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The first natural product described
2023-11-10
The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic ARL 67156 trisodium salt from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long time b
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Because LTs are proved to mediate
2023-11-10
Because LTs are proved to mediate multiple biological and pathological responses in various disease states, the 5-LO biosynthetic pathway producing LTs from AA have been the target of drug discovery efforts for over two decades. As observed from literature, a pile of research efforts has been direct
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In addition to the above mentioned synaptic
2023-11-10
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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The molecular mechanisms involved in
2023-11-10
The molecular mechanisms involved in the pathogenesis of cholestatic pruritus remain unknown [45], [46]. Indeed, there has been an enormous effort at understanding the etiology of PBC-related pruritus, including work at the cellular and molecular level, but such efforts have not been translated into
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br Apelin Discovered in apelin was initially identified as t
2023-11-10
Apelin Discovered in 1998, apelin was initially identified as the sole endogenous ligand for the APJ receptor (Tatemoto et al., 1998). Apelin-77 (pre-pro-apelin) is the precursor for various pharmacologically active apelin isoforms (e.g. apelin-12, -13, -17 and 36), and it shares 75–95% sequence
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In conclusion our data highlight that variable anti oxidativ
2023-11-10
In conclusion, our data highlight that variable anti-oxidative 2272 could be released through peptic hydrolysis of CMP fractions. Although casein hydrolysates produced a larger number of peptides (Table 1) with variable antioxidant capacities, all the peptides from whey hydrolysate exhibited higher
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Ambient levels of ppm ozone were recorded
2023-11-09
Ambient levels of 0.2ppm ozone were recorded during a recent 2017 weather event in Texas, United States (EPA, 2007). This concentration or higher levels have been used in several human clinical studies during intermittent exercise (Miller et al., 2016c). Although ozone concentration of 0.8ppm used i
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Adiponectin is an adipokine whose
2023-11-09
Adiponectin is an adipokine whose circulating level is depleted in a number of metabolic diseases including insulin resistance, diabetes and cancer (Khan et al., 2015, Singh et al., 2014a, Singh et al., 2014b, Yamauchi et al., 2014). Despite its importance in health and pathophysiology, adiponectin
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AdK as an important upstream regulator of
2023-11-09
AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inhi
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It has been recognized for decades that neurons in the
2023-11-09
It has been recognized for decades that neurons in the mammalian central nervous system may release both a fast-acting, typically amino acid derived neurotransmitter such as glutamate or GABA, and a second peptidergic neuromodulatory molecule such as neuropeptide Y, substance P, or cholecystokinin.
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Osteoblasts have been thought to be the major cell type
2023-11-09
Osteoblasts have been thought to be the major cell type that expresses RANKL (Suda et al., 1999) which is a ligand for osteoprotegerin (OPG) and which functions as a key factor for osteoclast differentiation and activation. Recently, Nakashima and his colleagues (Nakashima et al., 2011) demonstrated
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In the U S surveillance of ACEs has garnered traction
2023-11-09
In the U.S., surveillance of ACEs has garnered traction at the state level through administration of the ACE Optional Module in CDC’s Behavioral Risk Factor Surveillance System (BRFSS) (Centers for Disease Control & Prevention, 2003). Since 2009, select states have implemented the ACEs optional modu
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br Regulation and pharmacology of
2023-11-09
Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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The most potent compounds within the current series
2023-11-09
The most potent compounds within the current series of compounds were therefore , , , , and , with Fmoc-Phe-OPfp possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-OHas
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br Experimental br Results and discussion br Conclusion
2023-11-09
Experimental Results and discussion Conclusion Acknowledgments This work is supported by the National Basic Research Program of China (973 Program 2016YFA0201201 and 2013CB932702), a project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions (PAP
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