• As disclosed in our preceding paper medicinal chemistry SAR

  2022-06-05

  

  As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, GSK2126458 lacks an es

• Acute in vivo experiments were performed in normoglycemic SV

  2022-06-05

  

  Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding MK 571 receptor control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg pro

• Digoxin FFAR is highly expressed not only

  2022-06-05

  

  FFAR1 is highly expressed not only in β cells but also in α Digoxin (Segerstolpe et al., 2016), which gives the interesting perspective that 20-HETE may function both as an autocrine and as a paracrine regulator of islet cell function (Figure 1A), i.e., acting in symphony with the many other intra-

• Besides its established insulinotropic actions GIP has

  2022-06-05

  

  Besides its established insulinotropic actions, GIP has been shown to possess other direct beneficial effects on the beta cell, including stimulation of growth, differentiation, proliferation and survival.21, 22, 23 It has also been shown to stimulate proinsulin gene transcription and translation. M

• Ligand selectivity may directly be related to the conformati

  2022-06-02

  

  Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This

• Methods and materials Escherichia coli JM

  2022-06-02

  

  Methods and materials Escherichia coli JM109(DE3) 7340 receptor containing a derivative plasmid of pUCmod that encodes E. coli FDPS (IspA) previously described by Schmidt-Dannert and co-workers [22] were grown in LB media containing 150μg/mL of ampilicin. E. coli was grown directly from stock cell

• In spite of decades of research the mechanisms of

  2022-06-02

  

  In spite of decades of research the mechanisms of SV endocytosis and recycling remain controversial. Accumulating evidence suggests that SV endocytosis occurs by more than one mechanism (e.g. clathrin-independent endocytosis, clathrin-mediated endocytosis, bulk endocytosis; reviewed in (Dittman and

• Aberrant expression of HKII may be a required feature for

  2022-06-02

  

  Aberrant expression of HKII may be a required feature for cancer development and progression. Overexpression of HKII has been reported in tumor tissues of cancer patients with liver [9], ovary [8], [24] and larynx [25]. The clinical significance of HKII in cancer was noted as overexpression of HKII

• br Materials and methods br Results To examine the

  2022-06-02

  

  Materials and methods Results To examine the time and organ specific effect of normal photoperiod and dark environment on the chemokine receptor of different SlHXKs and on the enzyme activities, these parameters were determined in different leaf positions of tomato plants. Under control condi

• Similarly towards the acylsulfamoyl benzoxaboroles the boron

  2022-06-02

  

  Similarly, towards the 5-acylsulfamoyl benzoxaboroles, the boronate intermediate was prepared according to , while the boronate , an intermediate towards 4-acylsulfamoyl benzoxaboroles, was prepared according to . The sulfonamides and used in the synthesis were made from the starting sulfonyl chl

• Furthermore colistin induced mitochondrial dysfunction

  2022-06-02

  

  Furthermore, colistin induced mitochondrial dysfunction in mouse central nervous system and chicken neurons, axonal degeneration and demyelization of mice sciatic nerves [16,17,19]. Interestingly, mitochondrial dysfunction is a key determinant of neurodegeneration [20,21]. Also, it accumulates amino

• The NF B family of transcription factors

  2022-06-02

  

  The NF-κB family of transcription factors is involved in acquisition of resistance to anticancer drugs as well as to apoptosis. NF-κB-mediated mdr1 gene upregulation is part of the anti-apoptotic protection mechanism of proximal tubule (PT) fccp against cadmium-induced oxidative stress and apoptosis

• Conjugated BAs via S PR also

  2022-06-02

  

  Conjugated BAs via S1PR2 also activate ERK1/2- and AKT-signaling pathways leading to the growth and invasion of cholangiocarcinoma cells. The role of conjugated BAs via S1PR2 to regulate apoptosis or cancer progression remains to be dissected. Nevertheless, there is no doubt that the composition of

• GlyRs are members of the superfamily of Cys loop

  2022-06-01

  

  GlyRs are members of the superfamily of Cys-loop receptors (CLRs) [3]. They form postsynaptic pentameric receptor complexes of α1 and β subunits anchored via the scaffolding protein gephyrin [4]. GlyRs are composed of several domains with the large N-terminal extracellular domain (ECD) important for

• br Dysregulation of glutamate transporter

  2022-06-01

  

  Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi

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