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Multiple protein species are known
2019-11-08
Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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squalene epoxidase br Introduction The discoidin domain rece
2019-11-08
Introduction The discoidin domain receptors (DDRs), DDR1 and DDR2, are unique among the receptor tyrosine kinases (RTKs) in being activated by interaction with the extracellular matrix [1], [2]. Binding to triple-helical collagen is mediated by the receptor extracellular domains that include an N
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br Material and methods br Results br
2019-11-08
Material and methods Results Discussion In the present study, twenty strains of Y. enterocolitica were analyzed for their inhibitory potential on cysteine proteases. Five of these strains belonged to bioserotype 4/O:3, which is distinguished for its pathogenicity towards humans. The rest of
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van Linden et al developed a comprehensive guide that
2019-11-08
van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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It is interesting that of the control groups female
2019-11-08
It is interesting that of the control groups, female TG controls only had significantly higher MB-COMT protein than non-TG male controls (Supplemental Table 9, P = 0.005), while these two groups have almost equal expression of S-COMT protein (8.54- vs. 8.34-fold) and their COMT enzyme activity is al
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It would be very useful
2019-11-08
It would be very useful if unphosphorylated CK1s could be prepared using an E. coli expression system without the troublesome in vitro phosphatase treatment. So far, it has been shown that coexpressed λPPase, a Mn2+-dependent protein phosphatase that can dephosphorylate phospho-Ser/Thr/Tyr [20,21],
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The genetic basis of resistance to dieldrin
2019-11-08
The genetic basis of resistance to dieldrin has been described for several insect species as a mutation in the transmembrane domain II of the GABA-Cl or rdl (resistance to dieldrin) gene (ffrench-Constant et al., 2004; Bass et al., 2004; Du et al., 2005). A mutation in the GABA-Cl gene was found at
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Given the potency enhancing effect of the butyl group
2019-11-08
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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br Introduction Receptor tyrosine kinases RTKs are
2019-11-08
Introduction Receptor tyrosine kinases (RTKs) are critically involved in the development and progression of human cancers and are therefore useful targets for anti-cancer therapies [1]. The Eph receptors represent the largest subfamily of receptor protein kinases and interact with ligands called
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Functional studies revealed that these ESR mutations lead
2019-11-07
Functional studies revealed that these ESR1 mutations lead to constitutive activity of the ER, meaning that the receptor is active in absence of estrogen, conferring resistance against several endocrine agents. Recent studies reported that the occurrence of ESR1 mutations is rare in ER+ primary brea
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br Sources of funding br Disclosures br Acknowledgments br
2019-11-07
Sources of funding Disclosures Acknowledgments Introduction Insulin secretion from pancreatic β cells is a fundamental process to maintain blood glucose homeostasis. During glucose-stimulated insulin secretion, high glucose causes closure of ATP-sensitive K+ channels (KATP channels), sub
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Our data indicate that the ability
2019-11-06
Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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The all NTP pyrophosphatase and
2019-11-06
The all-α NTP pyrophosphatase and NUDIX families maintain the deoxynucleotide triphosphate (dNTP) pool balance, limit the incorporation of harmful nucleotides, and represent a promising therapeutic approach to develop anticancer and immunosuppressive agents., , , , Among these housekeeping enzymes
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The levels of circulating pro inflammatory
2019-11-06
The levels of circulating pro-inflammatory cytokines are markedly elevated in ESRD, and have been speculated to play an important role as causative factors in a number of uremic complications [37]. The impairment of phagocyte functions and deregulated cytokine productions are highly prevalent in CRF
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Pentamidine sale br Conflict of interest br Acknowledgements
2019-11-06
Conflict of interest Acknowledgements We wish to thank Arantza Pérez (University of the Basque Country) for her technical contribution to this study. This work was supported by grants from the Jesús Gangoiti-Barrera Foundation, Gobierno Vasco (GIC07/84), MEC () and SAIOTEK (SA-2008/00046).
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