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As a continuation of our search
2023-09-04
As a continuation of our search for a selective AChE radioligand bearing a meta-F substituted N-benzyl moiety, we designed and synthesized a novel meta-F-CP-118,954 analog along with a meta-18F-labeled form via diaryliodonium salt-based precursor (Fig. 1). For comparative purposes, we incorporate th
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Osteoblasts have been thought to be the major cell
2023-09-04
Osteoblasts have been thought to be the major cell type that expresses RANKL (Suda et al., 1999) which is a ligand for osteoprotegerin (OPG) and which functions as a key factor for osteoclast differentiation and activation. Recently, Nakashima and his colleagues (Nakashima et al., 2011) demonstrated
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It involves complementary and inflammatory system proteins m
2023-09-04
It involves complementary and inflammatory system proteins, mast cells, eosinophils, basophils, macrophages, natural killer (NK) cells and cytokines [1]. Innate immunity, not only include cells, but also barriers that defend the organism to the penetration of pathogenic agents [2]. Important mediat
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In our previous report we
2023-09-01
In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t
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Aurora A the polar kinase
2023-09-01
Aurora A the ’polar kinase’ is located at the centrosome and is required for its maturation, division, for the mitotic spindle assembly and entry into mitosis., Mutation or transcriptional silencing of Aurora A impairs centrosome maturation and separation, leads to mono/multipolar spindles, to dela
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Protein protein interaction networks are an important ingred
2023-09-01
Protein–protein interaction networks are an important ingredient for the system-level understanding of cellular processes. Such networks can be used for filtering and assessing functional genomics data and for providing an instinctive platform for annotating structural, functional and evolutionary p
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Here we investigate the ATM to ATR switch in
2023-09-01
Here, we investigate the ATM to ATR switch in normal human fibroblasts (82-6 cells) after irradiation with γ-rays, or high LET 56Fe and 28Si and moderate LET 16O particles. Our data provide important evidence of LET dependence on the transition of ATM to ATR as well as end resection at the sites of
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br Summary br Introduction With readily synthetic methods an
2023-09-01
Summary Introduction With readily synthetic methods and excellent chemical/physical characteristics, coumarins have received extensive attention and show great practical values in many fields, such as medicine discovery, dye chemistry, materials chemistry and so on [[1], [2], [3]]. Actually, o
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The excellent safety profile of solanezumab and
2023-09-01
The excellent safety profile of solanezumab and encouraging trends in the exploratory analyses in mild AD led to its inclusion in two secondary prevention trials, which are continuing in the hope that earlier intervention may yield more substantial benefit. The A4 study (NCT02008357) started in Febr
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Inhibition of autophagy has been shown to alleviate neuronal
2023-09-01
Inhibition of autophagy has been shown to alleviate neuronal damage after cerebral ischemia, both in cell culture and rodent models (Koike et al., 2008, Li et al., 2015, Wang et al., 2016, Zhang et al., 2014, Zheng et al., 2014). Therefore, blockage of autophagy is a potential target for prevention
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Various compounds have been designed
2023-09-01
Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic citco sale moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a po
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Interestingly intermittent high doses of AKT inhibitors have
2023-09-01
Interestingly, intermittent high doses of AKT inhibitors have been shown to be a more effective strategy both clinically and pre-clinically. High doses appear to be required for induction of apoptosis and intermittent schedules overcome the low therapeutic index of these compounds. This is particula
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APPL is highly expressed in pancreatic cells but
2023-09-01
APPL1 is highly expressed in pancreatic β cells, but its levels are significantly decreased in several mouse models of obesity and diabetes, including HFD-induced obese mice and db/db mice [6], [73], suggesting that the dysregulation of APPL1 may be associated with malfunction of the pancreas in obe
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cddo Derivatives of M that possess either
2023-09-01
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these cddo to maintain 5-HTR antagonist properties as (+)-M100907 was demonstrated to
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DMP 777 Since pyrrolopyrimidine dithiolanes and both display
2023-09-01
Since pyrrolopyrimidine dithiolanes and both displayed particularly excellent levels of ACK1 inhibition, these analogs were viewed as potential candidates for further investigation in tumor xenograft experiments. While in vitro metabolic studies indicated that pyrrolidine was predicted to be sign
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