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Present malarial chemotherapies mainly rely
2019-12-10

Present malarial chemotherapies mainly rely on a very few chemotypes or their allied structures such as quinolines, anti-folates and some cyclic endo-peroxides (Nayyar et al., 2012). Over the last few decades, the extensive and repetitive deployment of these drugs has stimulated resistance in the pa
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br Methods br Results and discussion br Acknowledgements
2019-12-10

Methods Results and discussion Acknowledgements Introduction Diacylglycerol O-acyltransferase (DGAT) is a key enzyme that catalyzes the final committed step in triglyceride synthesis and is highly expressed in the small intestine, adipose tissue, liver and mammary gland.1, 2, 3, 4 Its im
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pim inhibitor Our recent discovery M P H R A
2019-12-10

Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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br Materials and Methods br Results br Discussion Even thoug
2019-12-10

Materials and Methods Results Discussion Even though T cell checkpoint inhibitors alone have achieved impressive clinical benefit in some cancers, their application as single agents has had limited efficacy (Hamid et al., 2013; Wolchok et al., 2013). The resistance to immunotherapy is in pa
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Introduction Breast cancer is a highly prevalent malignancy
2019-12-10

Introduction Breast cancer is a highly prevalent malignancy. There are some recognized risk factors for breast cancer, like early menarche or late menopause, which increase the length of the exposure to hormones, as a result of a higher number of ovarian cycles [1]. Moreover, there is evidence supp
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ERR is constitutively active in the
2019-12-10

ERRγ is constitutively active in the absence of endogenous ligand. However, several synthetic ligands that can repress or induce ERRγ function by disrupting ERRγ-coactivator interactions have been reported to date. The estrogen receptor modulators diethylstilbestrol (DES) and 4-hydroxytamoxifen (4-O
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br Funding This work was supported by
2019-12-10

Funding This work was supported by intramural funding of the Department of Internal Medicine I-Cardiology, University Hospital Aachen, RWTH Aachen. Acknowledgments Introduction Cyclic adenosine monophosphate (cAMP) is a central second messenger that controls a plethora of vital functions.
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Potential break through technology poised to
2019-12-10

Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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Immunofluorescence assays were performed to localize the enz
2019-12-10

Immunofluorescence assays were performed to localize the enzyme during growth and differentiation to further characterize Giardia E1. As stated before, the assays showed that the Pefloxacin generated recognized specific E1 forms (E1-114, E1-90 and E1-67 with anti-gNTE1; and E1-47 with anti-gE1CT); t
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We analyzed whether HaCaT cells treated
2019-12-09

We analyzed whether HaCaT pergolide treated with PLD can alter the expression of genes involved in DNA damage response. Key DNA damage cues activate the sensory DNA-PK/ATM/ATR kinases, which relay two parallel cascades that ultimately serve to inactivate the Cyclin B-cdc2 complex. The protein kinas
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endothelin receptor antagonist Introduction Taenia solium is
2019-12-09

Introduction Taenia solium is the causative agent of human taeniasis/cysticercosis and porcine cysticercosis, a major health problem and a veterinary economic challenge in developing countries of Latin America, Africa, and Asia. In Mexico, approximately 500 human neurocysticercosis cases were repor
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The chemical structures of I C MOI
2019-12-09

The chemical structures of I3C, 3MOI, and 3MI and the Etifoxine hydrochloride responsible for 3MI metabolism in rainbow trout and carp are shown in Fig. 4. Discussion To determine the individual CYP450 isoforms involved in 3MI metabolism, we used specific inhibitors for CYP1A, CYP3A and CYP2E1.
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Circulating NK subsets also show
2019-12-09

Circulating NK subsets also show considerable differences in homing molecules. CD56bright CHIR-124 australia express the chemokine receptor CCR7 and L-selectin, which drive their migration to secondary lymphoid organs (Fehniger et al., 2003). In contrast, CD56dim display a high density of CX3CR1 an
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Gap19 br Acknowledgements br Introduction Serum
2019-12-09

Acknowledgements Introduction Serum triglyceride concentrations increase following ingestion of a fat containing meal resulting in postprandial hyperlipidemia. Peak serum triglyceride levels are observed within 2 to 4h of fat consumption and then gradually return to baseline levels within appr
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These cytokines except for TGF can also increase CysLT R
2019-12-09

These cytokines, except for TGF-β can also increase CysLT1R mRNA expression. We further demonstrated that TGF-β and IL-13 were able to increase the proliferation of human BSMC in response to LTD4. BSMC proliferation was CysLT1R-dependent, given that Montelukast ablated this effect. Taken together, o
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