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Although epigenetic mechanisms are implicated in the pathoge
2022-08-08

Although epigenetic mechanisms are implicated in the pathogenesis of hematopoietic malignancies, little is known about the role of lysine-specific histone demethylases and whether manipulation of these enzymes can be translated into targeted therapies. KDM6A is the most frequently mutated histone de
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Traditional methods for HATs activity assays mainly depend o
2022-08-08

Traditional methods for HATs activity assays mainly depend on radioisotope labelling of histone substrates, which is limited by the complex procedures, hazards and wastes of radioactive materials. Hence, various alternative approaches such as electrochemical analysis, fluorescence and colorimetric a
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While more detailed molecular studies on the
2022-08-08

While more-detailed molecular studies on the mechanistic basis for heightened H3 receptor function in PAE rats are underway, we have also been exploring whether PAE alters other markers of histaminergic neurotransmission in affected brain regions. One question is whether PAE affected the number of h
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On the other hand imidazolylcyclopropane derivatives
2022-08-08

On the other hand, imidazolylcyclopropane derivatives and having a 2-substituted benzimidazolyl group showed moderate binding affinities for both the HR and HR. Replacement of 4-chlororbenzylamino group of with a benzimidazolyl group () led to increase the affinity for the HR more than 5-fold ( =
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br Direct effect of HDACs
2022-08-05

Direct effect of HDACs on contractile function by deacetylating cytoskeletal and contractile proteins Role of HDACs in electropathology by transcriptional reprogramming Next to deacetylation of α-tubulin by HDAC6 in experimental and human AF, there is also evidence for transcriptional reprogra
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Using embelin and its analogs as surrogate
2022-08-05

Using embelin and its analogs as surrogate GPR84 agonists we discovered that GPR84 couples to G12 and G13 signaling pathways in addition to Gi, linking receptor function to Rho/Rac signaling and modulation of the cytoskeleton. In primary human macrophages, GPR84 activation leads to Gβγ signaling, Er
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GPR has been implicated in neuropathic and inflammatory
2022-08-05

GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow
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On the other hand it is quite possible that strychnine
2022-08-05

On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th
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As discussed above both endogenous and exogenous lesions can
2022-08-05

As discussed above, both endogenous and exogenous lesions can lead to adverse health effects [43]. Damaged nucleobases can block DNA replication which is often lethal to cells [44]. The effectiveness of DNA restoration by DNA glycosylases should be closely monitored to gain an insight of the functio
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To test our refinement protocol we considered
2022-08-05

To test our refinement protocol, we considered a benchmark set of 12 N-linked glycan-containing protein structures determined by X-ray crystallography at resolutions ranging between 1.9 Å and 3.5 Å and comprising a total of 133 glycan units. We identified four incorrect anomeric configurations and 2
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MG 149 Pediatric cancers are fundamentally different from
2022-08-05

Pediatric cancers are fundamentally different from adult tumors and usually display a lower mutational burden and a faster growth rate. About 30% of all childhood malignancies are solid tumors and, in a majority of cases, respond well to chemotherapy. However, in particular in neuroblastoma the succ
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The simple carrier model for GLUT transport
2022-08-05

The simple carrier model for GLUT1 transport activity proposes that the transporter alternates between an outward facing glucose binding site and an inward, cytoplasmic, facing glucose binding site. Cytochalasin B is an endofacial inhibitor and appears to preferentially bind to the open, inward faci
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Transient forebrain ischemia in rodents induces
2022-08-05

Transient forebrain ischemia in rodents induces a reduction in expression of mRNA encoding the AMPA receptor subunit GluR265, 66, 67, 68, 69 (Fig. 3). gluR2 mRNA expression is markedly reduced in the CA1 region (the 8380 region most vulnerable to ischemia-induced damage), but not in the CA3 region
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The plasma levels of glucose and amino acids at day
2022-08-05

The plasma levels of glucose and amino acids at day likely represent the function in utero since the blood was collected within 2h after birth. To elucidate the roles of intestinal transporters as determinants of plasma levels of glucose and amino acids, we analyzed the correlation between the expre
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LbGlcK crystallized as a ligandless dimer in
2022-08-05

LbGlcK crystallized as a ligandless dimer in the asymmetric unit of space group P21 (Fig. 1a) with two identical subunits stabilized by a large contact surface area of 2295 Å2 (13% of the total surface area) as determined by the Protein Interfaces, Surfaces, and Assemblies (PISA) server [18]. Each m
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