• Methyllycaconitine citrate The fact that GSK recognition of

  2022-04-14

  

  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

• GPR belongs to the G protein coupled

  2022-04-14

  

  GPR84 belongs to the G protein-coupled receptor family, and it was first identified from human peripheral blood neutrophils [,]. GPR84 is now considered to be a member of receptor for medium chain fatty gstp1-1 (MCFA) with carbon chain lengths of 9–14 []. GPR84 is mainly expressed in bone marrow, s

• The lactic acid receptor HCA is primarily expressed

  2022-04-14

  

  The lactic ghrelin receptor receptor HCA1 is primarily expressed in white and brown adipocytes 11, 12, 17, 18 (Table 1). Only relatively low expression levels of HCA1 have been described in several other tissues 16, 19, and it is not clear whether this is due to the presence of adipocytes in these

• In recent large clinical studies AIM HIGH

  2022-04-14

  

  In recent large clinical studies, AIM-HIGH and HPS2-THRIVE, the additional treatment of nicotinic MM-102 to statin-based LDL-C lowering therapy did not decrease the major vascular events on the patients who had atherosclerotic vascular diseases [43,44]. In the AIM-HIGH study, the secondary analysis

• The activation of the ERK pathway participates

  2022-04-14

  

  The activation of the ERK pathway participates in the transmission of pain signaling by sensitizing primary afferents (Ji et al., 2009, Lai et al., 2011). Thus, the blockade of ERK activation in the primary sensory SEW 2871 can reduce the mechanical hypersensitivity and the thermal hypersensitivity

• In summary we discovered azaindole substituted hydroxypyrido

  2022-04-14

  

  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

• The results obtained through in vitro

  2022-04-14

  

  The results obtained through in vitro, in vivo and in silico corroborated with those presented by other works and indicate that CpMutY is involved in oxidative damage repair in this organism. In this regard, MutY conservation in evolutionarily distant bacteria suggests that this protein plays an imp

• To test our refinement protocol we considered a benchmark

  2022-04-14

  

  To test our refinement protocol, we considered a benchmark set of 12 N-linked glycan-containing protein structures determined by X-ray crystallography at resolutions ranging between 1.9 Å and 3.5 Å and comprising a total of 133 glycan units. We identified four incorrect anomeric configurations and 2

• The typical pharmacophore for GPR agonists contains four par

  2022-04-14

  

  The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors

• Limitations of our study are the following we

  2022-04-14

  

  Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we

• Also a large number of small molecules

  2022-04-13

  

  Also a large number of small molecules are potent G-quadruplex ligands that exhibit anti-proliferative activity in cells [39,48]. Several small molecules, for example cyclic naphthalene diimide derivative [43], cationic porphyrins [2,[49], [50], [51], [52]] and pentaheteroaryls [53], quinacridines [

• chemicals informative post G quadruplex structures can be re

  2022-04-13

  

  G-quadruplex structures can be resolved by helicases. Consistently, many helicases are aberrantly expressed in cancer chemicals informative post [47]. In this study, we correlated HOXC10 expression with that of all helicases using a microarray dataset derived from 759 breast cancer patients [36] an

• Till date the first line treatment of T DM

  2022-04-13

  

  Till date, the first line treatment of T2DM is oral metformin followed by oral sulfonylureas, dipeptidyl peptidase-IV-inhibitors, and TZDs. As the disease progresses, injectable glucagon-like peptide-I analogues or ultimately insulin become necessary to maintain glycaemic control. Despite the establ

• br Introduction In addition to glucose which is the foremost

  2022-04-13

  

  Introduction In addition to glucose, which is the foremost stimulator of insulin secretion in beta-cells, other nutrients such as free fatty acids (also called non-esterified fatty acids, NEFA) contribute to glucose-stimulated insulin secretion (GSIS). Glucose triggers the processes leading to in

• p2y inhibitor A great number of proteins entering the nucleu

  2022-04-13

  

  A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous

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