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Type diabetes mellitus is characterised
2022-04-12

Type 2 diabetes mellitus is characterised by two major features: peripheral insulin resistance and impaired insulin secretion from pancreatic beta iwp2 [1]. The condition occurs when the pancreatic beta cells are unable to compensate for increased insulin demand due to insulin resistance in periphe
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Herein we describe the design
2022-04-12

Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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Tetrazole is one of the most
2022-04-12

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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In summary PPARG and FFAR are connected in several ways
2022-04-12

In summary, PPARG and FFAR1 are connected in several ways, and the presented interaction is mechanistically reasonable. Additional investigations are required to elucidate the exact details of the underlying physiology. However, our findings are of immanent importance for the treatment of type 2 dia
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We sought to deduce the role of membrane
2022-04-11

We sought to deduce the role of membrane lipid determinants on endo- and exocytosis by applying a combination of metabolic (lipid) engineering approaches and biophysical methods, e.g. classical optical imaging technologies and high-resolution time-resolved patch-clamp/capacitance measurements. The l
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In humans mutations in KDM A KDM
2022-04-11

In humans, mutations in KDM5A, KDM5B, and KDM5C are found in patients with ID, implicating KDM5-regulated transcription in the development or activity of neuronal tissues (Vallianatos and Iwase, 2015). KDM5D is Y-linked, and its role in cognition remains uncharacterized. Mutations in KDM5C are the m
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Introduction Histamine Imidazolyl ethylamine is an important
2022-04-11

Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric rp gift card secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histamine exe
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According to the experimental data HKI preferentially
2022-04-11

According to the experimental data, HKI preferentially binds to the mitochondrial inter-membrane contact sites formed by ANT and VDAC [[5], [6], [7],27], mainly via the VDAC1 isoform [7,8]. These electrogenic contact sites allow application of a part of IMP to MOM by transferring phosphoryl groups f
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br Acknowledgments br Introduction Histone deacetylases HDAC
2022-04-11

Acknowledgments Introduction Histone deacetylases (HDACs) related to tumor suppressor genes have become promising targets for the treatment of cancer [1,2]. Under the normal physiological conditions, Histone acetyltransferases (HATs) and histone deacetylases (HDACs) together regulate the acety
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Since its development the HCV replicon system Lohmann et al
2022-04-11

Since its development, the HCV replicon system (Lohmann et al., 1999) has been a critical tool in the HCV antiviral discovery process (Gottwein et al., 2009, Imhof and Simmonds, 2010, Lohmann et al., 1999, Pietschmann et al., 2001, Imhof and Simmonds, 2010, Gottwein et al., 2009). The replicon assay
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br STAR Methods br Acknowledgments We thank Prof Y
2022-04-11

STAR★Methods Acknowledgments We thank Prof. Y. Tomari at the University of Tokyo for experimental advice and K. Hanada for technical assistance. This research was supported by Grants-in-Aid for Scientific Research on Innovative Areas “Nascent Chain Biology” (JP15H01548 and JP17H05677 to T.I. a
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br AURK Functions br Concluding
2022-04-11

AURK Functions Concluding Remarks The AURKs are crucial regulators of cell division; however, little is known about the mechanisms by which these kinases function in meiosis. Recent work has begun to chip away at the specific roles that each of the kinases play; however, as more is uncovered,
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Polyunsaturated fatty acid components of brain are
2022-04-11

Polyunsaturated fatty faah inhibitors components of brain are more prone to oxidative attack, an event called lipid peroxidation. Consistent with previous findings on neurotoxicity [58,59], colistin sulphate increased the level of MDA in the brain of rats. The elevated MDA, a consequence of overwhel
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Several compounds have been described in
2022-04-11

Several compounds have been described in the literature as inhibitors of the sGC. Among them, methylene blue and LY83583 () are not direct sGC inhibitors, but rather block cGMP formation by generating superoxide anion radicals that deactivate NO. Despite their extensive use in plethora of research s
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Signaling pathways that control the redox stress response in
2022-04-11

Signaling pathways that control the redox stress response in P. brasiliensis are poorly known, but in other dimorphic fungi, the involvement of MAPK is an important factor in this process [[13], [14], [15]]. For example, when alveolar macrophages are challenged with Aspergillus or Cryptococcus conid
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