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As part of their ongoing effort
2021-12-24
As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile ABT-888 derivatives as TGR5
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Increasing evidence has shown that
2021-12-24
Increasing evidence has shown that blockade of glutamate uptake leads to aberrant behavioral consequences. For example, intracerebroventricular (i.c.v) injection or microinjection of the GLT-1 inhibitor, dihydrokainic SynaptoRedTM C2 (DHK), into the prefrontal cortex induces anhedonia [8,9]. Microi
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br Conclusion br Acknowledgment This
2021-12-24
Conclusion Acknowledgment This study was supported by grants from the Excellence Initiative of the German federal and state governments, the Else Kröner-Fresenius Foundation and the German Society for Cardiology (DGK) to F.K. and grants from the Deutsche Forschungsgemeinschaft (SFB TRR 219 M-0
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Polymerisation of HbS initiates the clinical complications
2021-12-24
Polymerisation of HbS initiates the clinical complications of SCD (Bunn and Forget, 1986). The resulting sequelae are multiple and diverse, and their individual impact on pathogenesis is difficult to elucidate. Early changes include altered red cell membrane permeability (Gibson and Ellory, 2002, Le
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br Conclusion and future directions GS
2021-12-24
Conclusion and future directions GS is an important therapeutic target for the treatment of Alzheimer's disease. Its structure and function have been studied during the last years to understand the substrate cleavage mechanism to modulate the Aβ42 peptide production. The recent elucidation of GS
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The effect of GC on Fgf was not directly
2021-12-23
The effect of GC on Fgf21 was not directly dependent on ileal Fgf15 because basal Fgf21 Golgicide A was similar in Fgf15+/+ and Fgf15−/− mice. Moreover, GC treatment induced similar Fgf21 up-regulation in both strains. Fxr activation has been reported to increase Fgf21 expression and secretion [28]
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br Conflicts of interest br Acknowledgment br
2021-12-23
Conflicts of interest Acknowledgment Introduction The quetiapine mechanism of action growth factor receptors (FGFRs) are a family members of receptor tyrosine kinase (RTK) that represent attractive therapeutic targets for anti-cancer therapy gaining more and more attention in recent years
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Consistent with our gene profiling analyses showing that gen
2021-12-23
Consistent with our gene-profiling analyses showing that genes involved in mutual compensation of EGFR or integrin/FAK were significantly downregulated by Tinagl1 overexpression, treatment with r-Tinagl1 inhibited the activation of EGFR and FAK in vitro, and phenocopied the combined inhibition of in
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Case report A yr old Caucasian female presented
2021-12-23
Case report A 66-yr-old Caucasian female presented to Raigmore Hospital in Inverness, Scotland for orthopaedic surgery, specifically a trapeziectomy with ligament reconstruction and tendon interposition and extensor pollicis longus realignment after a diagnosis of bilateral pantrapezial osteoarthri
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br Methods br Results br Discussion In
2021-12-23
Methods Results Discussion In the general population BNP has been established as a marker for AZ 10606120 dihydrochloride failure diagnosis. Moreover, there is growing evidence that elevated levels of natriuretic-peptides may improve CV risk prediction in the general population above tradit
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Whether histamine receptor distribution is altered in canine
2021-12-23
Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist, J
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Nuclear factor erythroid like NFE
2021-12-23
Nuclear factor erythroid 2-like-2 (NFE2L2; hereafter NRF2) plays a crucial role in the basal and inducible expressions of multiple cytoprotective genes in response to electrophilic and oxidative stress [23]. The cytosolic actin-binding protein Kelch-like ECH-associated protein 1 (KEAP1) primarily re
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In this precancerous condition though cancer
2021-12-23
In this precancerous condition, though cancer develops from the epithelium, the subepithelial connective tissue also play crucial biological role in pathogenesis and progression to malignancy. In this context it may be noted that some recent reports addressed the problem of the mechanical interactio
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It appears that not all GPR agonists require a
2021-12-23
It appears that not all GPR119 agonists require a high dose to elicit acceptable Tenofovir Disoproxil Fumarate control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achiev
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A linker length of and atoms
2021-12-23
A linker length of 4 and 5 atoms was found to be optimal ( and ) compared to the only weakly active compounds with longer linkers ( and ) or the inactive compounds with shorter linker chains (–). In a next step incorporation of hetero-atoms in the linker was explored (). An amide linker as in and d
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