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br Transporter based brain targeting nano DDS Drug delivery
2021-12-10
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 Anisomycin mg from harmful substances. Since only selected, neutral, lipophilic small
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Inhibitors against the proteasome a component of the ubiquit
2021-12-10
Inhibitors against the proteasome, a component of the ubiquitin-proteasome pathway that degrades cellular proteins, provide a new strategy for targeting the 26S proteasome [25]. Proteasome inhibitors can exhibit potent anti-cancer effects against different tumor SKL2001 and were shown to induce apo
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The orientation of the immobilized enzyme may
2021-12-10
The orientation of the immobilized enzyme may affect its activity and stability and therefore the final biocatalyst performance. Since proteins present areas more prone to unfolding in their surface or near to it [36], the immobilization through these areas may improve the final biocatalyst stabilit
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br Conflicts of interest br Acknowledgements
2021-12-10
Conflicts of interest Acknowledgements This research was supported by grants from National Research Foundation, Korea (NRF-2017RIDIA3B04033313) and Yeungnam University (216-A-061-042). Introduction Kluyveromyces lactis is a yeast that produces one of the ß-galactosidases (ß-gals) most wide
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Our paper also contributes to the large but hitherto inconcl
2021-12-10
Our paper also contributes to the large, but hitherto inconclusive literature that studies the effects of option-based compensation or convexity in compensation on corporate risk-taking policies. On the one hand, some studies document a positive relationship by showing that convexity increases lever
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Waldeck Weiermair et al demonstrated that in
2021-12-09
Waldeck-Weiermair et al. (2008) demonstrated that in endothelial cells, the activation of GPR55 by application of 10µM anandamide resulted in a marked increase of ERK1/2 phosphorylation that was evident 2min following drug activation and was sustained for up to 3h. Another example comes from our un
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Ning et al showed that LPC
2021-12-09
Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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Methods br Results br Discussion The current
2021-12-09
Methods Results Discussion The current study is the first to specifically investigate the role of hepatic GPR109A and GPR109B on HDL metabolism and response to niacin therapy. While niacin raises HDL-C levels in humans, it has been reported by others [20], [36] and confirmed by us here that n
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Apart from a few mutations which
2021-12-09
Apart from a few mutations, which affect intracellular and extracellular loops of hCRT-1, the mutations are primarily found in the hydrophobic core of the transporter; in fact, TMDs 7 and 8 appear to be a hot spot for mutations (Freissmuth et al., 2018). Several mutations are found at positions, whi
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It was previously proposed that
2021-12-09
It was previously proposed that glucagon acts in the liver, in which a signal is produced and relayed to the bromocriptine mesylate receptor via vagal nerves [8], [36], [37]. The concept that the liver is the primary target site was supported by the studies reporting that the glucagon receptor is l
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It is possible that regulation of adiposity and glucose
2021-12-09
It is possible that regulation of adiposity and glucose homeostasis by GIP are in part mediated by altering leptin levels and/or leptin signaling. However, we are unaware of reports that support this mechanism of action of GIP. In addition, leptin levels in GIP receptor knockout mice [12], [52] and
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Recently there are only a spot
2021-12-09
Recently, there are only a spot of FFA4 agonists reported in the literature (Fig. 1),13, 14, 15 and there is no selective FFA4 agonists have reached clinical trial for the treatment of T2DM. TUG-891, the first potent and selective FFA4 agonist, was developed in University of Southern Denmark as a wi
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br Introduction Farnesoid X receptor FXR is
2021-12-09
Introduction Farnesoid X receptor (FXR) is a bile PD 123319 ditrifluoroacetate regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporte
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However the clinical development of
2021-12-09
However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this recep
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Tedizolid Current studies have identified five orphan G prot
2021-12-09
Current studies have identified five orphan G protein-coupled receptors (GPCRs) that can be activated by free fatty acids (FFAs), GPR40, GPR41, GPR43, GPR84, and GPR120. Short-chain fatty acids (FAs) are specific agonists of GPR41 and GPR43 [21] and middle-chain FAs agonize GPR84 [22]. Long-chain FAs
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