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Obesity is one of the worldwide concerns with
2021-10-19

Obesity is one of the worldwide concerns, with high prevalence and adverse effects on human health and life expectancy. According to the World Health Organization (WHO), obesity is defined as abnormal or excessive fat accumulation in the body with body mass index (BMI) of 30 or more. Obesity increas
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Bile acids are the end products of cholesterol catabolism an
2021-10-19

Bile acids are the end products of cholesterol catabolism and have also been considered as hepatomitogens. Recently, Yap has been shown to be activated by the mevalonate pathway, which is essential for the biosynthesis of isoprenoids and downstream cholesterol and bile acids (Sorrentino et al., 2014
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Previous studies have shown that HER is also
2021-10-19

Previous studies have shown that HER2 is also involved in IL-6 expression and signaling. IL-6, HER2, and GP130, the beta-subunit of the IL-6 receptor (IL-6R), are physically associated and co-immunoprecipitate in response to IL-6 stimulation [1]. IL-6 induced HER2 clustering to the GP130 complex, le
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br Heme oxygenase inhibitors Historically the first class
2021-10-19

Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron HPF sale of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme for binding to the e
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84 9 synthesis Peripheral injury or disease induced
2021-10-19

Peripheral injury- or disease-induced alterations in synaptic efficacy occur not only at the first synapse made by the primary nociceptive afferents in the spinal dorsal horn but are also operational in several regions processing the sensorimotor as well as emotional-affective components of pain, su
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Herein in consider of the high similarity between GR
2021-10-19

Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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GLI proteins activate or repress
2021-10-18

GLI proteins activate or repress transcription of their target genes by binding to a similar sequence motif within a cis-regulatory module (CRM) (Hallikas and Taipale, 2006, Peterson et al., 2012). Transcriptional responses to the HH pathway can be elicited either by de-repression of GLI-R or in oth
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Acknowledgements br Introduction Alzheimer s disease AD is a
2021-10-18

Acknowledgements Introduction Alzheimer's disease (AD) is a devastating neurodegenerative disorder and the leading cause of dementia. There is currently no treatment available to slow or halt disease progression. The underlying mechanisms of AD on the cell and molecular levels are still not comp
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BDNF is intricately implicated in energy homeostasis Hamdouc
2021-10-18

BDNF is intricately implicated in energy homeostasis (Hamdouchi et al., 2016; Schwartz and Mobbs, 2012), regulation of mood (Sartorius et al., 2015) and adult neurogenesis (Taliaz et al., 2010; Waterhouse et al., 2012), our primary focus was to evaluate the effects of GPR40 stimulation on BDNF expre
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Potential roles for S P
2021-10-18

Potential roles for S1P in angiogenesis, cancer, and autoimmune diseases such as RA have been reported [73]. In RA synoviocytes, S1P has been shown to enhance expression of prostaglandin E2 (PGE2) and cyclooxygenase-2 (COX-2) in response to the pro-inflammatory cytokines, TNF-α and interleukin (IL)-
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Selected GSNOR inhibitors were assessed for potential off ta
2021-10-18

Selected GSNOR inhibitors were assessed for potential off-target activity with a panel of 54 transmembrane and soluble receptors, ion channels, and monoamine transporters. Off-target effects were estimated from the percent inhibition of receptor radio-ligand binding in the presence of 10μM of test c
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Human GPR hGPR was originally isolated in as an
2021-10-18

Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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In three independent groups identified GPR A
2021-10-18

In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niac
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br Discussion Agonist and antagonist action at the GluN
2021-10-18

Discussion Agonist and antagonist action at the GluN1/GluN3 DRB receptor is known to be complex [4], [10]. Recombinant GluN1/GluN3 receptors produce only small excitatory currents in response to glycine, likely because of a combination of activation via GluN3 and desensitization via GluN1 [2], [
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Growth hormone secretagogue receptor GHSR is a member
2021-10-18

Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s
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