatory diseases γ-Secretase appears to play a more important role than previously recognized in inflammatory diseases. Studies have shown that mice partially deficient in PS genes (PS1+/− PS2−/−) develop an immune system deficit in late adulthood, such as ulcerated skin or a

• br Materials and methods br Results

  2022-01-20

  

  Materials and methods Results Discussion G-quadruplex structures are extensively studied for its role in central dogma of molecular biology viz. replication problems leading to chromosomal translocations [20], [21], transcriptional inhibition [32] and alternative splicing and translational

• VS strategies have been building momentum in G drug

  2022-01-20

  

  VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com

• The highest metabolic stability observed for

  2022-01-20

  

  The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou

• Our paper also contributes to

  2022-01-20

  

  Our paper also contributes to the large, but hitherto inconclusive literature that studies the effects of option-based compensation or convexity in compensation on corporate risk-taking policies. On the one hand, some studies document a positive relationship by showing that convexity increases lever

• A large body of evidence supports a contribution of the

  2022-01-20

  

  A large body of evidence supports a contribution of the endocannabinoid (eCB) system in the regulation of stress and emotional behavior (Gorzalka and Hill, 2011, Hill and Patel, 2013, Morena et al., 2016). General findings from this work indicate that eCB anandamide signaling is critical for bufferi

• Recent findings of us suggest that compounds that inhibit bo

  2022-01-20

  

  Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that

• EZH interaction with HADC and HDAC through

  2022-01-20

  

  EZH2 interaction with HADC1 and HDAC2 through the EED subunit is known to recruit histone deacetylases [113,114]. Given that PRC2-mediated repression of transcription may be partly dependent on the function of HDACs in specific cell contexts [115], the leukemia cell treatment with hydroxamic EIPA a

• br Discussion The aim of the

  2022-01-20

  

  Discussion The aim of the present study was to extend the list of ASIC ligands and to check if histamine receptors ligands can also affect ASICs. The novel finding is that not only histamine but also thioperamide, 1-metylhistamine and Nα-methylhistamine are active ASIC1a potentiators, while other

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