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As illustrated in Table monocyclic
2020-03-21
As illustrated in Table 3, monocyclic BAY 41-8543 receptor analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one analog 9 exhibited
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br Conflict of interest br Acknowledgements This work was su
2020-03-21
Conflict of interest Acknowledgements This work was supported by the Basic Science Research Program through the National Research Foundation (NRF) funded by the Ministry of Science, ICT & Future Planning (2013R1A1A1076117) and also by the Priority Research Centers Program through the NRF funde
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Lymphocyte mobility and homing is modulated
2020-03-21
Lymphocyte mobility and homing is modulated by the chemoattractant receptor subfamily of G protein-coupled receptors (GPCRs) (Campbell et al., 2003, Rot and von Andrian, 2004). B cell migration and position are controlled to a large extent by the lymphoid chemokines CXCL13, CXCL12, CCL19, and CCL21
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Mulan protein level is regulated
2020-03-21
Mulan protein level is regulated with conditions that stimulate mitophagy such as treatment of Protease Inhibitor Cocktail (EDTA-Free, 100X in DMSO) sale with CCCP [12]. We found that exogenously expressed GFP-GABARAP and RFP-Mulan could co-precipitate and co-localize in mammalian cells and the deg
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br Concluding Remarks Synthetic cytokine
2020-03-21
Concluding Remarks Synthetic cytokine biology has become an important research area with novel solutions and ideas for therapeutic approaches, for example, synthekines, fusokines, immunocytokines, neoleukins, MESA receptors, or synthetic Notch or cytokine receptors. In addition to their huge impa
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br Material and methods br Results br Discussion Monomeric
2020-03-21
Material and methods Results Discussion Monomeric CDK5 shows no enzymatic activity and requires the association with a regulatory partner for activation (Dhavan and Tsai, 2001). Here, we found that CDK7 might be one of the partners required for activation of CDK5 in the skin tissue, based o
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br Methods and materials br Cyclooxygenase COX is
2020-03-21
Methods and materials Cyclooxygenase (COX) is the key enzyme required for the conversion of arachidonic MCB-613 to prostaglandin, prostacyclins and thromboxanes., , , Two distinct isoforms of COX were initially discovered: COX-1 is a constitutive, housekeeping enzyme that is expressed in many
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Introduction We have recently identified that
2020-03-21
Introduction We have recently identified that caseinkinase 2 (CK2) inhibition protects white matter (WM) from ischemic injury. We focused our research on CK2 because upregulation of CK2 activity is associated with many diseases, including ischemic injury [1,[6], [7], [8]]. This review highlights an
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All of the studies referred to
2020-03-20
All of the studies referred to above were on microvillous membrane from hSTB; however, there is little information regarding conductances in the basal membrane. Illsley and Sellers, using a fluorescent technique, determined the relative permeabilities of cations and chloride in basal membrane vesicl
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igf1r inhibitor Two GPCR subtypes of interest in the myocard
2020-03-20
Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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The redox sensitive transcription factor NF B
2020-03-20
The redox sensitive transcription factor NF-κB is reported to play a crucial role in the COPD pathogenesis via up regulating the expression of several cytokines, chemokines, growth factors, and adhesion molecules [71]. Incidentally, we and others have shown that PARP-1 modulates the NF-κB activation
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Despite a high affinity for progesterone and a relatively
2020-03-20
Despite a high affinity for progesterone and a relatively high affinity for testosterone [7], the binding of progesterone and testosterone to CBG is often disregarded [1], [2], [3]. However, the concentrations of these two hormones varies considerably under both normal physiological and pathophysiol
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br Acknowledgements We would like to
2020-03-20
Acknowledgements We would like to thank Dr Ron Mason (NIEHS, Research Triangle Park, NC) for helpful discussion regarding the analysis of CCl4 metabolism, to Dr Karla Thrall and Dr Rick Corley (Battelle) for helpful discussions regarding study design and data interpretation, and to Jim Merdink an
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br DDR receptor and MMP expression Type II collagen protein
2020-03-20
DDR2 receptor and MMP-13 expression Type II collagen protein in articular cartilage is highly stable structure as its half-life is 117 years [43]. The chondrocytes have limited ability to synthesis type II collagen protein in the matrix of mature articular cartilage once the collagen gets disrupt
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br Materials and methods br Results Metabolic stability of c
2020-03-20
Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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