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Several studies have found that
2022-05-17

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Tubastatin A HCl mg expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR14
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Conformational changes are observed in
2022-05-16

Conformational changes are observed in the LBDs after ligand binding, including partial cleft closure for GluN2A and complete cleft closure for GluN1. For GluN2A, additional conformational rearrangements in the protein and ligand may be required before the ligand can be accommodated within lobe 2. F
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br Introduction L Glutamate is one of the
2022-05-16

Introduction L-Glutamate is one of the most prevalent excitatory signaling molecules in the central nervous system (CNS) (Salazar et al., 2016) and plays a crucial role in a variety of Miltefosine functions such as memory and learning (Danbolt, 2001, Nedergaard et al., 2002). At elevated concent
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Medroxyprogesterone acetate receptor Although GLP has greate
2022-05-16

Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts
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Discrepancies in the reported results and conclusions from d
2022-05-16

Discrepancies in the reported results and conclusions from different groups regarding studies in ghrelin−/− and ghsr−/− mice are likely explained by the mixed background of the mutant mice used in the different studies [35]; although in the case of mice exposed to HFD, exposure to a HFD immediately
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br Ghrelin and energy balance To characterize the physiologi
2022-05-16

Ghrelin and Exemestane synthesis balance To characterize the physiological role of ghrelin in energy homeostasis, ghsr−/− and ghrelin−/− mice were generated [33], [36], [41], [47]. Although ghrelin regulates the amplitude of episodic GH release, ghsr−/− mice were not dwarfs, and in fact appear id
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In an immunohistochemical analysis of gastric cancer samples
2022-05-16

In an immunohistochemical analysis of 117 gastric cancer samples, reduced Cx43 and E-cadherin expression were shown to contribute to the development of primary gastric cancer; however, increased Cx43 and E-cadherin expression contributed to lymph node metastasis [13]. In primary urothelial PNU-12059
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In addition to inactivation of
2022-05-16

In addition to inactivation of Notch, we found that the combination of BTZ and GSI-I downregulated ERK phosphorylation in ALK+ ALCL cells, and we speculate this may occur through the inhibition of upstream regulators of the ERK pathway. These findings emphasize the functional complementation of the
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The sexual dimorphism in dlGALR a and dlGALR
2022-05-16

The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that
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jsh Two excellent GSMs with clear pharmacological effect acr
2022-05-16

Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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Most of the above mechanisms are
2022-05-16

Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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Although several new elements i e microsomes and
2022-05-16

Although several new elements (i.e., microsomes and NADPH) were added in E. coli cultures in the current study, the concentration of LacZ gene inducer, IPTG, to stimulate for the maximum production of β-galactosidase enzyme at media pH of 7.0 was observed to be the same as in the previous study (Fig
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br Materials and methods br Results Bgal from Alteromonas
2022-05-16

Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino dna staining residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other additional
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br FXR expression in normal intestine
2022-05-16

FXR BRD4770 in normal intestine and cancer Of note, there are several question marks about FXR post-translational modifications (such as acetylation or SUMOylation) and their involvement in the pathogenesis of metabolic and inflammatory disease (Balasubramaniyan et al., 2013, Kemper et al., 2009
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The ultimate success of multimodal probe in
2022-05-16

The ultimate success of multimodal probe in the inflammation imaging will be dependent on simplicity in synthesis (combining various modules without protection/deprotection), ease of optimization of pharmacological properties (linker group with tunable PEG moiety), co-registration of macroscopic and
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