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To the best of our
2022-02-10

To the best of our knowledge, this is the first study to examine functional GSTO1‐1 activity in the cornea. Therefore, comparative data for human or animals is not available. Moreover, we observed the nonspecific degradation of the GSTO1‐1 substrate 4NPG via an unknown mechanism, which was correcte
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The isoenzyme hGSTP is an attractive
2022-02-10

The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t
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The physiological role of lactate induced antilipolytic effe
2022-02-10

The physiological role of lactate-induced antilipolytic effects is less clear. It has been speculated that GPR81 mediates the inhibition of lipolysis during intensive exercise, a condition which results in high systemic lactate plasma concentrations 9, 10. Owing to oxygen shortage resulting from int
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Acknowledgments Financial support from the National Natural
2022-02-10

Acknowledgments Financial support from the National Natural Science Foundation of China (81730094, 81473262 and 81573299) is gratefully acknowledged. This project was also supported by the “111 Project” from the Ministry of Education of China, the State Administration of Foreign Expert Affairs of C
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Thus synthesized thienopyrimidine derivatives were evaluated
2022-02-10

Thus synthesized thienopyrimidine derivatives were evaluated in vitro for GPR119 agonistic activity, and the results are summarized in , , . First, we fixed the 4-methylsulfonylphenyl substituent at the R position on the thienopyrimidine ring, and derivatized at the R position. As shown in , and s
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Recently a receptor for nicotinic
2022-02-10

Recently, a receptor for nicotinic acid, named GPR109A (also known as HM74a in man or PUMA-G in the mouse) has been identified (Lorenzen et al., 2001, Lorenzen et al., 2002, Soga et al., 2003, Tunaru et al., 2003, Wise et al., 2003). This receptor, a member of the 7 transmembrane G-protein coupled f
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br Materials and methods br Contributors br Acknowledgements
2022-02-09

Materials and methods Contributors Acknowledgements This work was funded by the Ministry of Human Resources and Social Security, Shanxi Province [(2010)255], by a Shanxi Scholarship Council of China, and supported by a grant from the Alzheimer Society UK. The authors declare no conflict of
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br Results br Discussion Our studies highlight MUFAs as key
2022-02-09

Results Discussion Our studies highlight MUFAs as key lipid modulators of both non-apoptotic and apoptotic cell death. Recent studies show that a more mesenchymal phenotype, de-differentiation, and acquired resistance to targeted inhibitors, can all promote a ferroptosis-sensitive cell state (
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br Role of ferroptosis in PD Pathological progression of
2022-02-09

Role of ferroptosis in PD Pathological progression of PD displays features that may facilitate ferroptosis induction such as elevated iron in the SNpc [49], [57], [88], [122], depleted GSH [194] and lipid peroxidation [51]. Iron chelation has been shown to mitigate the motor impairment in mouse m
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Whether ferroptosis specific inhibitor could promotes
2022-02-09

Whether ferroptosis specific inhibitor could promotes spinal cord repair is a question worth to explore. A potent and stable ferroptosis specific inhibitor is essential for in vivo study. Ferrostatin-1 (Fer-1), the first generation of ferroptosis inhibitor, was shown actively suppressing ferroptosis
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A nitric oxide donor glyceryl trinitrite and the substrate
2022-02-09

A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri
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Unlike the bacterial SRP pathway for which the
2022-02-09

Unlike the bacterial SRP pathway for which the energetics, kinetics, and structure of almost every intermediate have been characterized, multiple questions remain for the GET pathway (Figure 3, marked with ‘?’). First, the targeting pathway demands distinct activities of Get3 before and after substr
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Dendritic damage and loss of synaptic connections correlate
2022-02-09

Dendritic damage and loss of synaptic connections correlate with cognitive decline in HAND patients. Synapse loss induced by HIV proteins occurs early and via a different signaling pathway from that leading to neuronal death (Kim et al., 2008), suggesting that synapse loss might be a mechanism to re
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GnRH ant have been designed to obtain
2022-02-09

GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p
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The findings in mice were echoed in the
2022-02-08

The findings in mice were echoed in the human studies, in which the effects of higher doses of LY3298178 caused greater weight loss than the selective GLP-1RA dulaglutide. In patients with T2DM, LY3298176 demonstrated meaningful weight loss after only four weeks of treatment. This was consistent wit
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