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In this paper we describe the
2022-11-01
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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br Autophagy at the Synapse The synapse is a highly
2022-11-01
Autophagy at the Synapse The synapse is a highly specialized neuronal compartment that forms the basic unit of communication between neurons. Communication relies on electrical signals that are propagated down the axon of the presynaptic neuron, where they trigger the quantal release of neurotran
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Demonstration of in vivo efficacy of potential chemopreventi
2022-11-01
Demonstration of in vivo efficacy of potential chemopreventive agents in animal models is necessary for their clinical development. Our present study provides experimental evidence that CuB 0.1μmol by oral administration (for 2weeks before the cancer cell injection, 5days per week) significantly inh
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We also measured macrophage infiltration and CLS presence in
2022-11-01
We also measured macrophage infiltration and CLS presence in peri-gonadal AT from db/db mice and controls. CLS are morphological features within AT that are accurate indicators of adipocyte death and macrophage infiltration [56]. An earlier study showed that CLS macrophages account for >90% of the t
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Somatostatin analogs also bind to somatostatin receptors It
2022-11-01
Somatostatin analogs also bind to somatostatin receptors. It has been reported that octreotide has a high affinity for hSSTR2, moderate affinity for hSSTR3 and hSSTR5, and does not bind to hSSTR1 or hSSTR4 (Ben-Shlomo and Melmed 2008). Compared to octreotide, pasireotide displays 40-, 30-, and 5-fol
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br Materials and methods br Results br Discussion
2022-11-01
Materials and methods Results Discussion The current treatment modalities for colorectal cancer are hampered by various issues such as high acquired resistance, long-term complication with potential of cancer recurrence, severe side-effects and poor therapeutic index [50], [51], [52]. Comp
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Enhancers are short regions of DNA that are bound by
2022-11-01
Enhancers are short regions of DNA that are bound by DNA-binding proteins (TFs) to increase the likelihood of a particular gene to be expressed. Importantly, enhancers can be identified, and classified, by their patterns of chromatin accessibility and of enrichment in certain histone modifications.
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br Conclusions br Funding This work was supported
2022-11-01
Conclusions Funding This work was supported by a Finnish government subsidy for health science research [grant numbers TYH2012141, TYH 2013218, and TYH 2014216]; the SSAC Foundation [grant numbers SLS-504141 and SLS-693781]; and the Paulo Foundation. The funding sources had no involvement in s
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br Materials and methods br Results
2022-10-31
Materials and methods Results and discussion Conclusions In this study, for the first time to the best of our knowledge, the stability of pure hsALDH has been studied under various conditions. The enzyme exhibited low storage stability both at 4°C and 25°C, which could be improved to a good
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RVX-208 In this article we have outlined the
2022-10-31
In this article, we have outlined the increasing, as yet still circumstantial evidence that the 6TM domains of bacterial ACs might operate as receptors for as yet unknown ligands. Intriguingly, several architectural arguments are also applicable to the 6TM domains of mammalian membrane-bound ACs (mA
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br Adenosine receptors and innate immunity
2022-10-31
Adenosine receptors and innate immunity Monocytes and macrophages. All four adenosine receptor subtypes are expressed on monocytes and macrophages, and their levels and function undergo significant changes during the maturation of macrophages from monocytes. Indeed, quiescent monocytes are charac
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Cofilin is an additional actin severing protein present in s
2022-10-31
Cofilin is an additional carboxypeptidase severing protein present in sperm cells that undergo phosphorylation/inactivation on serine 3 by Lim kinases (LIMK) and by Tes kinases (TESK) [48]. LIMK can be activated by several pathways, including one through the Rho/ROCK/LIMK cascade [49], [50], [51]. A
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To date the modes of
2022-10-31
To date, the modes of actions of pharmaceuticals in humans and mammals are well-known (Fent et al., 2006), whereas knowledge of aquatic organisms, particularly invertebrates, is limited. This is problematic as these contaminants/pollutants have potentially harmful effects on wildlife organisms that
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somatostatin receptor Using constant potential amperometry a
2022-10-31
Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of somatostatin receptor release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured si
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The next level of possible correlation
2022-10-31
The next level of possible correlation and comparison between the α7 and 5HT3 receptors is at the subunit arrangement and protein folding. Crystal structures of the nicotinic and serotoninergic MK-8669 receptors [45], [46] reinforced the concept of similarities between these families of receptors. N
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