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OS has a key role in the pathogenesis of micro
2021-12-29
OS has a key role in the pathogenesis of micro- and macrovascular diabetic complications [3]. There is now convincing evidence that the enzymes that generate ROS and gasotransmitters, such as nitric oxide (NO) and CO, are redox regulated at both the transcription and activity levels, and are also i
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br Clinical development of anti NASH
2021-12-29
Clinical development of anti-NASH drug therapies The current understanding of NASH pathogenesis has led to broad efforts to target several features of the disease, alone or in combination, even in the absence of liver-guided therapies. Therefore, drug development in NASH is a rapidly changing fie
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br Conclusion br Acknowledgments br Introduction
2021-12-29
Conclusion Acknowledgments Introduction The gyloxalase pathway is a well-conserved antioxidant defense system found in all cells of the body [1], [2], [3], [4]. The glyoxalase pathway facilitates the neutralization of highly reactive and oxidizing dicarbonyl molecules, with methylglyoxal (M
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br Transporter based brain targeting nano DDS Drug delivery
2021-12-29
Transporter-based brain-targeting nano-DDS Drug delivery to the central nervous system (CNS) is still challenging due to the bloodbrain barrier (BBB)53., 54.. The BBB is a natural defense barrier protecting the Viroptic from harmful substances. Since only selected, neutral, lipophilic small mole
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In respect of clinical development Takeda has pioneered the
2021-12-29
In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul
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Congenital Gcgr mice exhibit increased hepatic Fgf expressio
2021-12-29
Congenital Gcgr mice exhibit increased hepatic Fgf21 expression and circulating FGF21 levels. Previous studies by other investigators demonstrated that neutralization of circulating FGF21 with specific Demethoxycurcumin impairs glucose control in these mice [6]. In addition, the FGF21 analog LY2405
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br The potential of EPA Ffar signaling as a novel
2021-12-28
The potential of EPA-Ffar4 signaling as a novel intervention for HFpEF Conclusions and future directions Optimization of ω3-PUFA/EPA-therapy based upon titration to achieve therapeutic levels: A pressing clinical challenge is to continue to define the benefit of ω3-PUFA/EPA-therapy. Recent ana
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Our results demonstrated that most of the HUA rings incubate
2021-12-28
Our results demonstrated that most of the HUA rings incubated with 100 μM TBT do not have the capacity to contract in the presence of 5-HT or exhibit very low contractions in comparison to the control. Only 23.3% of the HUA rings were able to contract. These results seem to indicate that there may b
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blue nitro The CNP pGC B cGMP pathway has
2021-12-28
The CNP/pGC-B/cGMP pathway has been reported to be potent inhibitor of fibrosis, from an intrinsic compensatory protective response as well as a therapeutic in cardiorenal injury and disease states [6,12,13,22,30]. Indeed, fibrosis is a progressive process leading to increased risk for morbidity and
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coelenterazine As a result of the capability of modulating t
2021-12-28
As a result of the capability of modulating the dynamic changes and rearrangement of cytoskeletons, the Rho GTPases, in which RhoA, Cdc42 and Rac1 are best-characterized, have been highlighted as significant contributors for orchestrating neuronal development (Duman et al., 2015, Heasman and Ridley,
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Compounds and were synthesized according to The synthesis
2021-12-28
Compounds –, , and were synthesized according to . The synthesis of compounds – commences with C-acylation of 3,4-dibromothiophene to the form ketone , the ring closure to form the ester , Hiyama cross-coupling or Suzki cross-coupling to produce , or to , respectively. Compound was produced from
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With the administration of OM fatty acids it has previously
2021-12-28
With the administration of OM3 fatty acids, it has previously been shown that the activation of GPR120 is linked to the secretion and circulating levels of the adipokine adiponectin [123] promoting anti-inflammation (downregulation of NF-κB) and insulin sensitivity [124]. Interestingly, Nrf2 also de
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br Endogenous lipids as SLC transporter
2021-12-28
Endogenous lipids as SLC6 transporter modulators Lipids constitute part of the environment in which membrane-embedded transporters operate [62]. Endogenous lipids can act as inhibitory ligands [63] or functionally important components of the membrane that impart changes in transporter structure [
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In glioma or glial derived primary brain
2021-12-28
In glioma, or glial-derived primary NCT-502 tumors, as in other cancers, glutathione is an important survival mechanism. Glioma cells are dependent upon SXC-mediated cystine uptake for viability, as they require intracellular cystine/cysteine for GSH synthesis (Ogunrinu and Sontheimer, 2010, Sonthei
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Acknowledgments br Introduction Type diabetes mellitus T
2021-12-28
Acknowledgments Introduction Type 2 diabetes mellitus (T2DM) is caused by relative insulin deficiency or insulin resistance in peripheral tissues. The clinical management of T2DM is achieved by controlling blood glucose levels. Current therapies available for treatment of T2DM include biguanides
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