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PBI is an agonist of GPR and acts as an
2021-11-18

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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br Materials and methods br Results br Discussion The distri
2021-11-18

Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta Vincristine [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract, adipocy
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Therefore the histomorphology and the comprehensive analysis
2021-11-18

Therefore, the histomorphology and the comprehensive analysis of TMJ-RA pathogenesis need to be completed although clinical findings in TMJ-RA are similar to RA in other joints [41]. Especially for the dentist, the difficulties associated with diagnosing TMJ-RA patients [49] posing challenges to dia
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In conclusion we have shown that the brain penetrating
2021-11-18

In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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Before discovery of their histone demethylase function the J
2021-11-18

Before discovery of their histone demethylase function, the JARID1 isoforms were identified across diverse fields including stem cell biology and congenital disease, as detailed in Box 2. Their observed roles in cancer progression and therapy resistance have led to ongoing pursuit of inhibitors tai
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In this current study we
2021-11-18

In this current study, we not only demonstrated the growth-inhibitory effects of the 2nd generation analog SL-1-39 on the HER2+ breast cancer cells, MDA-MB-453 and SKBR3 (Table 1), but we also demonstrated that the decrease in cell number was associated with an interruption of kv1.3 inhibitor progr
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Interestingly systemic circulating levels of NOx were not dr
2021-11-18

Interestingly, systemic circulating levels of NOx were not dramatically increased by treatment with isosorbide mononitrate or sodium nitrite at a dose which exerted beneficial effects on the progression of PH. In line with our results, Mathew et al. [13] demonstrated that the long-acting NO donor mo
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Telatinib Financial nonfinancial disclosures The authors
2021-11-18

Financial/nonfinancial disclosures: The authors have reported to CHEST the following: M. J. A. has received investigator-initiated grants from Pfizer and Boehringer Ingelheim for unrelated research. None declared (X. D., S. C. D., G. B., N. T. W., J. L. P., J. H., B. E., A. J. L., J. A. B., C. S., C
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Tanshinone I br Materials and methods br Results br
2021-11-17

Materials and methods Results Discussion Until very recently, the anti-atherogenic activity of niacin was attributed almost exclusively to its impact on HDL and other plasma lipids, perhaps mediated via its action on GPR109A expressed in adipose or other tissues. However, recent clinical st
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Cichlasoma dimerus as most teleost fish species present neur
2021-11-17

Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most Nicardipine HCl species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA (Gon
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br Redox regulation in the brain Reactive oxygen species are
2021-11-17

Redox regulation in the brain Reactive oxygen species are generated in Edoxaban by the mitochondrial respiratory chain, which occurs on the inner mitochondrial membrane (Murphy, 2009, Jensen, 1966, Dickinson and Chang, 2011). Interestingly, although most cancer cells are thought to primarily rel
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KN-92 hydrochloride sale Acarbose and voglibose the classic
2021-11-17

Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug
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In summary this study shows
2021-11-17

In summary, this study shows that compound 4d has strong clinical potential as an efficient GLP-1/GCGR agonist exhibits weight-lowering, lipid-regulation and diabetes-protective effects and plays an important role in the prevention and therapy of diet induced obesity and dyslipidemia. The present st
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Retinal GAL receptor distribution suggests
2021-11-17

Retinal GAL receptor distribution suggests an intrinsic neuronal control since retina lacks an autonomic innervation, and a signal modulation seems most likely here, acting via GALR1 while GALR2 and GALR3 seem to play a rather minor role in this signal transduction. While sources acting on these ret
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KW 2449 VS strategies have been building
2021-11-17

VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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