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The ETA receptor has a
2021-10-11

The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec
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The H R couples to G i o
2021-10-11

The H3R couples to Gαi/o proteins, and hence its stimulation leads to inhibition of adenyalate cyclases, diminishing the level of cyclic AMP (cAMP) with the subsequent reduction in downstream signaling pathways such as protein kinase A (PKA) activation and cAMP-responsive element binding protein (CR
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Under increased drug pressure more protease variants with mo
2021-10-11

Under increased drug pressure, more protease variants with more than one substitution will likely become clinically relevant. The accumulation of additional substitutions can allow RAS variants to emerge that alone are not viable, but in combination can rescue the viral fitness. We previously demons
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Among RASs observed in patients
2021-10-11

Among RASs observed in patients from group 2, RAS T54S was identified in one patient infected with subtype 1b. This mutation had been shown to cause resistance to boceprevir and telaprevir, but not to simeprevir [36]. This was confirmed here since this patient achieved SVR after 12 weeks of treatmen
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br Methods br Results br
2021-10-11

Methods Results Discussion Peptide therapeutics represents a unique class of biopharmaceuticals that continues to evolve in drug discovery and development. We and others have been particularly interested in bioengineering innovative pGC-A and/or pGC-B peptide activators. This has been succe
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PDEs a group of metallophosphohydrolases hydrolyze the cycli
2021-10-11

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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MHC class II antigen (45-57) [Homo sapiens] synthesis br Con
2021-10-11

Conclusion GST expression was detected in the Hemicornea construct and the commonly used animal cornea models at both the protein and functional levels. The results are summarized in Table 1. However, the construct exhibited lower levels of activity of GST, a marker of phase II enzymatic activity
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br Acknowledgements br Introduction The study
2021-10-11

Acknowledgements Introduction The study methods consisted of the review of articles included in the Pubmed and Medline databases and in the clinicaltrials.gov clinical trials register between 2013 and 2016, and of the preliminary results of therapies presented at international trichology confe
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br The mode of binding of ligands to
2021-10-11

The mode of binding of ligands to GPR35 As noted above, although kynurenic BRL 37344, sodium salt synthesis is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GP
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Through a large scale phylogenetic analysis of UDG superfami
2021-10-11

Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 KB-R7943 mesylate can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are present in e
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br Material and methods br Results br Discussion Neurosteroi
2021-10-11

Material and methods Results Discussion Neurosteroids capable of blocking the NMDAR channel attract a lot of attention as possible therapeutic agents for the treatment of neurodegenerative diseases. A large number of new Retigabine dihydrochloride with different structures have been synthe
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Next we focused on B part the
2021-10-11

Next, we focused on B-part, the phthalazine ring. While both nitrogen atoms of the phthalazine ring were found to be important (data not shown), replacing the benzene ring of the phthalazine part was attempted, and shows the results of the substituted pyridazine rings with bearing 2-methoxy benzene
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LbGlcK and the HsHxKIV d glucose complex PDB entry
2021-10-11

LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key Digoxin binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, such as K169 and
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br Summary br Acknowledgement br
2021-10-11

Summary Acknowledgement GR: A Nuclear Receptor with Widespread Physiological Impact GR, or NR3C1 (see Glossary), is a transcription factor (TF) that regulates gene expression in nearly every cell of the body. A member of the nuclear receptor (NR) superfamily, its ligand-binding domain confe
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br Results br Discussion ER and GR
2021-10-11

Results Discussion ER and GR play opposite phenotypic roles in the normal endometrium, with ER promoting growth and GR inhibiting growth. Here, we show that in endometrial cancer, GR expression is associated with worse outcomes and higher-grade tumors, and this association is observed only in
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