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Which is the preferred dimer
2021-10-02

Which is the preferred dimer configuration, the one corresponding to the active state or the one corresponding to the desensitized state? Umbrella sampling simulations of a pair of GluA2 LBDs, using distances at the top (proximal to the ATD) and the bottom (proximal to the TMD), indicate that the de
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The lactam compounds including ceftriaxone CEF have shown to
2021-10-02

The β-lactam compounds, including ceftriaxone (CEF), have shown to attenuate drug-seeking in several drugs of abuse including methamphetamine [31], cocaine [32,33], nicotine [34] and morphine [35]. Moreover, in our laboratory, we have shown that CEF can reduce chronic alcohol drinking via upregulati
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It must be noted that
2021-10-02

It must be noted that while the accumulated evidence on molecular mechanisms has resulted in well-established experimental methods to externally act on single-cell characteristics and networks, safe and efficient external methods to modify multicellular states are still a matter of basic research. C
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Importantly bioelectric circuits in tissues Fig A have a cap
2021-10-02

(4) Importantly, bioelectric circuits in tissues (Fig. 2A) have a capacity to store long-term patterning information. An example is planarian anterior-posterior patterning: during regeneration, each fragment cut from a worm needs to build a head and tail at their correct ends. This process is regula
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The focused set of cyclopentapyrazoles
2021-10-02

The focused set of cyclopentapyrazoles produced six compounds with sufficient activity to warrant the evaluation of kinetic solubility. Despite the improved activity of the series, these compounds remain stalwartly insoluble (), indicating the need for additional chemical modifications which address
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br Acknowledgements This work was supported by grants
2021-10-02

Acknowledgements This work was supported by grants of the Argentine National Research Council (CONICET, PIP 0662). The authors express their appreciation to the Transmission Electron Microscopy Service (MET) of the Faculty of Veterinary Medicine of the National University of La Plata (Argentina)
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The only approved H R antagonist inverse agonist
2021-10-01

The only approved H3R antagonist/inverse agonist is BF2.649 (1- 3-[3-(4-chlorophenyl)propoxy]propyl piperidine), developed by Bioprojet and known as pitolisant (Wakix®). It was approved by the European Medicines Agency in March 2016 and marketed in the European Union to be used in narcolepsy with or
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Nazar and colleagues reported a normal HER gene number
2021-10-01

Nazar and colleagues reported a normal HER2 gene number in 13 primary and 2 recurrent ethmoid sinus adenocarcinomas, without any histological and immunohistochemical characterization, so a comparison with the present findings is impossible [14]. More recently, 552 head and neck carcinomas have been
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Finally worth of mention are few papers that
2021-10-01

Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a endo-iwr library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first series of
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br Conclusion Whilst acknowledging that forensic science
2021-10-01

Conclusion Whilst acknowledging that forensic science critically needs strategic investment across every domain [27], forensic science needs to bring both ‘hedgehog’ and ‘fox’ approaches together to address the roots of the major challenges the discipline faces. Addressing these challenges in a w
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A-443654 However although lactic acid suppresses the activat
2021-10-01

However, although lactic A-443654 suppresses the activation of effector , rendering them unable to buffer intracellular acidity [32], other T cell subpopulations such as regulatory T cells (Tregs) exhibit metabolic adaptations in low-glucose, high-lactate environments. In particular, Treg transcript
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br Next we explored the SAR around the
2021-10-01

Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic PRIMA-1 sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did not
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LbGlcK crystallized as a ligandless
2021-10-01

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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However protection against kainic acid
2021-10-01

However, protection against kainic acid-induced injury was not found by Lin et al. (2003) in the rats with AAV-GAL vector-mediated galanin overexpression, even though these animals, as mentioned earlier, exhibited attenuated of seizure severity. Although the reason for the controversy between the st
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A single ICV injection of GALP stimulated food intake
2021-10-01

A single ICV injection of GALP stimulated food intake in goldfish at 1h post-administration. This result is similar to that observed in rats, where ICV injection of GALP exerted an acute orexigenic effect [14], [15], [16]. Simultaneously, our findings counter the results found in mice, where central
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