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The manuscript provides mechanistic insights into the suppre
2022-08-24
The manuscript provides mechanistic insights into the suppression of EGFR, BCRP, PKM2, and other cancer biomarkers in response to pharmacological inhibition of GPR55 with MNF and CID (Fig. 7). Firstly, inactivation of ERK has been previously demonstrated following treatment of PANC-1 Acridine Orange
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A few of the islet
2022-08-24
A few of the islet-specific proteins identified in the present study have previously been described in various contexts of pancreatic islets, i.e. PTPRN, SCG5, SCGN, SNAP25 and SNED1, validating the search algorithm applied and supporting the notion that also the novel proteins identified are indeed
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Several studies have proposed that high levels of
2022-08-24
Several studies have proposed that high levels of KYNA in the PMX 205 contribute to cognitive dysfunctions presented by patients who suffer from schizophrenia [30], [31], [32], [33]. Considering that: (i) KYNA is a known GPR35 agonist [2], (ii) cognitive impairments in patients with schizophrenia a
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Originally identified as a GPCR
2022-08-24
Originally identified as a GPCR upregulated on Burkitt lymphoma cells upon Epstein-Barr virus infection (Birkenbach et al., 1993), Ebi2 was later found to play critical roles in immunity by regulating the migration of activated glycogen synthase kinase to extrafollicular sites for early plasmablast
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PF 04418948 Additionally increased GLO gene expression prote
2022-08-24
Additionally, increased GLO1 gene expression, protein expression, and activity have been reported in a variety of cancers, including breast,22, 23, 24 pancreatic, melanoma, and prostate.27, 28, 29 Vince and Daluge proposed that inhibitors of GLO1 could serve as anti-tumor agents, by increasing conce
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In conclusion we demonstrated that
2022-08-24
In conclusion, we demonstrated that extrasynaptic glutamate could in situ affect the AA metabolism via brain CYPs. CYP1B1 and CYP2U1 genes in the astrocytes are the downstream genes of CREB, and the up-regulation of CYP1B1 and CYP2U1 expression by glutamate was due to the increases in phosphorylated
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k j and d were then submitted
2022-08-24
15k, 15j and 14d, were then submitted to metabolic stability studies in human and mouse liver microsomes and permeability test with Caco-2 cells (Table 7). 15k, 15j and 14d all retained excellent permeability (Papp value greater than 15.2 × 10−6 cm/s) and displayed modestly improved metabolic stabil
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Although it is mainly a
2022-08-24
Although it is mainly a glial protein, 5–10% of total GLT-1 represents a neuronal form located at presynaptic terminals, but its physiological role remains elusive (for discussion, see (Rimmele and Rosenberg, 2016)). Nevertheless, this amount might be significant since GLT-1 has been estimated to be
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The development of metabolic stable non peptidergic galanin
2022-08-23
The development of metabolic stable, non-peptidergic galanin agonists could be the basis to clinical diagnosis and treatment of tumors with high levels of galanin receptor expression like gliomas and pituitary tumors. As for gliomas, penetration of the blood brain barrier by the compounds might be p
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br Ethics approval br Availability of data and materials br
2022-08-23
Ethics approval Availability of data and materials Consent for publication Competing interests Authors contributions Introduction Glucose supply to tissues is maintained through a complex regulatory network mostly driven by the pancreatic hormones insulin and glucagon which control
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In summary the SAR of a series of phenylpropanoic
2022-08-23
In summary, the SAR of a series of phenylpropanoic acid-free fatty conotoxin receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust effic
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In recent years many studies have demonstrated that the
2022-08-23
In recent years, many studies have demonstrated that the release of endogenous FPR ligands can influence severe diseases associated with inflammation, including systemic inflammatory response syndrome (SIRS)20, 21 and cancers, such as glioblastoma as well as gastric and colorectal cancer 22, 23, 24.
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The Jumonji JmjC domain containing KDM
2022-08-22
The Jumonji (JmjC) domain-containing KDM family members can be clustered into seven subfamilies (KDM2 – KDM8). The KDM2 cluster catalyzes H3K36me2/me1 demethylation; in addition, KDM2B/JHDM1B/FBXL10 has been suggested to catalyze demethylation of H3K4me3 [3]. Cell culture studies support that KDM2 p
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Long non coding RNAs lncRNAs are a class of
2022-08-22
Long non-coding RNAs (lncRNAs) are a class of RNA transcripts which are over 200 nucleotides in length and not translated into proteins (Ponting et al., 2009). Recent studies showed that lncRNAs have been identified as crucial regulators of gene expression, chromatin remodeling, and cell cycle (Wahl
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br Experimental section The parts of chemicals
2022-08-22
Experimental section The parts of chemicals and regents, preparation of solutions, pre-treatment of the bare Au electrode, cell culture, cytotoxicity in vitro, cell imaging, characterizations, and electrochemical measurements are supplied in the S1 (See the Supplementary Information). The prepara
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