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C PHNO has been described as a full agonist
2019-11-13

[11C]-(+)-PHNO has been described as a full agonist at both D2 and D3 receptors [54,55]. [11C]-(+)-PHNO was initially developed as a PET radiotracer for imaging the high affinity state of the D2 receptor (i.e., highD2) as a means of measuring synaptic dopamine changes in response to pharmacologic ch
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DNA damage represents a persistent threat to genomic stabili
2019-11-13

DNA damage represents a persistent threat to genomic stability. A critical link exists between DNA mutation, chromosomal rearrangement and cancer development. In myeloid malignancies, various chromosomal translocations and/or mutations increased cellular reactive oxygen species (ROS), followed by DS
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In the gel shown in Figure at
2019-11-13

In the gel shown in Figure 8, at early time-points, 14% of the input dsDNA is converted to these intermediate species. These persist in the gel to later times, with approximately 50% of these being unwound. This unwinding occurs at a considerably slower rate and is due to that fraction of the popula
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The aniline R group was extensively
2019-11-13

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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Within the BLA both CRF and the CRF receptor have
2019-11-12

Within the BLA, both CRF and the CRF1 receptor have been shown to functionally regulate synaptic activity. In vivo, CRF release into the BLA originates from projections from the CeA (Roozendaal, Brunson, Holloway, McGaugh, & Baram, 2002). Central administration of both CRF and CRF1 agonists has been
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Not all of the biological activities exhibited by progestoge
2019-11-12

Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the rac inhibitor is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of the cell to respo
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The mechanisms by which coregulators control the
2019-11-12

The mechanisms by which coregulators control the actions of estrogen receptors are still a topic of ongoing research. From studies in cancer cells, we have learned that a large group of coregulators have specific structural motifs that than affect their contact with ER ligand-binding domains (Heery,
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Enzyme selectivity of many enzymes like galactosidases acyla
2019-11-12

Enzyme selectivity of many Raloxifene HCl like β-galactosidases, acylases, epoxyhydrolases, lipases, etc. has also been modulated by using different immobilization techniques. It can result in the selection of optimal biocatalyst for different processes. This has many advantages over strategies like
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The structure of the HOIP RBR LDD module bound
2019-11-12

The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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One of the most fundamental distinctions between Ub signals
2019-11-12

One of the most fundamental distinctions between Ub signals is substrate monoubiquitination versus polyubiquitination. With the exception of the E2, UBE2W, which represents a special case because it melk pathway only ubiquitinates the flexible N-termini of substrates [5], [6], [20], most examples o
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N acetylation by N acetyltransferase NAT is
2019-11-12

N-acetylation by N-acetyltransferase (NAT) is an important metabolic pathway for some substances, and there are 2 functional NAT isoforms in humans—NAT1 and NAT2. Studies of etamicastat in healthy subjects showed an extensive N-acetylation of etamicastat to the inactive metabolite BIA 5-961, and a l
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Canrenone br Acknowledgments Grant support was provided by t
2019-11-12

Acknowledgments Grant support was provided by the Leading Academic Discipline Projects of Shanghai Municipal Education Commission (J5028) (J50201) to Dr. Mi, the China National Science Foundation Project (81072076) to Dr. Mi, the China National Science Foundation Project (31000349) to Dr. Shen, a
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ampa receptor br Methods To study electrostatic substrate ch
2019-11-12

Methods To study electrostatic substrate channeling, we employed two methodologies, Brownian dynamics and a continuum model based on the Smoluchowski theory. Whereas Brownian dynamics simulations are useful for tracking the motion of individual particles, the continuum model is convenient for cal
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br Conflict of interest br
2019-11-12

Conflict of interest Acknowledgments Part of this work was supported by Institut Francais en Egypte, and the Academy of Scientific Research and Technology in Egypt under the frame of “Imhotep Project N°: 31681XL” and “STDF/IFE project N° 30630″ Introduction NSAIDs play an important role in
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There are two general approaches to building Bayesian networ
2019-11-12

There are two general approaches to building Bayesian networks for the purpose of risk assessment. Researchers can implement static models that predict risk or survival at a snap-shot of time. For example, Loghmanpour et al. [10] created Bayesian network-based risk assessment models for patient data
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