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br Material and methods br
2021-06-08
Material and methods Results Discussion Conclusions To conclude, although CPT2 and CPT1 must have co-evolved to establish the carnitine shuttling, these enzymes are the most distantly related carnitine transferases, split early in evolution, during which a switch occurred in their locati
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In our ongoing investigation of the structure activity
2021-06-08
In our ongoing investigation of the structure activity relationship of benzenesulfonamide anti-inflammatory activity, we designed and synthesized a novel set of benzenesulfonamide derivatives starting from commercially available sodium saccharin. The pivotal features of our approach aimed to do some
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Another layer of CK regulation in the
2021-06-08
Another layer of CK1 regulation in the Hh and Wnt pathways is to employ different CK1 isoforms to phosphorylate distinct pathway components or even distinct sites on the same substrates. In this regard, it has been shown recently that the membrane-associated CK1 isoform CK1γ, but not the cytosolic i
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PLX3397 br STAR Methods br Acknowledgments We thank members
2021-06-08
STAR★Methods Acknowledgments We thank members of R.L. lab and F. Schweisguth for critical reading of the manuscript. We are also grateful to F. Janody, M. Miura, C. Bökel, H.D. Ryoo, G. Jiménez, the Bloomington Drosophila Stock Center, the Drosophila Genetic Resource Center, the Vienna Drosoph
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br Structure and function of EPAC isoforms EPACs
2021-06-08
Structure and function of EPAC isoforms EPACs are guanine nucleotide exchange factors (GEFs) for the Ras-like GTPases Rap1 and Rap2 [9]. There are two mammalian EPAC isoforms, EPAC1 and EPAC2 1, 2 (Figure 1). Whereas EPAC1 displays a wide tissue distribution, the expression of EPAC2 is more restr
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We continued to investigate the contribution of the EP recep
2021-06-07
We continued to investigate the contribution of the EP1 AS601245 to nociceptive sensitization by utilizing its natural ligand PGE and tested the effect of local subcutaneous injection of PGE (5nmol in 5μl) into one hindpaw on mechanical and heat pain thresholds. Wild-type mice displayed maximum sen
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Besides EGFR other tyrosine kinase receptors are currently g
2021-06-07
Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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Studies have focused on a hydrophobic
2021-06-07
Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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As before all calculations are based on thermodynamically fi
2021-06-07
As before [3], [4], all calculations are based on thermodynamically first- and second-order hydropathic (amino acid) scales [6], [7], linearly scaled to a common center and a common range for each of the 20 amino acids. These are then converted to a triangular matrix , where is the length of a sli
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Dipeptidyl peptidase inhibitors DPP is or gliptins stimulate
2021-06-07
Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit bcl-2 inhibitor secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good efficac
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AMPHs facilitate dopamine release which further triggers dop
2021-06-07
AMPHs facilitate dopamine release, which further triggers dopamine depletion [72]. Indeed, we observed that repeated treatment of MPA significantly inhibited TH-, DAT-, and VMAT-2 levels. Since DAT and VMAT-2 are important for dopaminergic terminal markers [10], their decreases suggest that MPA-indu
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Db model cells showed various aberrant phenotypes that
2021-06-07
Db model cells showed various aberrant phenotypes that seemed to reflect the pathological abnormalities found under diabetic conditions. First, in Db model cells after insulin stimulation, we found the inhibition of the transcriptional repression of the gluconeogenic genes, PCK1 and G6PC, and aberra
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The first transcription factor TF known to interact with one
2021-06-07
The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone AS 101 of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions during seed development an
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Previous research has suggested that the acetylcholine gated
2021-06-07
Previous research has suggested that the acetylcholine-gated chloride channels (ACCs) in Caenorhabditis elegans (Putrenko et al., 2005) exhibit the characteristics of promising drug targets. The genes that encode the various subunits of this family are present across the nematode phylum and appear t
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Berner et al used a meta analysis to
2021-06-07
Berner et al used a meta-analysis to show that sildenafil resulted in an effect of 9.65-point improvement. Tadalafil could be pooled into an effect of 8.52-point improvement, and vardenafil showed an effect of 7.50-point improvement. In our present studies, 200 mg udenafil resulted in an effect of 8
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