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Abstract CYP3A4, the predominant but variably expressed cytochrome P450 of adult human liver, is subject to multifaceted constitutive regulation as well as transcriptional induction by a variety of structurally unrelated xenobiotics. Using transient transfections in HepG2 cells, we previously...
Abstract Phenobarbital (PB) treatment impairs the biliary excretion of some organic anions. One mechanism may involve direct competition for biliary excretion by PB and/or a PB metabolite. Alternatively, PB may alter the expression and/or function of hepatic organic anion transport proteins. The...
Abstract Rel/nuclear factor-κB (NF-κB) transcription factors control a variety of cellular processes, such as cell growth and apoptosis, and are continually activated in many human diseases, including chronic inflammatory diseases and cancer. Jesterone dimer (JD) is a synthetic derivative of...
Abstract The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid subtype of ionotropic glutamate receptors consists of rapidly gating ion channels. Positive modulation of channel gating may slow gating kinetics through at least two distinct mechanisms, evidenced by the predominant slowing of...
Abstract KCNQ1 channels underlie the slow delayed rectifier K + current, mediate repolarization of cardiac action potentials, and are a potential therapeutic target for treatment of arrhythmia. ( E )-(+)- N -(3 R...
Abstract Arylamine N -acetyltransferases (NATs) catalyze the biotransformation of a variety of arylamine drugs and carcinogens and may play diametrically opposing roles in enhancing either the detoxification of these chemicals or their metabolic activation into DNA-binding electrophiles. To...
Abstract The human 5-hydroxytryptamine-2C (5-HT 2C ) receptor has been the target of potential anxiolytics and antiobesity drugs, and its positive allosteric modulator was discovered to be l - threo -α- d -galacto-octopyranoside,...
Abstract Treatment of rats with peroxisome proliferators is known to affect gene expression, including suppression of CYP2C11. The current study examined the mechanism of negative regulation of CYP2C11 , comparing the effects of a classic peroxisome proliferator, nafenopin, with those of the...
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