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rgd peptide VS strategies have been building momentum
2021-12-03
VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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It is considered that activations of MMP and
2021-12-03
It is considered that activations of MMP-2 and MMP-9 are closely related to progression process of cancer cells, such as invasion and metastasis [22], [23]. In fibrosarcoma cells, GPR40 suppressed not only MMP-2 and MMP-9 activations, but also cell motile and invasive activities, suggesting GPR40 ne
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Studies have revealed that ferroptosis is non apoptotic
2021-12-03
Studies have revealed that ferroptosis is non-apoptotic and peroxidation-driven form of cell death that requires abundant and accessible cellular Fe2+, and thus, the balance of Fe2+ metabolism is of great significance in regulating the process of ferroptosis (Cao and Dixon, 2016; Xie et al., 2016; Y
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98 8 synthesis Wolf et al then proceed to interrogate the
2021-12-03
Wolf et al. (2016) then proceed to interrogate the mechanism by which NAG activates the NLRP3 inflammasome. When examining potential triggers previously implicated in NLRP3 activation, they found that both PGN and NAG trigger appearance of mitochondrial DNA (mtDNA) in the cytosol, which led them to
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br Conclusions and future perspectives br Declarations of
2021-12-03
Conclusions and future perspectives Declarations of interest Acknowledgements The authors thank Mrs. Kamala Pandey for the help in the preparation of this manuscript. This work was supported by NIH grants R01HL057531 and R01HL062147. Introduction Separation of short exons by long non-co
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Overall ABC transporters are hypothesised
2021-12-02
Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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It is an aspiring task to apply the glutamate biosensor
2021-12-02
It is an aspiring task to apply the glutamate biosensor for in vivo measurements in lactacystin tissue. Due to a relatively large size of the electrode used in this work, the biosensor fits only ex vivo applications. However, it is possible to apply platinum microelectrodes 50–100 μm in diameter for
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Tetrazole is one of the
2021-12-02
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 a
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Administration of a fructose rich diet to
2021-12-02
Administration of a fructose-rich diet to normal rats induces insulin resistance and impaired glucose tolerance or diabetes, depending on treatment duration [23]. We have shown that development of these abnormalities as well as fat deposit in liver, are effectively prevented by co-administration of
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Regulation of pancreatic and cell mass
2021-12-02
Regulation of pancreatic α and β cell mass has been extensively studied and hotly debated, due to potential therapeutic implications. Early claims of Angptl8 as “betatrophin” and Angptl4 as a regulator of glucagon secretion and α cell proliferation (Yi et al., 2013, Ben-Zvi et al., 2015) have not st
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Next we asked how a common activation marker of
2021-12-02
Next, we asked how a common activation marker of fibroblasts, Acta2, defined gene expression signatures in alveolar airspaces by using Acta2-mKO1 reporter mice (Fig. 2A). In the lungs of Acta2-mKO1 mice, mKO1 was expressed in smooth muscle cells and mesenchymal cells in egfr pathway (Fig. 2B). By s
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Based upon the present findings it is tempting
2021-12-02
Based upon the present findings, it is tempting to imagine that selective, and especially stable blood–brain barrier (BBB) penetrating GalR1 antagonists might be useful as drugs for acute suppression of appetite. While this may be possible, previous studies using nonspecific galanin antagonists yiel
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br Declaration of competing interests
2021-12-01
Declaration of competing interests Acknowledgements The authors wish to thank the Natural Science Foundation of Jiangsu Province (BK20171261), the project of outstanding scientific and technological innovation group of Jiangsu Province, the National Science Fund for Distinguished Young Scholar
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Bile acids BAs are detergent like amphipathic molecules synt
2021-12-01
Bile acids (BAs) are detergent-like amphipathic molecules synthesized from cholesterol in the liver, stored in the gallbladder, and released into the intestine after food intake in order to facilitate the full of of dietary lipids and liposoluble vitamins. BAs travel along the intestine and once in
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br Conclusions br Conflicts of interest br Funding The
2021-12-01
Conclusions Conflicts of interest Funding The research work was partially supported by National Science Center (Contract Grant Number: UMO-2015/19/B/NZ1/00332). Introduction Frusectose-1, 6-bisphosphatase (FBPase) has long been recognized as a potential therapeutic target for the treatm
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