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Our overall goal is to develop
2021-11-17
Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and
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Recent studies revealed that synthetic oligomeric A decrease
2021-11-17
Recent studies revealed that synthetic oligomeric Aβ1-42 decreased GLT-1 expression and promoted mislocalization of GLT-1 from the cell surface of primary astrocytes, leading to glutamate dyshomeostasis in synapses (Abdul et al., 2009, Scimemi et al., 2013). To address the cause for reduction of ast
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Young et al described the role of adenine
2021-11-17
Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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Herein in consider of the high similarity between GR HBP
2021-11-17
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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Taken together previous data suggest that ghrelin signaling
2021-11-17
Taken together, previous data suggest that ghrelin signaling is causally linked to alcohol use and may regulate alcohol seeking and consummatory behaviors [[66], [67], [68]]. As such, the ghrelin system may represent a therapeutic target for AUD. Here, we provide a narrative review of the existing l
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br Chemistry Analog has been previously reported by our
2021-11-17
Chemistry Analog 12 has been previously reported by our group. Experimental procedures for the synthesis and characterization of 13–32 are available in Scheme 1, Schemes S1–S9 and Table S1 in Supplementary data. Preparation of 30 and 31 is depicted in Scheme 1 as the representative example. Commo
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Some malignant human tumors cells also express
2021-11-17
Some malignant human tumors NSC 652287 sale also express FPRs and respond to bacterial or endogenous agonists by increased motility and growth. For instance, FPRs expressed by human gastric cancer cells, mediate epithelial–mesenchymal transition, cell proliferation, migration, and resistance to apo
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The minimal segment of the SIM appears to be a
2021-11-17
The minimal segment of the SIM appears to be a core of RSL3 synthesis residues, which frequently matches the consensus sequences ΨΨΨΨ, ΨxΨΨ, or ΨΨxΨ (where Ψ is V, I, or L and x is typically D, E, S, or T) [29,31,32]. In a subset of SIMs, this hydrophobic core is flanked by serine residues and a st
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More recently the JmjC domain histone H
2021-11-17
More recently, the JmjC domain histone H3K36 di-demethylase KDM2B/FBXL10 has also been shown to play an important role in definitive hematopoiesis [17]. Kdm2b is highly expressed in the HE, and its deletion (Tie2) caused embryonic lethality due to a precipitous drop in the number of hemogenic endoth
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There are several limitations in our study First
2021-11-17
There are several limitations in our study. First, only the naturally occurring resistance-associated mutations in patients coinfected with HIV/HCV Protease Inhibitor Cocktail (100X in DMSO, EDTA plus) 1b were analyzed. The result was only applicable to HCV genotype 1b, but not the HCV genotype 1a
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The endocytic inhibitors MDC and CPZ
2021-11-17
The endocytic inhibitors MDC and CPZ and dynamin GTPase blocker (dynamin mutant) have been shown to significantly decrease the intracellular accumulation of cGMP. Moreover, earlier reports suggested that G-protein-coupled receptor (GPCRs) continue to signal by generating cAMP throughout internalizat
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Modulation of the cannabinoid system has been reported to ex
2021-11-16
Modulation of the cannabinoid system has been reported to exert anti-parkinsonian properties through different mechanisms. On one hand, cannabinoids have neuroprotective properties in different rodent models of PD, both through a CB1/CB2 receptor-independent mechanism (Lastres-Becker et al., 2005) a
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It is an aspiring task to apply the glutamate
2021-11-16
It is an aspiring task to apply the glutamate biosensor for in vivo measurements in Trimidox tissue. Due to a relatively large size of the electrode used in this work, the biosensor fits only ex vivo applications. However, it is possible to apply platinum microelectrodes 50–100 μm in diameter for t
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Recent studies suggested that non coding RNAs participate in
2021-11-16
Recent studies suggested that non-coding RNAs participate in the modulation of Glut1 expression. For instance, the lncRNA NBR2-Glut1 axis was suggested to modulate cancer cell sensitivity to phenformin [37]. In renal carcinoma, miR-1291 is involved in the regulation of Glut1 Kasugamycin hydrochlorid
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A number of GCK activators for treating T D have
2021-11-16
A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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