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br Results br Discussion br Conclusions The present study de
2020-11-16

Results Discussion Conclusions The present study demonstrates that CRF1 receptor-deficiency prolongs whereas CRF2 receptor-deficiency shortens the duration of recognition memory deficits induced by morphine discontinuation, unraveling opposite roles for the two known CRF receptor subtypes i
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br Results br Discussion Drug resistance
2020-11-16

Results Discussion Drug resistance poses the greatest hurdle of achieving high efficacy with AADs in cancer patients. AAD-treated cancer patients often encounter intrinsic and evasive drug resistance that diminishes the therapeutic efficacy to only minor survival benefits in most cancer types.
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Where a a a and
2020-11-16

Where a, a, a and b, b, b are respectively, repulsive friction constants and attraction friction constants. c represents the quadratic repulsive friction constant and P is critical pressure (bar). CPA equation of state CPA model is an EOS that simply combines a cubic EOS (SRK-EOS) and an associ
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To simulate the inhibition of the enzyme by organophosphorus
2020-11-16

To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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In S cerevisiae Mek a paralog of
2020-11-16

In S. cerevisiae, Mek1, a paralog of the checkpoint kinase Chk2, mediates cell-cycle arrest in response to meiotic defects (Bailis and Roeder, 2000, Xu et al., 1997). Mek1 is associated with meiotic chromosome axes, where its activation requires interactions with two other axis proteins, Hop1 and Re
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Thus the understanding of the various mechanisms of action
2020-11-14

Thus, the understanding of the various mechanisms of action of estrogen and SERMs is an important medical challenge and could help to develop an “ideal” SERM, preserving the beneficial effects of estrogen in the bone and urogenital system, and reducing the unwanted side effects, mainly increased ris
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br Nuclear estrogen receptors Indirect genomic signaling As
2020-11-14

Nuclear estrogen receptors: Indirect genomic signaling As mentioned earlier, the transcription of several genes that do not contain EREs in their promoter regions can also be regulated by estradiol, without direct binding of the estrogen receptors to the DNA. According to the most recent reports,
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br Experimental Procedures br Acknowledgments br Bisphenol A
2020-11-14

Experimental Procedures Acknowledgments Bisphenol A (BPA) has been recognized as one of the most potent endocrine disruptors, functioning even at very low doses. Although it is anticipated that ret proto oncogene receptor (ER) would mediate these effects of low-dose BPA, studies revealed th
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Among RAS mutant tumors analyzed we found that
2020-11-14

Among RAS mutant tumors analyzed, we found that the efficacy of either the SHP2 inhibitor SHP099, or combined MEK and SHP2 inhibition was best in those expressing RAS mutations at G12 (Figure 7B). Recent studies revealed that cellular RAS(G12C) activity depends on RTK-mediated nucleotide exchange, a
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In conclusion the data suggest that doses
2020-11-14

In conclusion, the data suggest that doses of COX-2 inhibitors and EP1 receptor antagonists which have previously been reported to exert disease modulating or antiepileptic drug potentiating effects do not negatively affect seizure control in temporal lobe epilepsy. The contrasting impact of the EP1
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Furan analogs and N methylpyrrole analogs had completely dif
2020-11-14

Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 Dihydroeponemycin receptor affinity and an increased antagonist activity, while the corresponding
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br Halogenases Enzymatic C H activation leading to
2020-11-14

Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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In addition to providing substantial insight
2020-11-14

In addition to providing substantial insight into substrate recognition, structural studies have revealed important details about mechanisms of glycosylation and HCF-1 cleavage [28,30,33]. Activation of the nucleotide-sugar is accomplished through interactions of the β-phosphate with the N-terminus
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Purmorphamine Anaesthetized mice of one eNOS KO strain showe
2020-11-14

Anaesthetized mice of one eNOS-KO strain showed a paradoxical decrease in blood pressure (BP) in response to i.p. administration of the NOS-inhibitor L-NA suggesting a role for non-endothelial isoforms of NOS in maintaining BP [1]. Alternatively, diminution in the activity of the renin-angiotensin s
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The total reduced glutathione content was determined
2020-11-13

The total reduced glutathione content was determined in both 5'-Iodoresiniferatoxin to examine whether retinol was decreasing glutathione concentrations and thus decreasing the conjugation of NAPQI. Total hepatic (3.9±0.3 vs 4.9±1.0 μmol/g, retinol vs untreated, respectively) and renal (0.4±0.1 vs 0
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