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The present studies show that despite the
2021-09-08

The present studies show that, despite the high level of GSTP1-1 achieved in transfected cells, GSTP1-1 expression has no effect on sensitivities to the cytotoxicities of the oxazaphosphorines 4-OH-CP, 4-OOH-CP, and maf in MCF7 beta 2 adrenergic receptor (Fig. 4). The failure of GSTP1-1 to augment r
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As part of their ongoing effort in the field Kalypsis
2021-09-08

As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile nisoldipine sale derivatives
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Interestingly mGlu and mGlu receptors differ notably
2021-09-08

Interestingly, mGlu2 and mGlu3 receptors differ notably by their cellular distribution. Whereas mGlu2 receptors are mostly neuronal, mGlu3 receptors are expressed both in glia and in neurons. In neurons, mGlu3 receptors are present at the post-synapse and in presynaptic elements (Tamaru et al., 2001
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Recently unimolecular multi functional peptides that combine
2021-09-08

Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with TPCA-1 and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and weight lo
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The eradication of agonist activity
2021-09-08

The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary hdac inhibitors as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagoniz
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However ghrelin has a short half life of min
2021-09-08

However, ghrelin has a short half-life of 15–20 min, because it is a natural peptide containing 28-amino acids, its clinical usefulness as a therapeutic agent may be limited (Mosińska et al., 2017; Vestergaard et al., 2007). Hence, many efforts have been made to elucidate the smallest segment of ghr
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For the two KO models CX and CX
2021-09-08

For the two KO models (CX30 and CX43), fluorescence recovery is almost always best fitted with a 2-component exponential (Fig. 6A and D). Statistical analysis of the parameters (Table 1) shows that in both cases the two time scales and the fraction of recovery associated with the fast intracellular
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NO has been shown to be necessary for long term
2021-09-08

NO has been shown to be necessary for long-term potentiation (LTP) of GABAergic neurons in the amygdala (Lange et al., 2012), the hippocampus (Zhuo et al., 1993), the ventral tegmental area (VTA) (Nugent et al., 2009), and the spinal cord (Fenselau et al., 2011). NO is also known to increase GABA re
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The Hippo pathway has been
2021-09-08

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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To evaluate the role of increased FPPS expression in paclita
2021-09-08

To evaluate the role of increased FPPS expression in paclitaxel-treated cells, we investigated the effects of FPPS on 74 9 sale progression. DNA content analysis showed that the number of cells accumulating in the G/M phase increased in a dose-dependent manner in paclitaxel-treated cells (A and B),
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Biliary tract cancers BTC are
2021-09-07

Biliary tract cancers (BTC) are categorized into intrahepatic, perihilar, extrahepatic BTC (or cholangiocarcinoma) as well as gallbladder cancer (GBC). Although the incidence of BTC is low in developed countries (3% of gastrointestinal cancers), BTC is the second most common primary liver tumor afte
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br GPR GPR has been described
2021-09-07

GPR55 GPR55 has been described as a type 3 cannabinoid receptor due to its ability to detect endocannabinoids and may play a role in the endocannabinoid lipid sensing system [28]. GPR55 is activated by both cannabinoid endogenous agoinsts (endocannabinoids) and non-cannabinoids fatty acids namely
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ML133 HCl The lactic acid receptor HCA is primarily expresse
2021-09-07

The lactic ML133 HCl receptor HCA1 is primarily expressed in white and brown adipocytes 11, 12, 17, 18 (Table 1). Only relatively low expression levels of HCA1 have been described in several other tissues 16, 19, and it is not clear whether this is due to the presence of adipocytes in these tissues
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adefovir Ning et al showed that LPC appeared to
2021-09-07

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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To apply the recently developed
2021-09-07

To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the ion channel and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this end, th
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