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There is no doubt that GPR is a LPI receptor
2022-10-10

There is no doubt that GPR55 is a LPI receptor; however, we should re-consider whether or not GPR55 is in fact another cannabinoid receptor. The pharmacologies of the GPR55 and CB1 receptors are complicated; CB1 inverse agonist/antagonists SR141716A (rimonabant) and AM251 were shown to be potent ago
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br Experimental br Acknowledgments This research was
2022-10-10

Experimental Acknowledgments This research was supported by the Korea Research Foundation (2013R1A1A2007509). The authors thank to Dr. Moon Ho Son (Dong-A Pharm. Co. Ltd) for hGPR119 agonist activity assay. We also thank to Pharmacal Research Institute and Central Laboratory of Kangwon Nationa
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As preclinical toxicity and efficacy both appear to be assoc
2022-10-10

As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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br Introduction Herpes viruses are members of
2022-10-10

Introduction Herpes viruses are members of Herpesviridae family. This family consists of DNA viruses and it is a very large family. The viruses related to this family cause many diseases in animals and humans [1]. Herpes simplex viruses cause mucocutaneous lesions in the affected humans. These le
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In the liver ghrelin has opposite effects to
2022-10-09

In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty STF 083010 oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de novo in a GH-independent
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br Presenilins in protein trafficking proteolysis and degrad
2022-10-09

Presenilins in protein trafficking, proteolysis and degradation An obvious explanation for the role of presenilins and γ-secretase in protein trafficking and degradation is that many reported γ-secretase substrates are functionally involved in protein transport. For example, members of the mammal
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More polar substituents introduced on
2022-10-09

More polar substituents introduced on the 5-position of the aniline ring (e.g., dimethyl amine in ) decreased the lipophilicity of the compounds (4.3 for vs 5.1 for ), but did not affect their potency. For instance, was highly potent in vitro and demonstrated a surprising 51% lowering of Aβ42 in m
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chemokine receptor antagonist br FXR expression in normal in
2022-10-08

FXR chemokine receptor antagonist 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., 201
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All of the abovementioned effects of PUFAs signal their invo
2022-10-08

All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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The pharmacokinetic properties of were amenable to
2022-10-08

The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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br Materials and methods br Results br Discussion The distri
2022-10-08

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 Reparixin sale [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract, adip
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Remarkably most of these molecules are also quite effective
2022-10-08

Remarkably, most of these molecules are also quite effective in interfering with the proliferation of the drug-resistant cancer cell lines, with IC50 values ranging from 0.59 to 2.93 μM against MCF-7/ADR cells, and from 0.160 to 1.17 μM against NSCLC-resistant H1975 cells. Among these molecules, com
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br Interference in coagulation assays Conversely to heparin
2022-10-08

Interference in coagulation assays Conversely to heparin, or heparin like [Ala92]-p16 (84-103) (LMWH, Fondaparinux, Sodium Danaparoid), which are catalytic inhibitors requiring the presence of AT for their activity, as depicted on Fig. 2, DiXaIs are directly targeted to Factor Xa, and are revers
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br Experimental procedures br Conflicts of interests br
2022-10-08

Experimental procedures Conflicts of interests Introduction Here we investigate differences in growth properties and short-term morphological changes in response to ET-1 in Chinese hamster ovary (CHO) cells stably and separately expressing ETA or ETB receptors. A stably transfected CHO syst
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br Introduction Chronic hepatitis C CHC caused by hepatitis
2022-10-04

Introduction Chronic hepatitis C (CHC) caused by hepatitis C virus (HCV) infection affects approximately 170 million individuals worldwide [1]. HCV and human immunodeficiency virus (HIV) have similar routes of transmission, including blood-to-blood contact, sharing of injection equipment, and sex
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