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In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results.
TLDR
In vivo brain concentration ratios of mdr1a (-/-) to (+/+) CF-1 mice, either at a certain time point or up to 60 min, correlated well with the in vitro transcellular transport ratios from L-mdr 1a cells, indicating that, at least in mice, the in intestine data are valid predictors of the in vivo contribution of P-gp.
p62/Sqstm1 promotes malignancy of HCV-positive hepatocellular carcinoma through Nrf2-dependent metabolic reprogramming
TLDR
The data indicate that this Nrf2 inhibitor could be used to make cancer cells less resistant to anticancer drugs, especially in HCV-positive HCC patients.
A typical Y1 receptor regulates feeding behaviors: effects of a potent and selective Y1 antagonist, J-115814.
TLDR
It is certified that the Y1 receptor is a major feeding receptor of NPY by using the potent and selective Y1 antagonist J-115814 and concluding that theY1 receptor plays a key role in regulating food intake.
Substituent elimination from p-substituted phenols by cytochrome P450. ipso-Substitution by the oxygen atom of the active species.
TLDR
Experiments using 18O2 proved that the elimination is accompanied with ipso-substitution by the oxygen atom of the active species in cytochrome P450, and indicated that the mechanism of the substituent elimination can be divided into two types: the substitUent is eliminated as an anion or as a cation.
Effect of P-glycoprotein-mediated efflux on cerebrospinal fluid/plasma concentration ratio.
TLDR
The present study indicated that fp and PEI measurements may be useful in predicting in vivo CSF/plasma fractions for central nervous system-targeting drugs.
Evaluation of drug interactions with P-glycoprotein in drug discovery: in vitro assessment of the potential for drug-drug interactions with P-glycoprotein.
TLDR
This review will focus on the evaluation of drug candidates to assess the potential for drug interactions at the level of P-gp, the role ofP-gp in drug disposition, the biochemistry of P -gp efflux as it relates to model systems to study drug interactions with P-glycoprotein, and the implementation of p-gp assay models within the drug discovery process.
A neuropeptide Y Y5 antagonist selectively ameliorates body weight gain and associated parameters in diet-induced obese mice.
TLDR
Y5R is involved in the regulation and development of DIO and utility for Y5R antagonists in the treatment of obesity is suggested, as the compound did not affect DIO of Y 5R-deficient mice.
Novel metabolic pathway of estrone and 17beta-estradiol catalyzed by cytochrome P-450.
TLDR
The results show that estrone and 17beta-estadiol were converted into the corresponding quinols by CYP1A1, CYB2B6, and CYP2E1.
Pharmacokinetic and Pharmacodynamic Properties of the Glucokinase Activator MK-0941 in Rodent Models of Type 2 Diabetes and Healthy Dogs
TLDR
Key pharmacokinetic and pharmacodynamic findings from preclinical studies of the GKA 3-[[6-(ethylsulfonyl)-3-pyridinyl]oxy]-5-hydroxy-1-methylethoxy]-N-(1-methyl-1H-pyrazol-3-yl)benzamide support further investigation of MK-0941 as a potential therapeutic agent for treatment of type 2 diabetes.
Aromatic Substitution Reaction of 2-Chloropyridines Catalyzed by Microsomal Glutathione S-Transferase 1
TLDR
This work investigated the substitution reaction of a series of 2-chloropyridine derivatives catalyzed by rat liver microsomal glutathione S-transferase 1, finding the presence of a Meisenheimer complex and its influence on the reaction rate.
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