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To evaluate the ability of both sets
2024-01-05
To evaluate the ability of both sets of compounds to inhibit the activity of 15-LOX an initial screen was performed, whose results are shown in . The comparison of inhibition values would seem to indicate that, in the HYD series, an electron donor group at the position increases and an electron at
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Based on the extracellular domain structures we can infer
2024-01-05
Based on the extracellular domain structures, we can infer that the dimer arrangement of GABAB receptor will undergo substantial changes upon receptor activation (Geng et al., 2013). First, agonist-stimulated closure of GABAB1 VFT would cause an upward rotation of its LB2 domain, coupled with an inw
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D609 br Acknowledgment Supported in part by NIH R
2024-01-05
Acknowledgment Supported in part by NIH1R21EB012707 (Biegon, Anat PI). Introduction Estrogens exert pleiotropic effects on a variety of morphological, physiological and behavioral responses in all vertebrate classes ranging from fishes to mammals. Effects of estrogens in the D609 concern repr
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The neural circuitry involved in
2024-01-05
The neural circuitry involved in the production of the EOD, its modulations, and in the sensory processing of communication signals has been well characterized (Bell and Maler, 2005; Chacron et al., 2011; Krahe and Maler, 2014; reviewed in Metzner, 1999). Pacemaker cells located in the pacemaker nuc
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On the other hand key enzymes also involved in
2024-01-05
On the other hand, key 2-NBDG receptor also involved in NO metabolism are nNOS and eNOS. Apparently, during acute ischemia, eNOS activity and NO concentration surge for a short period of time (Schulz et al., 2004) but eventually the expression and activity of the synthase and consequently NO concen
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Indications that HMGA proteins are involved in regulating
2024-01-04
Indications that HMGA proteins are involved in regulating the structure and function of large chromatin domains come from the early work of Saitoh and Laemmli [143]. Employing immunolocalization techniques, these workers demonstrated that HMGA1 proteins are co-localized with both histone H1 and the
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The control group participants of the current study were
2024-01-04
The control group participants of the current study were very similar in age to those of Puertas et al. There was no significant correlation between age and enzyme activity over the short age span studied although age-related changes in the activity of ApA and aspartyl aminopeptidase, typically incr
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In conclusion we show that HBP is phosphorylated
2024-01-04
In conclusion, we show that HBP1 is phosphorylated on three sites, which control HBP1 transcriptional activity and glioblastoma cell proliferation. This phosphorylation largely depends on AKT, although other kinases may also be involved. In a previous study, we had shown that the PI3K-AKT pathway re
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br Liver specific AHR deficiency and
2024-01-04
Liver-specific AHR deficiency and energy balance In contrast to the amelioration of hepatic steatosis by global AHR deficiency, targeted knockout of Ahr in hepatocytes exacerbated it in B6 mice fed on a high-fat diet, without interfering with body weight gain [21]. This appeared to result from au
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br Materials and methods br Results The average body weights
2024-01-04
Materials and methods Results The average body weights for each group of mice over the course of the study are shown in Fig. 2A. The average body weights of the mice in the saline control group and PACAP group increased slightly during the study. In contrast, starting at day 17, the body weigh
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br Materials and methods br Results br Discussion Very few
2024-01-04
Materials and methods Results Discussion Very few ARF inhibitors have been developed to study the key functions these small GTP-binding proteins play in pathophysiology. The natural compound Brefeldin A (BFA) has exhibited drastic effects in cells such as collapse of the Golgi because of it
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br ACK inhibitors Since ACK activation
2024-01-04
ACK1 inhibitors Since ACK1 activation is correlated with poor prognosis in various cancers, strong efforts are being directed by multiple groups towards developing highly potent and specific small molecule inhibitors targeting the ACK1 kinase. At least eight small molecule kinase inhibitors have
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LO is a soluble kDa
2024-01-04
5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell
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Derivatives of M that possess either an alkyne
2024-01-04
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these Hordenine receptor to maintain 5-HTR antagonist properties as (+)-M100907 was d
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In this paper we describe the formation of a
2024-01-04
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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