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br Regulation of GCK by intrinsic conformational dynamics
2021-12-10

Regulation of GCK by intrinsic conformational dynamics GCK is a 465-residue, 52-kDa enzyme comprised of two domains, hereafter referred to as the large domain and the small domain, that are separated by a flexible hinge region. As with other proteins that adopt the hexokinase fold, substrates bin
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Our results revealed that when subjected to intravenous gluc
2021-12-10

Our results revealed that when subjected to intravenous glucose tolerance tests, the RIP-Gcgr mice showed enhanced glucose tolerance and increased beta cell function, which is in agreement with the findings of Gelling et al. [6]. However, we also show that there is a reduced responsiveness of the be
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In Solloway and colleagues reported that mice with
2021-12-10

In 2015, Solloway and colleagues reported that mice with alpha cell hyperplasia due to inactive hepatic glucagon receptor signaling may most likely be caused by amino Licarbazepine dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of rapamycin
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These reports have gradually established
2021-12-10

These reports have gradually established G-quadruplex binding small molecules as promising anti-cancer therapeutic agents. Besides the stabilization of G-quadruplex structures, some of these molecules also serve as diagnostic probes and sensors for G-quadruplexes in vitro and in vivo. Of these, Thio
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br Materials and methods br Results br Conclusions
2021-12-10

Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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JMJD C is another JmjC domain protein discovered
2021-12-10

JMJD1C is another JmjC domain protein discovered as a putative oncogene in shRNA screens in MLL-AF9-, HOXA9-, and AML1-ETO-driven AML 40, 41, 42. Depletion of JMJD1C decreased the frequency of LICs by inducing their differentiation and impaired the growth and establishment of leukemia in serial tran
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In this study there is a
2021-12-10

In this study, there is a limitation in the study of sex differences. Only female rats were used in our study. This is because the rats cannot urinate autonomously after SCI. Manual JNJ-7706621 emptying was needed until reflex bladder emptying was established (Lu et al., 2008, Ma et al., 2015). Bec
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2-Methoxyestradiol mg The first wave of cells infiltrating
2021-12-10

The first wave of 2-Methoxyestradiol mg infiltrating heart shortly after MI is composed mainly of neutrophils, with the highest number on the first day after ischemic episode [101]. These cells are recruited via C-X-C motif chemokine ligand-2 (CXCL-2)- and CXCL-5-mediated chemotaxis. Both chemokine
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Our last area of exploration was the piperidine core as
2021-12-09

Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th
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Introduction Substantial body of evidence supports
2021-12-09

Introduction Substantial body of evidence supports the notion that GABA, the dominant inhibitory neurotransmitter in the hypothalamus of mammals, affects GnRH release by two classes of membrane receptors: GABAA (GABAAR) [1] and GABAB (GABAB R) [2]. Studies in rodents and sheep have documented that
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One possible pathway summarizing the overall action
2021-12-09

One possible pathway summarizing the overall action involves NMDA receptor activation – Ca2+ influx – protein kinase A (PKA) activation – ERK phosphorylation and subsequent synaptic plasticity (Thomas and Huganir, 2004). A few studies have also shown modulation of synaptic glutamate transporters in
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br Acknowledgements br Introduction Benzodiazepine BZ treatm
2021-12-09

Acknowledgements Introduction Benzodiazepine (BZ) treatment is widely used for quick and efficient anxiolytic and sedative responses. However, when the use is extended to longer periods, adverse effects emerge. These include tolerance to the initial drug effect, dependence as revealed by withd
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The novel Ghsr IRES Cre knock
2021-12-09

The novel Ghsr-IRES-Cre knock-in mouse line allowed us to deconstruct the involvement of MBH GHSR-expressing neurons in mediating food intake responses using chemogenetic modulation of their neuronal activity. In our studies, hM4Di DREADD virus injections to inhibit GHSR neurons targeted several nuc
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The GAL also modified HT system Millon et al
2021-12-09

The GAL(1–15) also modified 5-HT system (Millon et al., 2015). Using a rat medullary raphe-derived cell line RN33B, we observed that GAL(1–15) significantly decreased the 5-HT immunoreactivity in the RN33B dihydrofolate reductase inhibitor antibacterial (p Conclusion All these data emphasized the
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br BA induced activation of TGR TGR is
2021-12-09

BA-induced activation of TGR5 TGR5 is a membrane-bound G protein-coupled receptor for BAs and its activation is dependent on cAMP formation and further stimulation of protein kinase A [53], [31]. The receptor is expressed in the enterochromaffin cells, smooth muscles, immune cells and more import
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