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During the course of our research on mGlu PAMs
2021-02-03
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology,
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br Materials and methods br
2021-02-03
Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul
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Fatty acid oxidation plays a crucial
2021-02-03
Fatty Hydroxyzine 2HCl β-oxidation plays a crucial role in maintaining body energy homoeostasis mainly during catabolic states. It mainly occurs in mitochondria and involves a cyclical series of reactions that result in the shortening of fatty acids. Fatty acids comprise an efficient source of ener
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br Method br Results br Discussion In
2021-02-03
Method Results Discussion In this cross-sectional study, we investigated the relationship between the COMT ValMet polymorphism and age on regional cortical thickness in healthy adults across the lifespan. The mesocortical pathway was of primary interest because of its projections from the v
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It would be very useful if unphosphorylated CK s
2021-02-03
It would be very useful if unphosphorylated CK1s could be prepared using an E. coli expression system without the troublesome in vitro phosphatase treatment. So far, it has been shown that coexpressed λPPase, a Mn2+-dependent protein phosphatase that can dephosphorylate phospho-Ser/Thr/Tyr [20,21],
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It has long been known that native BChE is a
2021-02-03
It has long been known that native BChE is a major factor in the inactivation of cocaine, an ester-type drug of abuse [190]. But recently some researchers conceived the idea that BChE mutations could improve that function to a point that would favorably impact cocaine overdose. Rapid progress was ma
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Fujimoto et al pointed out
2021-02-03
Fujimoto et al. pointed out that RPN2 knockout alleviated the resistance of GC Wiskostatin synthesis (MKN74 and KATO III) to docetaxel and DDP [23]. Yuan et al. demonstrated that the depletion of RPN2 resulted in the reduction in resistance of GC cells to drugs such as irinotecan, docetaxel, doxoru
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Exposure to UV instead of DMBA
2021-02-03
Exposure to UV instead of DMBA also produced a sloughing and angiogenic response in transgenic, but not WT, mice, indicating that the epidermis of the BK5.EP4 mice has a much lower apoptosis threshold than WT mice, as suggested by others (Chun and Langenbach, 2007). Overall, these studies suggest th
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Our results demonstrate that pt PGE in
2021-02-03
Our results demonstrate that 17-pt-PGE2 - in addition to its described effects on EP1 and EP3 receptors - also acts as an EP4 agonist and thereby enhances vascular barrier function. Materials and methods Results Discussion In this study we demonstrate that the purported EP1/EP3 receptor ag
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In general terms PLA s participate in the
2021-02-03
In general terms, PLA2s participate in the Lands cycle of phospholipid fatty ivosidenib recycling [1,15,25], whereby the fatty acid composition at the sn-2 position of phospholipids is tightly controlled by a balance between hydrolytic reactions mediated by PLA2s versus activation of the free fatty
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br Materials and methods br Results br Discussion
2021-02-03
Materials and methods Results Discussion and conclusion The cardiac hypertrophy model can be established by two methods: drug induction and operation. The drug induction method is simple, while the operation method is closer to the real development of the disease. In this experiment, accord
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Several DA receptors heteromers with a therapeutic
2021-02-02
Several DA receptors heteromers with a therapeutic potential have been described, including D1R/D3R (Fiorentini et al., 2010), but their roles remain to be established. Moreover, most studies on receptor heteromers in addiction focused on the striatum because of its key role in the pathology and its
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If the unwanted objects detected by OpenComet are manually d
2021-02-02
If the unwanted objects detected by OpenComet are manually deleted, and then the DNA (%) in tail is computed, the performance of the present method can be compared more effectively. Therefore, performance of OpenComet is analysed in two ways as Approach 1 and Approach 2. Approach 1, considers the DN
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Sp family protein has been regarded as the housekeeping
2021-02-02
Sp family protein has been regarded as the housekeeping gene and is ubiquitously expressed. Although Sp family expression is regulated with some stimuli [17], [20], the total Sp family protein levels are not changed in most cases, as observed in our present study (Fig. 4). Constitutive binding of th
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br Conformational properties of DGK br Interaction of DGK
2021-02-02
Conformational properties of DGKϵ Interaction of DGKϵ with its lipid substrate A major component of the interaction between DGKϵ and lipid bilayers is the insertion of the hydrophobic segment comprising residues 20–42 into the membrane, as discussed above. However, this is not the only interac
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