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Under optimized assay conditions very low concentrations
2019-11-08
Under optimized assay conditions, very low concentrations (20pM) of [125I]YP20 bound to hCRF1-CHO Perhexiline maleate membranes with high specificity (>95% inhibited by 1μM astressin) and in a membrane protein-dependent manner. Specific binding was selective vs. the hCRF2α subtype because little spe
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As noted earlier while exogenously administered BChE can
2019-11-08
As noted earlier, while exogenously administered BChE can protect against OP toxicity, its efficacy is limited by clearance of the protein from the circulation within a few days. A number of investigations have attempted to increase the circulation time of ChEs by chemical modification, gene transfe
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The phenolic hydroxyl group of ezetimibe tolerated various s
2019-11-08
The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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The same reservoir of genes is involved
2019-11-07
The same reservoir of D-(-)-Salicin is involved in fusions in all types of cancers, which predominantly encode kinases and transcriptional factors [102]. This makes fusion genes potential pan-cancer targets, and renders tumor categorization based on genetic profiling therapeutically reasonable. For
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From an industrial perspective the low turnover numbers and
2019-11-07
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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N Cyclopentylmethyl analog exhibited fold less potent recept
2019-11-07
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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Two GPCR subtypes of interest in the
2019-11-07
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 in vitro enantioselective metabolism of
2019-11-07
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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cp-690550 In addition to demonstrating the importance of DNM
2019-11-07
In addition to demonstrating the importance of DNMTs, we show that TGFβ1 differentially regulated DNMTs, and that TGFβ1 is both necessary and sufficient to induce lineage conversion of hepatocytes into MLCs with phenotypes and multipotency resembling MSCs. Upon withdrawal of TGFβ1 on day 28, we obse
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A set of small molecule LigI
2019-11-07
A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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Keeping the cofactor content oligomeric state subcellular lo
2019-11-07
Keeping the cofactor content, oligomeric state, subcellular localization, and membrane association in view, DHODH has been broadly divided into two classes, class 1 and class 2 [26], [27]. In many species it is present to either cytoplasm (Class 1) or to the inner mitochondrial membrane (or plasma m
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Acknowledgment This work was supported
2019-11-07
Acknowledgment This work was supported by the Swedish Research Council, the Knut and Alice Wallenberg Foundation, the Göran Gustafsson Foundation, the Swedish Pain Relief Foundation, the Torsten Söderbergs Stiftelse, the Swedish Children\'s Cancer Foundation, and the Swedish Cancer Society. The
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br Acknowledgements br Introduction Ischemic retinopathy is
2019-11-07
Acknowledgements Introduction Ischemic retinopathy is common to the major causes of blindness, including proliferative diabetic retinopathy, venous occlusion, and retinopathy of prematurity. The hypoxia that follows retinal capillary obliteration drives deregulated growth of new blood vessels
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Molecular imaging that provides a non invasive means
2019-11-07
Molecular imaging that provides a non-invasive means to visualize and measure a biological process of interest at the molecular and cellular level in living subjects has emerged as a promising approach for in vivo detection of enzyme activity in recent decades [6]. In ku catalog to anatomical imagi
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The absence of the LIG gene in yeasts has
2019-11-06
The absence of the LIG3 gene in yeasts has prevented the use of genetically tractable lower eukaryotes, such as Saccharomyces cerevisiae and Schizosaccharomyces pombe, as models to gain insights into the cellular functions of and interplay between the DNA ligases encoded by the LIG1, LIG3 and LIG4 g
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