• br Trifluoromethylketones This group of compounds

  2022-04-02

  

  Trifluoromethylketones This group of compounds was demonstrated to bind the zinc 7ACC2 receptor in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the core mot

• Most of the GSNOR inhibitors

  2022-04-02

  

  Most of the GSNOR inhibitors presented here were synthesized according to . The synthesis started from either commercially available ketones or the ketones prepared as described in the . In , condensation of ketone and 2-furanaldehyde provided intermediate in good yield. Furan ring opening of inte

• A number of in vivo studies have investigated the

  2022-04-02

  

  A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g

• Others demonstrated that Paneth cells maintain

  2022-04-02

  

  Others demonstrated that Paneth cells maintain stem cell function and crypt homeostasis by providing metabolic lactate to sustain the enhanced mitochondrial oxidative phosphorylation in the Lgr5+ ISCs (Rodriguez-Colman et al., 2017), which substantially agrees with our findings in this study. Furthe

• Acknowledgments This research was supported by the Korea Res

  2022-04-02

  

  Acknowledgments This research was supported by the Korea Research Institute of Chemical Technology (KRICT) funded by the Ministry of Science, ICT & Future Planning (KK1703-G00, KK1707-C05, SI1707-02, KK-1607-C09, and SKO1707C05) and a grant of the Korea Health Technology R&D Project through the Kor

• br Conclusion br Introduction The intracellularly

  2022-04-01

  

  Conclusion Introduction The intracellularly generated metabolite methylglyoxal (MG, 2-oxopropanal) acts as a potent electrophile causing irreparable cellular damage if allowed to build to cytotoxic concentrations [1], [2], [3], [4], [5], [6]. The glyoxalase (Glx) system is an enzyme couple cri

• In summary we discovered azaindole substituted hydroxypyrido

  2022-04-01

  

  In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that

• An alternative to the chemoenzymatic preparation of glycopro

  2022-04-01

  

  An alternative to the chemoenzymatic preparation of glycoproteins is the production through total chemical synthesis or semi-synthesis [2,3,]. Many successful glycoprotein syntheses are based on native chemical ligation (NCL) [11], a reaction where unprotected peptides and glycopeptides of any lengt

• In conclusion we demonstrated that

  2022-04-01

  

  In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 dpat sale results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network acts as “Cl− lo

• Given the proposed importance of conformational dynamics to

  2022-04-01

  

  Given the proposed importance of conformational dynamics to GCK's allosteric regulation, a number of biophysical methods have been utilized to probe the enzyme's dynamic structural landscape. Investigations into the mechanism of Angiotensin 1/2 (1-7) amide binding, using changes in the enzyme's int

• br Glucocorticosteroid receptor structure and

  2022-04-01

  

  Glucocorticosteroid receptor structure and function The gene encoding for the human GR is composed of 9 exons (Oakley and Cidlowski, 2011) and the translated protein is described as having 4 functional regions. The protein contains a highly conserved central DNA-binding domain (DBD) or C-domain,

• Until now various reports have demonstrated the therapeutic

  2022-04-01

  

  Until now, various reports have demonstrated the therapeutic potential of enzyme-resistant forms of GIP in experimental diabetic animal models , , . In essence, structural modifications performed at the Tyr residue in GIP generate analogues that are completely resistant to the actions of DPP-IV and

• Receptor tyrosine kinases RTKs consist of subfamilies

  2022-04-01

  

  Receptor tyrosine kinases (RTKs) consist of 20 subfamilies in humans, all of which share a common structure consisting of extracellular ligand-binding region, a single-pass transmembrane domain and an intracellular tyrosine kinase domain [2]. Binding of a growth factor to the ligand-binding domain r

• In conclusion our results showed that FFAR can

  2022-04-01

  

  In conclusion, our results showed that FFAR1 can mediate the effect of PIO in attenuating β-cell lipoapoptosis through anti-oxidative stress, which may be related to the activation of the PLCγ-ERK1/2-PPARγ pathway. Our study helps not only to distinguish the role played by FFAR1 in lipotoxicity, but

• Previous studies have shown that inhibition of

  2022-04-01

  

  Previous studies have shown that inhibition of voltage-gated Na+ MLN4924 has a reduced effect on GABAergic boutons compared with other neurotransmitter phenotypes,46, 47 and voltage-gated Na+ channel subtypes are differentially expressed in hippocampus. In addition, SV exocytosis evoked by elevated

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