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br Additional CDKs with a role in
2020-07-20

Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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Today many strategies have been developed
2020-07-20

Today, many strategies have been developed to enhance CXCR-4 receptor aldehyde dehydrogenase inhibitor on the cell surface, either by modifying the cell culture medium or by modifying the CXCR-4 gene in BMSCs to stimulate stem cell recruitment (Jiang et al., 2012, Liu et al., 2014b). For instance,
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Ligand binding RTK activation induces the endocytic internal
2020-07-20

Ligand binding (RTK activation) induces the endocytic internalization of RTKs, and this has been demonstrated for CSF-1R [15], [16], [17]. Endocytosed RTKs are targeted to the lysosome, which we and others have established to be dependent on ubiquitination via CBL-family and recognition by ESCRT com
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br Introduction To detect exposure to and effects
2020-07-20

Introduction To detect exposure to and effects of neuroactive pesticides in aquatic organisms, one widely used biomarker is cholinesterase (ChE) activity, which, among other possible functions, catalyzes the hydrolysis of the neurotransmitter Actinomycin D (ACh) in the cholinergic synapses of the
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A recent analysis of urine samples collected
2020-07-20

A recent analysis of 2721 urine samples collected from 245 men and 408 women across the US general population between 2005 and 2010 showed that MP, PP and BuP were measurable in 99.9%, 98.3% and 73.6% of samples from women and 99.3%, 90.2% and 35.9% of samples from men, respectively (Smith et al., 2
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The present study also showed
2020-07-20

The present study also showed that EP2 deficiency and EP4 antagonism significantly suppressed psoriatic GX-674 in an imiquimod model. Notably, however, the combined EP2 deficiency and EP4 antagonism did not completely suppress ear swelling in this model, possibly because there is the IL-17–independe
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2020-07-20

Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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Acknowledgments We are grateful to Dr Jean Marie Bernassau
2020-07-17

Acknowledgments We are grateful to Dr. Jean-Marie Bernassau for his leadership in establishing our virtual screening platform and Dr. Julie Bick for protein purification. X-ray data collection for compound 4 was performed by Shamrock Structures at Southeast Regional Collaborative Access Team (SER-C
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Our finding that activating DDR variants are a cause
2020-07-17

Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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Enzyme selectivity of many enzymes like
2020-07-17

Enzyme selectivity of many NVP-BGJ398 phosphate like β-galactosidases, acylases, epoxyhydrolases, lipases, etc. has also been modulated by using different immobilization techniques. It can result in the selection of optimal biocatalyst for different processes. This has many advantages over strategi
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Among our patients with anti
2020-07-17

Among our patients with anti-enolase drusen, those with a relatively short duration from the onset of visual symptoms to the first visit tended to have normal structure of photoreceptors with preserved visual function, despite the presence of drusen-related RPE abnormalities (Cases 1-3 and 8). In co
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PKA signalling in the nucleus was
2020-07-17

PKA signalling in the nucleus was thought to be due to the translocation of the catalytic subunit upon activation from the GDC-0084 to the nucleus via diffusion [72]. However, a new understanding has emerged, as both the regulatory and catalytic subunits have been identified in the nucleus and func
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As the communications interface was developed by two separat
2020-07-16

As the communications interface was developed by two separate organisations with differing software processes and tools, a modular approach to the safety case was deemed appropriate. The modular approach related the communications interface safety argument to the safety arguments for both the ACS an
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Ultrasound is an acoustic wave with a frequency
2020-07-16

Ultrasound is an acoustic wave with a frequency >20 kHz that needs a medium to propagate [20]. Accompanied by the spread of an ultrasonic wave, a series of alternating cycles of compression and rarefaction emerge in the liquid medium. During the rarefaction cycle, microbubbles are formed because of
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Similar to EGFR another receptor tyrosine kinase RTK fibrobl
2020-07-16

Similar to EGFR, another receptor tyrosine kinase (RTK), fibroblast growth factor receptor 4 (FGFR4), is gaining attention in the lung cancer setting. The protein expression of this receptor has been recently associated with a negative impact on lung cancer prognosis, supporting the idea that FGFR4
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