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CID 755673 After the synthesis of methylsulfonyl or tetrazol
2022-02-10
After the synthesis of methylsulfonyl or tetrazole surrogate derivatives, compounds synthesized by introducing hydrogen, fluoro, and methyl groups into the head group of GPR119 agonists were synthesized. Compounds – were synthesized by reacting hydroxybenzaldehyde with fluorine, hydrogen, or a methy
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Molecular properties as well as metabolic stability in rat a
2022-02-10
Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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br Brief overview of the glutamate system and rationale for
2022-02-10
Brief overview of the glutamate system and rationale for targeting the glycine site of NMDARs In the central nervous system (CNS), glutamate is the major excitatory neurotransmitter and works in concert with gamma-aminobutyric MMP-2 Inhibitor I (GABA), the primary inhibitory neurotransmitter. To
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Increased expression of Glut is detected in a number
2022-02-10
Increased expression of Glut1 is detected in a number of cancer types including lung [7], brain [8], bladder [9], cervical [10], colorectal [11], esophageal [12], hepatocellular [13], head and neck [14], gastric [15], ovarian [16], renal cell [17], pancreatic [18], thyroid [19] and breast [20]. Over
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br Introduction The mammalian skin
2022-02-09
Introduction The mammalian skin forms the largest organ of the body and includes a network of cutaneous nerves, cells of the immune system, and mediators of the neuro-endocrine axis (Theoharides et al., 2016). Analogous to the hypothalamic-pituitary-adrenal axis, neuropeptides and their receptors
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A comparison of our results with literature data on the
2022-02-09
A comparison of our results with literature data on the action of pregnane and androstane steroids on the functional activity of NMDAR, GABAAR and GlyR enables us to draw the following conclusions. First, androstane steroids (with no substituents at C-17) at a concentration up to 50 μM do not affect
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Michiel S van der Heijden had
2022-02-09
Michiel S. van der Heijden had full access to all apigenin australia data in the study and takes responsibility for the integrity of the data and the accuracy of the data analysis. Wang, Sustic, de Oliveira, van den Heuvel, Bernards, van der Heijden. Wang, Sustic, de Oliveira, van de Ven. Wang
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FFAs are essential nutritional molecules that can also
2022-02-09
FFAs are essential nutritional molecules that can also modulate numerous cellular functions. Fatty Piceatannol receptor derivatives like prostaglandins, leukotrienes lysophosphatidic acid, spinhgosine-1-phosphate and others are well documented to carry out signal transduction via G-protein coupled
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The Hippo pathway has been well established as
2022-02-09
The Hippo pathway has been well established as a tumor suppressor pathway and is involved in many diverse biologic processes including cell growth, cell death, and organ size control in organisms, ranging from Drosophila to mammals [4]. Central to this pathway is a kinase cascade in which the Ste20-
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br Materials and methods br Results br Discussion
2022-02-09
Materials and methods Results Discussion Protein degradation plays a vital role in nearly all cellular processes, nearly 5% of genes are dedicated to the control of protein stability [31], [32]. The ubiquitin-proteasome system (UPS) represents the major way for degradation of proteins, wher
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Accumulating evidence suggests that the NGF family of
2022-02-09
Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, SB273005 derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37]. BDNF knockout mi
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Overall while cART has significantly prolonged life and amel
2022-02-09
Overall, while cART has significantly prolonged life and ameliorated HIV-associated disease, HIV infection of the CNS still induces a number of cognitive, behavioral and motor symptoms, along with substantial neuropathology. Data show that the inflammatory processes driving neurological disease pers
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Histamine H and H receptor
2022-02-09
Histamine H2 and H3 receptor expression is altered in the S-Adenosylhomocysteine of Hdc mice (Chepkova et al, 2012, Fitzsimons and et al, 2001). Because these mice lack HA, expression of HA receptors might be thought to be irrelevant. This is not the case in Hdc heterozygotes, however, or in patient
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GSK dimethylpiperidin yl butoxy phenyl piperidine carbonyl n
2022-02-09
GSK-835726 (3-[4-[4-[4-[4-(3,3-dimethylpiperidin-1-yl)butoxy]phenyl]piperidine-1-carbonyl]naphthalen-1-yl]propanoic acid) is a dual H1/H3 receptor antagonist with the potential to be used in allergic rhinitis. Likewise GSK-1004723, the drug-likeness criteria have not been passed by this drug candida
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br Conclusion br Conflict of
2022-02-09
Conclusion Conflict of interest Introduction The human epithelial receptor 2 (HER2 or erbb2) is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases that act through the EGF signaling cascade [1,2]. Approximately 20% of breast cancers overexpress HER2
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