• The fact that GSK recognition of its substrate

  2021-09-10

  

  The fact that GSK-3 recognition of its substrate involves pre-phosphorylation supports the rational for using synthetic phosphorylated peptides as substrate competitive inhibitors [57]. Phosphorylated peptides derived from the N-terminal pseudosubstrate sequence of GSK-3β were very weak inhibitors o

• MMAF receptor Ikaros utilizes chromatin remodeling to activa

  2021-09-10

  

  Ikaros utilizes MMAF receptor remodeling to activate or repress the transcription of its target genes (Su et al., 2004). Ikaros directly associates with histone deacetylases HDAC1 and HDAC2 and can recruit them to the upstream regulatory elements of its target genes (Kim et al., 1999, Koipally et a

• A number of anti diabetic drugs

  2021-09-09

  

  A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore

• Due to its unusually long pre

  2021-09-09

  

  Due to its unusually long pre-implantation period [20,21], the horse conceptus is entirely dependent on histotrophic nutrition for the first 40 days of gestation [22]. During the pre-implantation period, glucose transporters in the endometrium and conceptus membranes must deliver the glucose require

• Regulation of pancreatic and cell mass has been extensively

  2021-09-09

  

  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

• Recently multiple receptor agonists have been developed to t

  2021-09-09

  

  Recently, multiple receptor agonists have been developed to treat type II diabetes (Finan et al., 2013, Finan et al., 2015). We have tested novel dual GLP-1/GIP receptor agonists that showed good neuroprotective effects that are superior to single GLP-1 analogues (Cao et al., 2016, Jalewa et al., 20

• SNL in rats led to upregulated

  2021-09-09

  

  SNL in rats led to upregulated Panx1 mRNA and protein level in DRG but not in spinal cord, and immunostaining revealed increased Panx1 in DRG neurons [50]. Although it was not emphasized, Panx1 labeling in SGCs was also increased in this pain model. Intrathecal injection of Panx1 blockers or Panx1-s

• In this study it was demonstrated that also

  2021-09-09

  

  In this study it was demonstrated that also in mice chronically exposed to CS, lung inflammation persists after SC and is associated with a progressive alveolar loss and remodeling of respiratory tract, characterized by the onset of bronchial and bronchiolar GCM and peribronchiolar fibrosis. Persist

• The inhibitory activities of the compounds with the modifica

  2021-09-09

  

  The inhibitory activities of the compounds with the modification of the amino group against human liver FBPase are summarized in . Replacement of the amino group of with hydrophobic substituent such as a methyl group () led to a substantial loss of activity (IC=995nM). Similarly, replacement with h

• br Acknowledgements The authors have no

  2021-09-09

  

  Acknowledgements The authors have no ethical conflicts to disclose. The authors have no conflicts of interest to declare. This work was funded by the Research Council of Lithuania. Introduction This paper studies whether there is a causal influence of the risk-taking incentives provided by op

• Conflicting data concerning the involvement of H

  2021-09-09

  

  Conflicting data concerning the involvement of H2R on glycaemia has also arisen. Its antagonism was reported to decrease [35], not affect [36], [37] and increase [38], [39] Cy5 TSA levels. In comparison, the clinical experience with antipsychotic drugs generated clearer evidence for the involvement

• sh4 The occurrence of naturally HCV

  2021-09-09

  

  The occurrence of naturally HCV NS3 resistance-associated substitutions (RAS) affects virological outcome of DAA-based combination therapies [14], [15], [16], [17], [18], [19]. For the majority of NS3 protease inhibitors the frequency of natural occurrence of single RASs in HCV genotype 1-infected p

• Accessibility and physico chemical features of

  2021-09-08

  

  Accessibility and physico-chemical features of cysteine residues define their redox-reactivity and the 3-dimensional structure of GSNOR allows to identifying such surface-exposed, redox-sensitive cysteine residues. GSNOR crystal structures are available from human (Protein Data Bank code: 1MP0), tom

• Based on the results of compound appeared

  2021-09-08

  

  Based on the results of , SCF, murine recombinant protein appeared to have the best overall profile, so our efforts were then devoted to using 5-(-propyl)pyrimidine as the right-hand nitrogen attachment to optimize the R group of (). Analog was synthesized using the reaction conditions from , while

• We started our investigation by evaluating the impact

  2021-09-08

  

  We started our investigation by evaluating the impact of changes to the piperidine moiety of (). As demonstrated with morpholine and piperazine , attenuation of nitrogen basicity resulted in complete loss of activity, suggesting that a basic heterocyclic nitrogen is important for potent inhibition

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