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br Challenges and open questions Deepening our understanding
2021-09-09

Challenges and open questions Deepening our understanding of PKC’s role in GSIS will require harnessing recently developed techniques and developing new tools. Here we describe three challenges remaining in the field and offer suggestions on experimental approaches to address them. PKC plays an
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In addition to indoles two additional structural variants we
2021-09-09

In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic R406 free base side chain to prepare compound (). The extension of the chain
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br Conclusion and perspectives Guanylyl cyclases are ubiquit
2021-09-09

Conclusion and perspectives Guanylyl cyclases are ubiquitous enzymes that regulate critical functions in bacteria to humans. In mammals there are seven mGCs and activators of all members have now been identified. Mutations in the genes that encode mGCs or pathologic activation of these enzymes or
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Our results show that deletion of the
2021-09-08

Our results show that deletion of the first loop of Obg does not abolish the augmentation of the GTPase activity of CgtAvc, revealing that the first loop is mainly responsible for the anchoring of the protein in the 50S and the transient interaction with ribosome is enough for augmentation of GTPase
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Given the involvement of dysregulated S
2021-09-08

Given the involvement of dysregulated S-nitrosylation in multiple pathological conditions, a number of approaches to regulate S-nitrosylation therapeutically are being tried in multiple indications [18]. In the lung, GSNO releasing compounds and GSNOR inhibitors are being considered as potential the
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Little is known about the role of GPR in physiology
2021-09-08

Little is known about the role of GPR35 in physiology and pathology. Using GPR35 knockout and wild-type mice showed that GPR35 activation by KYNA improves energy metabolism and inflammation, while demonstrated that GPR35 plays an important role in the development of angiotensin II-induced hypertensi
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br Materials and methods br Results br Discussion
2021-09-08

Materials and methods Results Discussion Although large-scale purification of homogeneous and functional membrane proteins is challenging, it is essential for biochemical, biophysical and structural characterization. This is particularly true for human P-gp, as its atomic structure has only
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The neurobiological mechanisms underlying DHK
2021-09-08

The neurobiological mechanisms underlying DHK-induced NOR learning and memory impairments remain unclear. Accumulated evidence shows that astrocyte-neuron lactate shuttle is of crucial important in synaptic plasticity and memory formation, and regulation of neuronal gene expression related to synapt
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Data were collected using a Powerlab
2021-09-08

Data were collected using a Powerlab and Chart 5 software (ADInstruments, Bella Vista, NSW, Australia) and were analysed using GraphPad Prism 5 (GraphPad Software, San Diego, CA). Responses to ghrelin receptor agonists in phenylephrine, methoxamine, endothelin-1, U46619 and 60mM [K+] contracted vess
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The absence of differences between GalR knockout and wild
2021-09-08

The absence of differences between GalR1 knockout and wild type mice in kainic acid-induced seizures suggests that GalR1 do not interfere with the seizure-inducing action of kainic acid. Postsynaptic kainate receptors are excitatory ionotropic glutamate receptors and their activation leads to seizur
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We next investigated whether pharmaceutical inhibition of th
2021-09-08

We next investigated whether pharmaceutical inhibition of the PI3K pathway was synergistic with FGFR inhibition using BKM120, a pan-PI3K inhibitor with modest antitumor activity in cancer patients, as a single agent. We found that RT112 (- translocation) and JMSU1 ( amplification) were not signifi
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Andexanet alfa works as a decoy for the FXa inhibitor
2021-09-08

Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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The finding that a peptide consisting of d amino acids
2021-09-07

The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino rxr receptor ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1 and
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The initial hyperproliferation phase during
2021-09-07

The initial hyperproliferation phase during crypt regeneration is reminiscent of the effects of Apc loss during tumour initiation and genetic studies show Yap and Taz are also required for adenoma formation in mice [10••, 12•, 13]. Furthermore, Yap activation by Mst1/2 or Sav deletion increases cry
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Hexokinases HXKs are major regulatory enzymes in sugar metab
2021-09-07

Hexokinases (HXKs) are major regulatory enzymes in sugar metabolism and in sugar sensing in plants (Claeyssen and Rivoal, 2007, Granot et al., 2013, Sheen, 2014, Aguilera-Alvarado and Sánchez-Nieto, 2017). HXK can phosphorylate both glucose and fructose to respective hexose-6-phosphates as a first s
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