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Since obesity appears to impact leptin and adiponectin
2023-04-17

Since obesity appears to impact leptin and adiponectin levels in opposite manners, several studies have suggested that the serum adiponectin/leptin ratio may be a key parameter in indicating the relative risk of postmenopausal breast cancer (Ollberding et al, 2013, Cleary et al, 2009). Therapeutic s
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In addition unconventional mechanisms of internalization
2023-04-17

In addition, unconventional mechanisms of internalization cannot be ignored. It is generally believed that the conventional homologous internalization of a GPCR depends on the activation of G proteins, since GRK activation requires the pre-activation of G proteins (Fig. 2). Feng et al. demonstrated
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Not all secondary metabolites or natural products can
2023-04-14

Not all secondary metabolites or natural products can be fully synthesized due to their very complex structures that are too difficult and expensive on industrial scale. Hence, there is an urgent need to search for alternative remedies as naturally occurring biologically active secondary metabolites
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br Acknowledgements br Introduction Microbial enzymes have g
2023-04-14

Acknowledgements Introduction Microbial enzymes have gained interest for their widespread uses in industries and medicine owing to their stability, catalytic activity, and ease of production and optimization than plant and animal enzymes (Singh et al., 2016). Microbial aminopeptidases (amino-a
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Introduction Rapeseed oil production is very
2023-04-14

Introduction Rapeseed oil production is very important not only because of its application in food industry, but also in petrochemical branch. Additionally, post-extraction meal and bagasse from oilseed rape are important sources of proteins in animal feedstuffs production. Oilseed rape (Brassica n
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br Materials and methods br Results Table
2023-04-14

Materials and methods Results Table 1 presents the metabolic phenotype of obese minipigs. After 60 d of HFHS feeding, minipigs not only showed an increased body weight (+45%), but also a perturbed opiod receptors homeostasis, with higher insulin levels (about +2-fold), HOMA-IR (+5.5-fold), and
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br Mortality and morbidity Alzheimer s disease
2023-04-14

Mortality and morbidity Alzheimer's disease is officially listed as the sixth-leading cause of death in the United States [208]. It is the fifth-leading cause of death for those age 65 and older [198]. However, it meclozine may cause even more deaths than official sources recognize. Alzheimer's i
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The excellent potencies selectivities and improved
2023-04-14

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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interleukins br Materials and methods br Results br Discussi
2023-04-14

Materials and methods Results Discussion Conclusions These studies provide important mechanistic insights to explain the long-established physiological observation that obese adipose tissue has higher rates of basal lipolysis. Increased lipolysis contributes to increased hepatic interleu
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We have previously shown that the antinociceptive effect
2023-04-14

We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific 9-cis-Retinoic Acid receptor blockade or activation (Rojas-Corrales et al.,
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It is worth mentioning that cordycepin as
2023-04-14

It is worth mentioning that cordycepin, as an adenosine analogue, is structurally similar to adenosine. A previous study has shown that the anti-apoptotic effects of cordycepin are partially dependent on the activation of A1R [16], and cordycepin increases theta waves power density via nonspecific a
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br Conflict of interest br Acknowledgments This work was
2023-04-14

Conflict of interest Acknowledgments This work was supported by research grant [PR26/20326] from Santander Bank/UCM. The authors would like to thank Miguel Capo, Professor of Toxicology from the Universidad Complutense de Madrid, for his counseling during the preparation of the present work.
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The consensus amino acid recognition sequence for p substrat
2023-04-14

The consensus amino adefovir mg recognition sequence for p38α substrates is (Ser/Thr)Pro (Cuadrado and Nebreda, 2010), typically assisted by upstream docking motifs (Remenyi et al, 2005, Sharrocks et al, 2000). P450c17 has 32 Ser and 25 Thr residues, of which only Thr 341 and Ser 427 are immediatel
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In this paper we describe the formation of
2023-04-14

In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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In conclusion we have designed and synthesized
2023-04-14

In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative pr
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