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br Conclusion New series of thiazolo
2019-11-27

Conclusion New series of thiazolo[4,5-d]pyridazine and imidazo[2′,1′:2,3]thiazolo[4,5-d]pyridazine were designed and synthesized using thiazole as scaffold based on its previously observed activity as DHFR inhibitor. Compounds 13 and 43 (Fig. 9) proved to be the most active DHFR inhibitors with I
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I-BET151 Interferon IFN induces formation of a heterotetrame
2019-11-27

Interferon (IFN)-γ induces formation of a heterotetrameric, IFN-gamma-activated inhibitor of translation (GAIT) complex in human monocytic I-BET151 (Mazumder et al., 2003a, Sampath et al., 2004). The complex binds a bipartite stem-loop element in the 3′UTR of vascular endothelial growth factor (VEG
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Next to organophosphates carbamates and metals cholinesteras
2019-11-27

Next to organophosphates, carbamates and metals, cholinesterase activity can also be affected by other pesticides, such as newer generation neonicotinoid insecticides (NN). NNs do not inhibit AChE activity via the organophosphate-sensitive binding site of the enzyme, but rather, by acting as a struc
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ERR is constitutively active in the absence of endogenous li
2019-11-27

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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2 hydroxypropyl β cyclodextrin ERR is constitutively active
2019-11-27

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 Epac in cardiovascular pathophysiology Epac orchestrates
2019-11-27

Epac in cardiovascular pathophysiology Epac orchestrates signaling actors that regulate fundamental cellular functions and general biological effects. However, some important gaps still remain in the knowledge of the physiopathological role of Epac in the heart. So far, Epac has been implicated i
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is one of the few parasites
2019-11-27

is one of the few parasites that can be encysted and excysted and we tested the localization and role of HA-tagged gEno in both differentiations, using a recently developed integrated vector that introduces a C-terminal triple HA tag under the selection marker puromycin . The localization of HA-tagg
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Some antioxidants including N acetylcysteine
2019-11-27

Some antioxidants, including N-acetylcysteine and SOD, have been shown to decrease collagen deposition and protect the lungs in various animal models and even in clinical trials (Chan et al., 2013, Loomis-King et al., 2013, Rafii et al., 2013, Teixeira et al., 2008, Wang et al., 2013). Bleomycin-ind
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α-Conotoxin PIA mg At baseline mutant allele frequency of EG
2019-11-27

At baseline, mutant allele frequency of EGFR in tissue and plasma samples did not correlated with anti-tumor response (Supplementary Fig. 1). Among 35 patients who were positive for cell-free DNA (cfDNA) at baseline, changes of cfDNA during treatment were analyzed. Negative conversion (NC) of cfDNA
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568 synthesis We elucidated that the ten DGK isozymes
2019-11-27

We elucidated that the ten DGK isozymes have different relative 1-MGK and 2-MGK activities vs DGK activity under the same conditions. However, because the octylglucoside-mixed micellar assay was developed for DGK, it is not known whether the DGKs exhibit maximum 1-MGK and 2-MGK activities in this as
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br Introduction Biocatalysis can be used to synthesize chira
2019-11-26

Introduction Biocatalysis can be used to synthesize chiral building blocks, such as monomers for polymer materials, and precursors for pharmaceuticals [[1], [2], [3], [4]]. Enzymes are very suitable for catalyzing reactions with high enantioselectivity to obtain chiral products. For instance, alc
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In this review we first introduce the in
2019-11-26

In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), an
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LPS is the major toxic
2019-11-26

LPS is the major toxic component of the outer membrane of gram-negative bacteria and high dose of LPS challenge in animal can induce a rapid systemic inflammatory response which resembles septic shock in clinical [15]. We demonstrated that administration of KPT330 significantly attenuated lung injur
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br Acknowledgments We would like to thank the
2019-11-26

Acknowledgments We would like to thank the Bloomington Stock Center and the Vienna Drosophila RNAi Center for stocks used in this study. RMG was supported in part by a Professors grant to R. Losick from the HHMI and this work was supported by NSF grant 074578 to A.A.N. Introduction The catabo
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Iris domestica L Goldblatt Mabb syn Belamcanda
2019-11-26

Iris domestica (L.) Goldblatt & Mabb. (syn. Belamcanda chinensis L.) DC. (Iridaceae) occurs naturally in South and East Asia. Despite the fact that former monotypic genus Belamcanda has been included in the extended genus Iris, this classification has been questioned (Wilson, 2011; Mavrodiev et al.,
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