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Adenosine triphosphate ATP is thought to be
2022-06-14

Adenosine triphosphate (ATP) is thought to be a crucial molecule in acute pain signaling in the DRG, as well as in the development and maintenance of chronic pain (Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). Extracellular ATP activates the ionotropic P2X receptors (Bur
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br Materials and methods br
2022-06-14

Materials and methods Results Discussion All the UDG superfamily glycosylases examined here, UDG, SMUG1, TDGFL, and TDG82−308, are capable of completely converting U-containing duplex substrates to product, though at different rates. Under STO conditions, kobs reflects the slowest kinetic s
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Initial studies generally focused on
2022-06-14

Initial studies generally focused on the co-administration of glutamate with transport inhibitors and clearly revealed the ability of the blockers to exacerbate excitotoxic injury in both in vitro and in vivo models (McBean & Roberts, 1985, Robinson et al., 1993a). In addition to demonstrating the c
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The LBD experiences a large scale conformational transition
2022-06-14

The LBD experiences a large-scale conformational transition between open and closed states upon agonist binding within the cleft separating the two lobes of the domain. The upper lobe (Lobe 1, also called D1) is connected to the ATD, and the lower lobe (Lobe 2, also called D2) is connected to the TM
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As a part of our continuing efforts towards discovery of
2022-06-14

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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In order to elucidate the
2022-06-14

In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen human leukocyte elastase of the BOC group to a nitrogen atom, decreased the activity (EC = 0.1
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br Experimental br Results br
2022-06-14

Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,
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Emergent studies have recently shown that
2022-06-14

Emergent studies have recently shown that Sherpas living at high altitude have adaptations that make life at high altitude more compatible. Sherpas are known to have blood Hb concentrations about the same as lowlanders and Han populations [30]. This is different from what happens to lowlanders, Han
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The significance of A and tau as therapeutic
2022-06-14

The significance of Aβ and tau as therapeutic targets is not only derived from pathological evidence of postmortem brain but also from biochemical analysis of cultured human neurons. This is largely based on the induced pluripotent stem cell (iPSC) technology that has been established to study Aβ, t
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br Fenton reaction based nanomaterials for ferroptosis In
2022-06-14

Fenton reaction-based nanomaterials for ferroptosis In Fenton reaction, H2O2 is converted by Fe2+ or Fe3+ to highly oxidative ROS (Eqs. (1) and (2)), which is commonly used to catalyze the degradation of refractory organics [34]. Since the tumor microenvironment is characterized by low acidity an
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Glucose induced nuclear translocation of
2022-06-14

Glucose-induced nuclear translocation of several enzymes, including GK, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), muscle GS, aldolase, lactate dehydrogenase (LDH) and phosphoglycerate kinase (PGK) is a well-known phenomenon. Additional functions have been proposed for these enzymes in the nu
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SAR 405 synthesis Considering their good FAAH inhibitory act
2022-06-14

Considering their good FAAH inhibitory activity, compounds and have been selected for an in vivo study in a DSS-induced colitis model. Specific Pathogen Free male 7weeks old C57/Bl6 mice received 2.5% DSS in drinking water during 8days. Concomitantly, they were administrated daily intraperitoneally
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PKC does not however directly stimulate secretion by
2022-06-14

PKC does not, however, directly stimulate secretion by initiating calcium influx into the cell [51]. Work from multiple groups measuring calcium currents has shown that PMA alone or coupled with glucose does not modulate intracellular calcium influx [34], [51], [52], [53]. Instead of contributing to
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Third across all three signaling molecules examined
2022-06-13

Third, across all three signaling molecules examined, the baseline abnormalities seen in Hdc-KO mice resemble the effects seen after H3R activation in wild-type animals. Specifically, MAPK activity (indexed by MSK1 phosphorylation) is increased at baseline in dMSNs of Hdc-KO mice to a similar degree
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Compared to the other histamine receptor subtypes the
2022-06-13

Compared to the other KN-93 hydrochloride receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (
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