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The aniline R group was extensively explored and a large
2020-04-26

The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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CRF binds to CRF and
2020-04-24

CRF binds to CRF1 and CRF2 receptor subtypes, triggering downstream cascades and leading to stimulatory G protein (GsP) activation. Once activated, GsP undergoes a structural change provoking the separation of the subunits Gα and Gβγ. The Gα subunit induces the production of the second messenger cAM
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According to this theory the chemical potential of the basic
2020-04-24

According to this theory, the chemical potential of the basic hydrate in the equilibrium condition can be calculated as: , and denote the chemical potentials of the basic hydrate, water and gas, respectively. Also, is the number of gas molecules per water molecules in the basic hydrate. After su
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The phenolic hydroxyl group of ezetimibe
2020-04-22

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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A set of small molecule LigI inhibitors were
2020-04-22

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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br Acknowledgements br Introduction Serum triglyceride conce
2020-04-22

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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Introduction Robust evidence suggests that genetic factors
2020-04-22

Introduction Robust evidence suggests that genetic factors influence an individual\'s susceptibility to BD (Craddock and Sklar, 2013). Yet, no single, high penetrance gene has been identified with direct causality (Craddock and Sklar, 2009). The largest GWAS to date for identifying genes conferring
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WRTs AI AI and AI showed the
2020-04-22

WRTs AI-82/1, AI-9-1 and AI-60 showed the same ST as was published by Dingle et al. in RTS 103, 013 and 097 (Dingle et al., 2011). WRTs 015 and 002 were assigned as WRTs 015-like and 002-like due to slight changes in their CE-ribotyping profiles; however, the ST of WRT 002-like (ST8) was identical t
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Plasminogen is composed of five N
2020-04-22

Plasminogen is composed of five N-terminal kringle domains and a C-terminal serine protease domain. The kringle domains have an affinity to lysine and binding of plasminogen with its receptors is dependent on its lysine interacting kringle domains [10], [28]. In the current report, we show that enol
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Because stimulation and blockade of dopamine D receptor all
2020-04-22

Because stimulation and blockade of dopamine D2 receptor all cause a similar disruption of maternal behavior, one critical question is whether they do so through the same or different behavioral mechanisms. One idea is that stimulation or blockade of D2 receptors similarly suppresses maternal motiva
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The methods used for cytokine analysis such
2020-04-22

The methods used for cytokine analysis, such as ELISA or multiplex systems could also influence the concentrations of cytokines analysed. It is therefore crucial to use the same lot of the multiplex analysis kit to make such a comparison [21]. In our study, we ensured that the analysis was performed
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Costunolide Among the Ub interactions observed in the HOIP s
2020-04-22

Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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CSN was initially identified based on the constitutitvely ph
2020-04-22

CSN was initially identified based on the constitutitvely photormophogenic (cop) mutants from Arabidopsis thaliana [48]. csn mutants are Cullin deneddylation-deficient, consequently accumulate neddylated Cullins, and arrest growth shortly after germination [49, 50, 51]. Weak csn mutants have defects
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With regard to the DGATs
2020-04-22

With regard to the DGATs, we have found that the majority of algal species encode at least one DGAT1, although it appears to be absent from Ostreococcus and Micromonas, as is the case for yeast, S. cerevisiae. More surprising is the presence of multiple DGAT2 genes in algae, with the exception of C.
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guanfacine hcl A different example of substrate dependent ac
2020-04-21

A different example of substrate-dependent activation is seen in CSN5, a JAMM-type DUB found in the eight subunit COP9 signalosome (CSN) [34]. The CSN deconjugates NEDD8 (neural precursor cell expressed developmentally downregulated 8) from Cullin Ring ubiquitin E3 ligases (CRLs). Through this activ
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