• Potential platelet related mechanisms that

  2022-07-18

  

  Potential platelet-related mechanisms that might explain an augmented risk of MI in dabigatran treated patients have been investigated: Enhanced platelet reactivity is known to be associated with the risk of MI (Mangiacapra et al., 2018) and catalytically active thrombin is a potent stimulus to indu

• In C elegans KDM A appears

  2022-07-18

  

  In C. elegans, KDM4A appears to be involved in H3K36me3 reduction on the X chromosome, suggesting that this protein has a relevant role in germ cell development (Figure 2A) (47). In addition, in HeLa cells, KDM4A is associated with the repression of the achaete-scute complex homologue 2 (ASCL2) gene

• MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl q

  2022-07-18

  

  MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr

• MCB-613 br Materials and methods br Results

  2022-07-18

  

  Materials and methods Results Discussion Directly modulating specific target proteins and signaling pathways with small-molecule drugs or agonistic MCB-613 is widely used for cancer metastasis therapies [[39], [40], [41]]. ANXA7 acts as a metastasis suppressor in prostate cancer. However,

• br Materials and methods br Results br

  2022-07-16

  

  Materials and methods Results Discussion Main results obtained in this work are presented in Table 1 and can be summarized as follows: 1) AEA inhibits FcεRI receptor-induced degranulation with the participation of CB2 and GPR55 receptors by a PTX-insensitive mechanism; 2) AEA does not block

• br The methyl aspartate receptor NMDAr hypofunction hypothes

  2022-07-16

  

  The -methyl--aspartate receptor (NMDAr) hypofunction hypothesis of schizophrenia correlates disease symptomology with glutamatergic neurotransmission dysfunction., , , Therefore, inhibition of glycine transporter 1 (GlyT1) to elevate synaptic levels of glycine and potentiate NMDAr signaling is a p

• Then the seven complexes GLOI indomethacin GLOI zomepirac

  2022-07-16

  

  Then the seven complexes (GLOI-indomethacin, GLOI-zomepirac, GLOI-fenoprofen, and GLOI-ketoprofen, GLOI-tolmetin GLOI-curcumin, and GLOI-bisdemethoxycurcumin) were energy-minimized to remove unfavorable steric strain relative to the force field adopted. Further MD simulations were carried out based

• br Acknowledgments This work was supported

  2022-07-16

  

  Acknowledgments This work was supported by the Russian Foundation for Basic Research [grant number 16-04-00205], The Russian Science Foundation [grant number 16-15-00235], Czech Academy of Sciences [grant number RVO 61388963], and the Technology Agency of the Czech Republic [grant number TE010200

• To study the effects of GPR

  2022-07-16

  

  To study the effects of GPR40 at the whole-animal level, GPR40 mice have been generated in two different genetic backgrounds [18], [19]. GPR40 mice from both backgrounds were apparently healthy with no overt signs of metabolic or other abnormalities. As expected, pancreatic islets taken from GPR40 m

• If some of the experimentally determined

  2022-07-16

  

  If some of the experimentally determined tRNAGlu identity elements are unique to E. coli, then there also must be some unique phylum-specific residues in the corresponding GluRS (E. coli in particular, and proteobacteria in general) as well. In this paper we focus on identifying such residues in E.

• Regulation of pancreatic and cell mass has been extensively

  2022-07-16

  

  Regulation of pancreatic α and β cell mass has been extensively studied and hotly debated, due to potential therapeutic implications. Early claims of Angptl8 as “betatrophin” and Angptl4 as a regulator of glucagon secretion and α cell proliferation (Yi et al., 2013, Ben-Zvi et al., 2015) have not st

• br Materials and methods br Results br Discussion Prior stud

  2022-07-16

  

  Materials and methods Results Discussion Prior studies established that Notch signaling regulates the differentiation of hair cells and supporting cells during inner ear development (reviewed in Kiernan (2013)). Notch signaling is a multistep process that requires the interaction between a

• The focused set of additional pyrazole analogs

  2022-07-16

  

  The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro

• There are additional implications of subunit alterations in

  2022-07-16

  

  There are additional implications of α2-subunit alterations in the hippocampus. P has anticonvulsant activity (Herzog, 1995, Herzog et al., 1997, Herzog et al., 2012, Reddy et al., 2001, Reddy, 2010). These actions result from the metabolic conversion of P to GABA-A receptor-modulating, antiseizure

• VS strategies have been building momentum in G drug discover

  2022-07-16

  

  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

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