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PDEs a group of metallophosphohydrolases hydrolyze
2022-01-13

PDEs, a group of metallophosphohydrolases, hydrolyze the 3′,5′-cyclic phosphate group on cyclic nucleotides to a 5′-monophosphate, thereby blocking cyclic AMP (cAMP) or cGMP signaling [8,9]. There are different types of PDE isozymes, with different substrate specificities. PDE5 (specific to cGMP) an
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histamine receptor antagonist Acknowledgments Financial supp
2022-01-13

Acknowledgments Financial support from the National Natural Science Foundation of China (81730094, 81473262 and 81573299) is gratefully acknowledged. This project was also supported by the “111 Project” from the Ministry of Education of China, the State Administration of Foreign Expert Affairs of C
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The results of our study indicate the general importance of
2022-01-13

The results of our study indicate the general importance of the gp120 V3 loop aromatase inhibitors patch in the subunit association of primate immunodeficiency virus Env trimers. Our observation that the stem insertion mutants and hydrophobic patch mutants exhibit similar phenotypes with respect to
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An alternative to the chemoenzymatic preparation of
2022-01-13

An alternative to the chemoenzymatic preparation of glycoproteins is the production through total chemical synthesis or semi-synthesis [2,3,]. Many successful glycoprotein syntheses are based on native chemical ligation (NCL) [11], a reaction where unprotected peptides and glycopeptides of any lengt
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Although glycine receptors predominate in the
2022-01-13

Although glycine receptors predominate in the brain stem and spinal cord, they are also expressed in higher brain regions such as the nucleus accumbens, frontal cortex, and hippocampus (Jonsson et al., 2012, Jonsson et al., 2009, Molander and Söderpalm, 2005b). A variety of drugs of abuse, including
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PTMs have been shown to
2022-01-13

PTMs have been shown to influence transporter kinetics, both directly and indirectly (Xu & You, 2017). They do not just regulate the innate structure-function relationship driven by a transporter's global architecture, but rather are also able to regulate this relationship down to the resolution of
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It is known that hypercapnia as well as hypoxia
2022-01-13

It is known that hypercapnia, as well as hypoxia, can result in a decrease in body temperature, but the mechanisms involved are not very well known (Barros and Branco, 1998; Saiki and Mortola, 1996). One Fmoc-Leu-OH is that when there is an acute hypercapnic exposure, acidosis plays an inhibitory r
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GPR can signal through not only IP but also
2022-01-13

GPR40 can signal through not only IP3 but also cAMP depending upon the type of agonist ligand used. A full agonist engages both signaling mechanisms in contrast to the endogenous long-chain fatty Sulfo-NHS-SS-Biotin receptor (LCFA) ligands and partial agonists. Thus, stimulation of GPR40 by endogen
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The dopamine substrate currents IDA
2022-01-13

The dopamine substrate currents (IDA – IControl) were determined at different holding potentials (IV curves) in transfected HT22 cells (Fig. 5A). The plot for HT22 cells transfected with DAT exhibited the typical behavior of dopamine transporter currents (Ingram et al., 2002; Sonders et al., 1997),
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Recent studies suggested that non coding RNAs participate
2022-01-13

Recent studies suggested that non-coding RNAs participate in the modulation of Glut1 expression. For instance, the lncRNA NBR2-Glut1 axis was suggested to modulate cancer cell sensitivity to phenformin [37]. In renal carcinoma, miR-1291 is involved in the regulation of Glut1 Maraviroc mg [38]. Ther
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br Results and discussion br Conclusion In conclusion we des
2022-01-12

Results and discussion Conclusion In conclusion, we designed and synthesized a novel series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o. Further, α-glucosidase inhibitory activity of the synthesized compounds 10a-o was evaluated. The obtained results showed that all the synthesized thios
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Nuclear export of GK has
2022-01-12

Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros
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In summary the SAR of a series of phenylpropanoic
2022-01-12

In summary, the SAR of a series of phenylpropanoic acid-free fatty Almorexant receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust effi
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We reveal that the four well known vertebrate families of
2022-01-12

We reveal that the four well known vertebrate families of KAT enzymes (GNAT, MYST, P300/CBP, Basal transcription factor/nuclear receptor co-activator) seem to be conserved (Karmodiya et al., 2014; Roth et al., 2001; Sheikh & Akhtar, 2018) in the mangrove rivulus, together with Camello, a potential n
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Nuclear factor erythroid like NFE L
2022-01-12

Nuclear factor erythroid 2-like-2 (NFE2L2; hereafter NRF2) plays a crucial role in the basal and inducible expressions of multiple cytoprotective genes in response to electrophilic and oxidative stress [23]. The cytosolic actin-binding protein Kelch-like ECH-associated protein 1 (KEAP1) primarily re
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