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Several studies have shown that independently
2020-02-03
Several studies have shown that, independently of body-weight control, the central actions of leptin improve glycemic control in obese diabetic rat and mouse models [62]. For instance, restoration of OB-Rb expression in OB-Rb-deficient mice, and in particular in POMC neurons, was sufficient to norma
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PI K is a lipid kinase and
2020-02-03
PI3K is a lipid kinase and generates phosphatidylinositol-(3,4,5)-trisphosphate, which is a second messenger critical for the translocation of Akt to the cytoplasmic membrane. The phosphorylation of Ser473 Akt is important in the cell survival by regulating the eNOS among other targets (Dimmeler et
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Preliminary studies suggest that dimerization of the AT
2020-02-03
Preliminary studies suggest that dimerization of the AT1 receptor occurred during the biosynthesis in the endoplasmic reticulum before surface expression [27,40], which may explain the presenece of these MK-0752 before the addition of any ligand. Our results showed that the presence of Ang II did n
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br The classical ubiquitination pathway Ubiquitination is an
2020-02-03
The classical ubiquitination pathway Ubiquitination is an enzymatic process that involves the addition of an ubiquitin protein to a substrate that usually becomes inactivated followed by degradation in the proteasome; however, several other functions have also been described. For the discovery of
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br Results and discussion br Conclusion We
2020-02-03
Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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br Conformational properties of DGK br Interaction of DGK wi
2020-02-03
Conformational properties of DGKϵ Interaction of DGKϵ with its lipid substrate A major component of the interaction between DGKϵ and lipid bilayers is the insertion of the hydrophobic segment comprising residues 20–42 into the membrane, as discussed above. However, this is not the only interac
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Herein we explored by docking studies
2020-02-03
Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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Pulmonary fibroblasts can regulate the wound
2020-02-03
Pulmonary fibroblasts can regulate the wound healing process by secreting and processing extracellular matrix (ECM), chemokines, and cytokines. However, persistent and atypical fibroblast proliferation can result in ECM accumulation and may trigger the onset or development of pulmonary fibrosis [[17
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A series of monocarboxylated chalcones e g compounds and Fig
2020-02-03
A series of monocarboxylated chalcones (e.g. compounds 7 and 8, Fig. 2A) was previously identified as good CysLT1 antagonists [20], and none of them exhibited CysLT2 antagonistic activities (Supplementary Table S1). This study was consistent with reported result that CysLT2 3065 synthesis was not s
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We further examined our hypothesis that the activation of CR
2020-01-30
We further examined our hypothesis that the activation of CRF and CCK systems is responsible for the enhanced anxiety-like behavior induced by immobilization stress using two antagonists to block the expression of CRF1 and CCK2 receptors. It was found that CCK2 receptor antagonist CR2945 or CRF1 ant
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NMS-873 Our results on the acute
2020-01-30
Our results on the acute effects of THC on resting state NMS-873 function are in line with previous neuroimaging findings. Increased perfusion after THC administration in insular and prefrontal regions has previously been reported in smaller samples (Mathew et al., 1997, Mathew et al., 2002, van Hel
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Protein kinase casein kinase CK
2020-01-30
Protein kinase casein kinase 1 (CK1) comprises a family of highly related, constitutively active serine/threonine protein kinases (reviewed by [15]). CK1 is involved in controlling a wide variety of different cellular events including protein turnover [16], [17], nuclear import [18] and the cellular
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The repeat sequence TTAGGG of telomere could
2020-01-30
The repeat sequence “TTAGGG” of telomere could be directly recognized by TERF1. TERF1 is indispensable for the maintenance of telomere Z-IETD-FMK sale structure and integrity (Tan et al., 2017). Trf1 genetic depletion in vivo induces a persistent DNA damage response and telomere uncapping, which eff
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br Discussion Several DPP inhibitors are currently available
2020-01-29
Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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br Protein acetylation Several reports show that
2020-01-29
Protein acetylation Several reports show that MTX is able to induce acetylation of histones and other proteins. Extensive studies have established that histone acetylation is primarily associated with gene activation. Acetylation occurs at lysine residues on the amino-terminal tail of the protein
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