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br Introduction Breast cancer is the most common malignant
2021-02-09
Introduction Breast cancer is the most common malignant tumor in women and the second leading cause of female death [1]. In recent years, with the improvement of early detection and the emergence of new treatment methods, the mortality rate of breast cancer has been greatly reduced. However, the
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melanocortin 1 receptor Grapiprant is a selective antagonist
2021-02-09
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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Expression of MGMT in human cells can
2021-02-09
Expression of MGMT in human XL413 hydrochloride can be switched off by enzymatic methylation of a cytosine residue in the MGMT promoter sequence. In this regard, both MGMT and the mismatch repair function MLH1 belong to a subset of DNA repair genes that are subjected to epigenetic control. In conse
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Nitric oxide NO is synthesized by conversion of
2021-02-09
Nitric oxide (NO) is synthesized by conversion of the l-arginine to NO and l-citrulline through reaction which is catalyzed by nitric oxide synthetase (NOS) (Knowles and Moncada, 1994). NO as an important molecule not only play a role as second messenger but also binds to cytochrome c oxidase and de
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For a physiologically relevant interaction ligand and
2021-02-09
For a physiologically relevant interaction, ligand and receptor have to be expressed in the same place. Collagen II is found primarily in cartilage. DDR2 is expressed in proliferating chondrocytes in vivo, and its staining pattern in tibial growth plates is similar to that of collagen II. In additio
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We neither observed changes in
2021-02-09
We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c
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br Conclusion br Acknowledgements This work is
2021-02-09
Conclusion Acknowledgements This work is supported by the National Natural Science Foundation of China (41806151, 41706144), the National Natural Science Foundation of China (31330082). We would like to thanks the support of young science and technology talents training fund of South China Agr
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Multiple lines of evidence now indicate that mitochondrial
2021-02-09
Multiple lines of evidence now indicate that mitochondrial decay is a fundamental factor that leads to alterations in energy metabolism in the aged heart (Hagen et al., 2002, Judge and Leeuwenburgh, 2007, Lesnefsky et al., 2001c). Nevertheless, the exact biochemical events that cause such an alterat
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br Introduction To detect exposure to and
2021-02-09
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 Mepivacaine HCl (ACh) in the cholinergic synapses of t
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Considering these reports and with
2021-02-09
Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on b
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br Significance Ubl post translational modifications are pot
2021-02-09
Significance Ubl post-translational modifications are potential targets for developing novel therapeutics for life-threatening diseases, such as c-Myc- and KRas-driven cancers that lack targeted therapy. However, only a few drugs are available to target these modifications. This lack of drugs hig
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Upon assembly of HLA tetramers loaded
2021-02-09
Upon assembly of HLA tetramers loaded with either of the two peptide versions, we could query the T cell repertoires of RA subjects and healthy individuals for the presence of cognate T UM 171 recognizing the respective peptide-HLA complexes. We found no significant difference in frequencies of T ce
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br Introduction Abdominal aortic aneurysm AAA
2021-02-09
Introduction Abdominal aortic aneurysm (AAA) is a daily concern in vascular surgery, as successful treatment is exclusively achieved by open or endovascular repair. Its prevalence is 2–11% among male smokers, and rupture the major complication, is associated with unacceptably high morbidity and m
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br Introduction In mammals there
2021-02-08
Introduction In mammals there are ten known isoforms of the enzyme diacylglycerol kinase (DGK), as well as gene splice variants. Enzymes of this family all have a homologous active site but differ widely in their molecular mass, mechanisms of activation and biological function (Shulga et al., 201
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Moreover a ligand for fusin has recently been
2021-02-08
Moreover, a ligand for fusin has recently been found: the lymphocyte chemoattractant stromal-derived factor-1 (SDF-1) binds to CHO 3-Deazaadenosine transfected with fusin and promotes secondary messenger production (Bleul et al., 1996; Oberlin et al., 1996). A new name, CXCR-4, has been proposed fo
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