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dopamine antagonist drugs Materials and methods Construction
2019-11-18
Materials and methods Construction of the Chk-YB-1b-Neo vector. Approximately 107 plaques from a chicken genomic library established in EMBL3 vector (Clontech Palo Alto, CA) was screened and one clone containing a 12kb insert was selected. Digestion of this clone with SalI and EcoRI restriction enz
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One possible pitfall of using EPAC activators in the
2019-11-18
One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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b ng mg While showing that deletion of EP maintains femur bo
2019-11-18
While showing that deletion of EP1 maintains femur bone volume fraction and trabecular bone parameters during aging, perhaps more importantly we have also demonstrated that increased initial BV/TV in EP1 is protective against OVX-induced bone loss. That is, while mice lose an approximately equal pe
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To identify and characterize new possible molecular targets
2019-11-18
To identify and characterize new possible molecular targets, the mechanisms of various kinds of TCDD toxicities that occur by abnormal regulation in the downstream of AhR signals have been studied (Yoshioka et al., 2011). Experimental evidence has revealed that prostanoids (i.e., prostaglandins and
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br Results br Discussion Repair by NHEJ implicitly
2019-11-18
Results Discussion Repair by NHEJ implicitly requires the pairing together of broken chromosome ends. A complex of Ku, XRCC4, DNA ligase IV, and XLF (PEC) is necessary and sufficient for this purpose (Reid et al., 2015). Here, we describe dynamic changes in this complex that are triggered by d
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AAG has a broad substrate specificity
2019-11-18
AAG has a broad substrate specificity and besides 3-methyladenine can excise other altered purine residues, such as the minor lesions hypoxanthine and 1, N6-ethenoadenine from DNA. AAG initially activates these neutral base lesions by protonation of the base to allow for general Tamoxifen receptor c
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As part of a program to
2019-11-18
As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substit
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br Results br Discussion Cell responds to
2019-11-16
Results Discussion Cell responds to fluctuating environmental factors by activating a set of compensatory mechanisms including changes in the lipid profile. Compensatory reactions occurring in membranes in response to phosphate deprivation include replacement of phospholipids by phosphorus-fre
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We first confirmed LPS induction of markers
2019-11-16
We first confirmed LPS-induction of markers known to induce NF-κB signaling in Caco2BB cells, as established for numerous other cell types [31]. We initially selected this approach to monitor NF-κB activation instead of directly monitoring p65 as it is technically straightforward and provides both u
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Given the potency enhancing effect of the butyl group
2019-11-16
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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DGK is a key enzyme in glucose uptake in skeletal
2019-11-16
DGKδ is a key enzyme in glucose uptake in skeletal muscle. Chibalin et al. demonstrated that a decrease in DGKδ expression increases the severity of type 2 diabetes [20]. Additionally, DGKδ expression was increased in people who exhibited enhanced insulin sensitivity after exercise training [56]. Fr
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Besides by substrate and product KSTDs may
2019-11-16
Besides by substrate and product, Δ1-KSTDs may also be inhibited by other steroids. N. simplex ATCC 6946 Δ1-KSTD was strongly inhibited non-competitively by dicortinone (60), a steroidal dimer, and by bis-1-dehydrodicortinone, with values of 0.7 and 0.75 μM, respectively. This enzyme was also inhibi
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We found that both DDR and DDR ECD increased
2019-11-16
We found that both DDR1 and DDR2 ECD increased matrix mineralization as compared to native cells, with the effect of DDR2 ECD being more prominent. Both soluble (DDR2/ECD) and membrane-bound DDR2 ECD (DDR2/-KD), when compared to wild-type cells, induced larger mineral deposits. In this regard, a rec
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As the principal receptors for regulating the inflammatory p
2019-11-16
As the principal receptors for regulating the inflammatory process in mammals, CXCR1 and CXCR2 have an important role in regulating the trafficking of phagocytes such as neutrophils, monocytes and macrophages (Viola and Luster, 2008). The evidence gathered to date from fish studies are in agreement
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The most important cytotoxic lesion formed by the nitrogen m
2019-11-16
The most important cytotoxic lesion formed by the nitrogen mustards is generally considered to be the DNA–DNA interstrand cross-link 12, 13. DNA–DNA interstrand cross-links are thought to exert their cytotoxic effects by inhibiting DNA duplex strand separation, progression of the jnk inhibitor fork
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