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br Results br Discussion The sequence homology based cluster
2019-11-16
Results Discussion The sequence homology-based clustering of the human kinome by Manning et al. (2002) has been extremely useful to organize kinases into guanabenz by sequence relationship. Since kinases are such prominent drug targets, we expect that clustering of the kinases by their inhibi
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Expression of DDR in endothelial cells
2019-11-16
Expression of DDR1 in endothelial cells has been previously described in human corneal blood vessels, and more recently, in murine atherosclerotic plaques (Franco et al., 2008, Mohan et al., 2001). So far, there is a lack of evidence for DDR1 expression in endothelial cells in the mouse iniparib pri
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br P Y receptor structure br Pharmacology Several subtype
2019-11-16
P2Y receptor structure Pharmacology Several subtype selective compounds have been developed in recent years (Jacobson and Müller, 2016; Rafehi and Müller, 2018). These compounds are helpful tools for analyzing the roles of P2Y receptor subtypes in physiology and pathophysiology. The present ar
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In the course of our program which was aimed at
2019-11-16
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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cck 1303 Alzheimer s disease AD is a chronic progressive
2019-11-16
Alzheimer’s disease (AD) is a chronic, progressive neurodegenerative disorder of the cck 1303 which is considered a leading cause of dementia and affects 20–30 million people worldwide. Presently, a suitable treatment and prevention strategy against AD is hardly available. Various studies have been
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T16Ainh - A01 From an industrial perspective the low turnove
2019-11-16
From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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br Orthotopic liver transplantation OLT is the
2019-11-16
Orthotopic liver transplantation (OLT) is the only curative therapy available for patients with end-stage liver disease. The surgical procedure of liver transplantation inherently involves cold ischemia during graft preservation , followed by reperfusion of the transplanted graft which results in
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Our finding that activating DDR variants are a
2019-11-15
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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Another question concerns the mechanism of
2019-11-15
Another question concerns the mechanism of PC reduction during the phosphate starvation response. There are at least three main mechanisms of PC depletion: suppression of PC synthesis due to substrate exhaustion, downregulation of PC synthase expression by suppression of gene transcription or intens
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Various domains of the HSA
2019-11-15
Various domains of the HSA molecule have also been used to make bioconjugates with increased stability, better targeting properties, and/or extended half-lives in blood. For example, domain I of HSA has been used in the preparation of antibody conjugates. This was achieved through the use of a cyclo
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br Conclusion br Acknowledgement The project was
2019-11-15
Conclusion Acknowledgement The project was supported by National Natural Science Foundation of China, China (No. 31872535); Natural Science Foundation of Shandong Province, China (ZR2018MC027, ZR2016CQ29); and Funds of Shandong \"Double Tops\" Program, China. Introduction High-altitude hyp
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Ageing is associated with increased reactive oxygen species
2019-11-15
Ageing is associated with increased reactive oxygen species (ROS) production, oxidative stress and oxidative damage [43,44]. Overproduction of ROS can impair endothelial function by suppressing NO synthesis and scavenging NO thereby decreasing its overall bioavailability. Moreover, sustained oxidat
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The repair pathway of DNA
2019-11-15
The repair pathway of DNA-DSBs through HR and the role of BRCA1 in repair kinetics by HR is also an important factor to unravel the radiation sensitization of novel small molecule inhibitors. The involvement of the breast cancer susceptibility gene 1 (BRCA1) in tumorigenesis and its role in facilita
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Isotretinoin br Experimental section br Author contributions
2019-11-15
Experimental section Author contributions Acknowledgements Introduction Many Isotretinoin in cells are sequential enzymatic reactions where the product of one enzyme serves as the substrate of a second enzyme (1, 2). Experimental evidence suggests that some of these consecutive enzyme-c
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br The DDR kinase domain The DDR intracellular kinase domain
2019-11-15
The DDR1 kinase domain The DDR1 intracellular kinase domain shares the typical structure of other kinase domains (Fig. 1). However, how DDR1 kinase is activated upon collagen binding is poorly understood. It is thought that the process is fundamentally different from the accepted paradigm of liga
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