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Recently we suggested that KYNA an
2022-02-25
Recently, we suggested that KYNA – an endogenous GPR35 agonist could be produced in a human cornea since we showed the presence of the enzymes that catalyze the synthesis of KYNA – kynurenine aminotransferases I-III in corneal epithelium, stroma and endothelium (). Therefore, these findings provided
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br Clinical development of anti
2022-02-25
Clinical development of anti-NASH drug therapies The current understanding of NASH pathogenesis has led to broad efforts to target several features of the disease, alone or in combination, even in the absence of liver-guided therapies. Therefore, drug development in NASH is a rapidly changing fie
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Selective pharmacological inhibition of tonic currents
2022-02-25
Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i
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br Experimental br Results and discussions br Conclusions In
2022-02-25
Experimental Results and discussions Conclusions In this work, a novel label-free ECL biosensing method was developed to detect TDG activity using signal amplification strategy of HCR which was triggered by DNA functionalized AuNPs. The label-free ECL biosensing platform has been constructe
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LbGlcK and the HsHxKIV d glucose complex PDB entry IDH
2022-02-25
LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key ibuprofen solubility binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, suc
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br Mechanisms of action Ghrelin is a amino acid peptide
2022-02-25
Mechanisms of action Ghrelin is a 28-amino Palomid 529 peptide hormone primarily produced in the oxyntic mucosa of stomach, but also in other gastrointestinal tissues [7] (Fig. 1). It acts as the endogenous ligand for the ghrelin receptor [GHS-R1a] and causes the release of growth hormone from t
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In the course of our ongoing attempts to
2022-02-24
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric Tamoxifen type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the proces
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br Acknowledgments We apologize to the researchers who
2022-02-24
Acknowledgments We apologize to the researchers who were not referenced due to space limitations. We thank Dave Primm (Department of Surgery, University of Texas Southwestern Medical Center) for his critical reading of the manuscript. This work was supported by grants from the US National Institu
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Conformational analysis provides further insight into the
2022-02-24
Conformational analysis provides further insight into the SAR trends apparent in . Acyclic precursors – are 25–50-fold less active than their macrocyclic counterparts – against Pyk2. The global minima for – are conformations in which the –NHCH– linker between the pyrimidine and pyridine rings is sta
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Interestingly evidence has emerged recently that suggests
2022-02-24
Interestingly, evidence has emerged recently that suggests noncanonical roles of EZH2 in various cancers. For example, in addition to histone H3, EZH2 has been shown to methylate non-histone substrates, such as Jarid2 and STAT3, to regulate their transcriptional activities (He et al., 2012, Sanulli
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br Formation of secretory vesicles
2022-02-24
Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for cyclosporin off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013). Bin/Am
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It is an exciting time
2022-02-24
It is an exciting time for translational histamine research, since preclinical studies show potential value for histamine receptor ligands. As reviewed above, there are several concerns for future studies of histamine and its role in the CNS. 1) Because of the availability of HDC-Cre mice (Williams
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The glycolytic activator phosphofructo kinase fructose bisph
2022-02-24
The glycolytic activator 6-phosphofructo-2-kinase/fructose 2,6-bisphosphatase 3 (PFKFB3) is well-known as a downstream substrate of hypoxia-inducible factor 1α (HIF-1α) signaling pathway [5,6]. Tumor hypoxia has long been associated with increased malignancy, poor prognosis and drug resistance. HIF-
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In the present study fasting blood glucose and
2022-02-24
In the present study, fasting blood glucose and insulin levels were not significantly different between GA patients and control cases. Normal mammalian cells typically acquire fatty acids from the circulation owing to insulin, which is the most lipogenic hormone in the subset of adult tissues, inclu
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Theoretically the majority of resistance
2022-02-24
Theoretically, the majority of resistance mechanisms identified so far could be targeted by compounds that are already available, such as inhibitors of ER, PIK3CA/mTOR or FGFR1. However, the potential therapeutic advantage of combining these agents with standard HER2-targeting treatments must be wei
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