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Here we performed TEM and AFM
2021-09-29

Here, we performed TEM and AFM imaging to study APE1–DNA interactions. The results showed that APE1 can dynamically polymerize on DNA in an apparently sequence-independent manner. We propose that this protein polymerization allows for scanning of the structural properties of DNA with short residence
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In spite of the impressive progress made in DNA glycosylase
2021-09-29

In spite of the impressive progress made in DNA glycosylase assays in recent years, few of them have clearly been viable candidates for further development and implementation in biomedical research and clinical practice. Future research efforts should be devoted to devising assays with improved perf
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Overall ABC transporters are hypothesised to prevent the pen
2021-09-29

Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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In experiments using D to displace binding of specific high
2021-09-29

In experiments using D22 to displace binding of specific high-affinity radioligands for DAT, NET, and SERT in mouse Busulfan tissue, we observed a ranking with D22 displacement efficiency in the order of DAT > SERT > NET (IC50 values being ~ 11 (DAT), 26 (SERT), and 101 (NET) µM; Fig. 1, Fig. 2, Fi
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Free fatty acid receptor FFAR
2021-09-29

Free fatty HOAt receptor 1 (FFAR1, also known as GPR40) belongs to the family of G protein-coupled receptors (GPCRs) and was de-orphanized in 2003 as a receptor for medium-to long-chain free fatty acids (FFAs) [9,10]. Mainly expressed in beta cells of pancreatic islets, GPR40 can be activated by th
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The fibroblast growth factor receptor
2021-09-28

The fibroblast growth factor receptor (FGFRs), including four highly conserved proteins (FGFR1-4), are important membrane sensors for extracellular signals [4]. By binding to their ligands, FGFRs are activated and can trigger various downstream intracellular signaling cascades, which is required for
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br Site of expression FASTK is
2021-09-28

Site of expression FASTK is expressed in various parts of human body including heart, skeletal muscle, brain, placenta, lung, liver, kidney pancreas (Ota et al., 2004) and many other organs (Fig. 1). It has been reported that FASTK is highly expressed in pancreatic tumors, where it is involved in
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We have expanded these studies
2021-09-28

We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA isrib or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist or t
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YAP TAZ nuclear function is also influenced by interaction
2021-09-28

YAP/TAZ nuclear function is also influenced by interaction with the TEAD family of transcription factors [96, 97, 98, 99, 100, 101]. The RAC1 used the survey exchange factor protein TIAM1 has recently been linked to YAP/TAZ regulation in the nucleus and cytoplasm. Nuclear TIAM1 inhibits YAP/TAZ bin
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Prolonged sGC oxidative inhibition occurs in many diseases K
2021-09-28

Prolonged sGC oxidative inhibition occurs in many diseases [46,[86], [87], [88]]. Keeping sGC membrane-bound and functional under conditions of high oxidative stress requires a mechanism for restoring oxidized sGC (Fe3+) heme iron to its reduced (Fe2+) state. Without this redox regulation, the sGC e
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Routine administration of exogenous GC
2021-09-28

Routine administration of exogenous GC is pertinent during late gestation, particularly in women who are at risk of delivering a preterm infant, aiming at ensuring proper neonatal outcome and survival (Kamath-Rayne et al., 2012). Unfortunately, despite its beneficial roles in foetal survival, variou
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In the pathogenesis of insulin resistance chronic activation
2021-09-28

In the pathogenesis of insulin resistance, chronic activation of inflammatory pathways plays an important role, and the macrophage/adipocyte inter-communication provides a key mechanism underlying the common disease states of decreased insulin sensitivity [10]. This involves the migration of macroph
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As a part of our continuing efforts towards discovery of
2021-09-28

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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Recently several dual GLP GIP receptor agonists have been
2021-09-28

Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously
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Notch signaling maintains the balance
2021-09-27

Notch signaling maintains the balance between neural stem cells and neural progenitors (Aguirre et al., 2010, Basak and Taylor, 2007, Mizutani et al., 2007). Conditional knock out of Notch causes depletion in the progenitor pool, showing that Notch is required for the maintenance of neural stem cell
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