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For example nM MTX markedly
2021-07-27
For example, 200nM MTX markedly stimulates the differentiation of the monocytic U937 VKGILS-NH2 australia [39], but only 10nM MTX is sufficient for the inhibition of clonogenicity in the ALL and APL cell lines [22]. Furthermore, an even lower concentration of MTX (2nM) selectively induces the expre
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br Introduction Acylglycerol acyltransferases AGATs are
2021-07-27
Introduction Acylglycerol acyltransferases (AGATs) are predominantly responsible for triglyceride synthesis in the body, via two major pathways: the glycerol phosphate (GP) pathway (Kennedy, 1957) and the monoacylglycerol (MG) pathway (see Coleman and Lee, 2004, Yen et al., 2008). The final step
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Our recent discovery M P H R A
2021-07-27
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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br P Y receptor structure
2021-07-26
P2Y receptor structure Pharmacology Several subtype selective compounds have been developed in recent years (Jacobson and Müller, 2016; Rafehi and Müller, 2018). These compounds are helpful tools for analyzing the roles of P2Y receptor subtypes in physiology and pathophysiology. The present ar
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Injurious effects of cigarette smoke CS
2021-07-26
Injurious effects of cigarette smoke (CS) on human health are progressively being acknowledged both in animal and human studies. CS is a highly complex mixture that contains substantive amounts of toxic oxidants, nitric oxide, organic compounds, free radicals and microbial cell components including
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The enzyme cyclooxygenase COX or prostaglandin endoperoxide
2021-07-26
The enzyme cyclooxygenase (COX) or prostaglandin endoperoxide H synthase (PGHS) is the key enzyme in the conversion of arachidonic Spadin (AA) into prostaglandins (PGs) [1]. In 1991, researchers found that there were two isoforms of this enzyme called COX-1 and COX-2 with independent genes and diffe
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br Conclusions In the present
2021-07-26
Conclusions In the present study, decreased AChE and increased BuChE and BeChE activities were observed in greenhouse workers relative to control subjects; however, these changes cannot be related to OP exposure but likely to pesticide-induced oxidative stress or a mild inflammatory state. The in
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Prenylation may turn a flavonoid
2021-07-26
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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EP receptors belong to the
2021-07-26
EP1–4 receptors belong to the family of G protein-coupled receptor (GPCR). Trafficking events such as externalization, internalization, recycling and degradation dynamically regulate GPCR cell surface density. A fast-rate of internalization and degradation reduces GPCR surface density to desensitize
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PET CT static images of F CJ acquired
2021-07-26
PET/CT static images of F-CJ-042794 acquired at 1h p.i. from LNCaP tumour-bearing mice with/without co-injection of non-radioactive CJ-042794 (50μg) are shown in . The LNCaP tumours were clearly visualized in PET images with a moderate tumour-to-background contrast. High radioactivity accumulation w
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Kinetic isotope effects KIEs inform on
2021-07-26
Kinetic isotope effects (KIEs) inform on bond vibrational changes between the ground state (GS) and TS of a chemical reaction and remain one of the most powerful experimental techniques for interrogating TS structure. KIEs on enzyme reactions measured by the internal pkm2 of labeled substrates repo
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The significance of the difference in the
2021-07-26
The significance of the difference in the DDR2 binding specificity towards fibrillar and non-fibrillar collagens is not understood, but may imply differences in biological responses when chondrocytes bind to different collagens in the growth plate. Investigations by Labrador et al. (2001) have shown
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The EGFR belongs to the ErbB family of
2021-07-26
The EGFR belongs to the ErbB family of receptor tyrosine kinases (RTKs), comprised of four members: EGFR (ErbB1, HER1), HER2 (ErbB2), HER3 (ErbB3) and HER4 (ErbB4) [24]. HER receptors are activated by a group of epidermal growth factor (EGF) ligands and undergo homo- or hetero-dimerization during th
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Because of the complexity of DNA
2021-07-26
Because of the complexity of DNA damage and its repair, several pathways are candidates in HN2-induced DPC repair. Considering the 23kDa molecular weight of MGMT, NER may be ineffective for MGMT-adduct removal. This presumption is supported by that the mRNA level of ERCC1, a core gene in NER pathway
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Bax channel blocker Methylation of histone tails is importan
2021-07-26
Methylation of histone tails is important in regulating Bax channel blocker structure and transcription. Methylation occurs at arginine and at mono-, di- or tri-methylated lysine residues. The reversibility of histone methylation was recently revealed by the identification of two histone demethylas
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