Selective phthalate activation of naturally occurring human constitutive androstane receptor splice variants and the pregnane X receptor

JG DeKeyser, EM Laurenzana… - Toxicological …, 2011 - academic.oup.com
Phthalates and other endocrine-disruptive chemicals are manufactured in large quantities
for use as plasticizers and other commercial applications, resulting in ubiquitous human …

Di (2-ethylhexyl) phthalate is a highly potent agonist for the human constitutive androstane receptor splice variant CAR2

JG DeKeyser, MC Stagliano, SS Auerbach… - Molecular …, 2009 - ASPET
… In separate experiments (DeKeyser et al., manuscript in preparation), we demonstrated that
no … assistance of Denise Weyant and thank Matthew DeKeyser for graphical assistance. …

Considerations from the innovation and quality induction working group in response to drug-drug interaction guidances from regulatory agencies: focus on CYP3A4 …

…, M Mohutsky, HJ Einolf, L Chen, JG Dekeyser… - Drug Metabolism and …, 2018 - ASPET
The Innovation and Quality Induction Working Group presents an assessment of best practice
for data interpretation of in vitro induction, specifically, response thresholds, variability, …

Considerations from the IQ induction working group in response to drug-drug interaction guidance from regulatory agencies: focus on downregulation, CYP2C …

…, D Ramsden, J Palamanda, JG Dekeyser… - Drug Metabolism and …, 2017 - ASPET
The European Medicines Agency (EMA), the Pharmaceutical and Medical Devices Agency (PMDA),
and the Food and Drug Administration (FDA) have issued guidelines for the conduct …

CAR2 displays unique ligand binding and RXRα heterodimerization characteristics

SS Auerbach, JG DeKeyser, MA Stoner… - Drug metabolism and …, 2007 - ASPET
The constitutive androstane receptor (CAR; NR1I3) regulates the expression of genes involved
in xenobiotic metabolism. Alternative splicing of the human CAR gene yields an array of …

Bioassay‐directed fractionation for discovery of bioactive neutral lipids guided by relative mass defect filtering and multiplexed collision‐induced dissociation

MC Stagliano, JG DeKeyser… - Rapid …, 2010 - Wiley Online Library
We report a synergistic method using bioassay‐directed liquid chromatography fractionation
and time‐of‐flight mass spectrometry to guide and accelerate bioactive compound discovery…

Studies on titin PEVK peptides and their interaction

Y Duan, JG DeKeyser, S Damodaran… - Archives of biochemistry …, 2006 - Elsevier
Experiments were conducted on several synthetic and expressed peptides from the PEVK
region of titin, the giant muscle protein. Different secondary structure prediction methods …

Species differences of drug‐metabolizing enzymes

JG DeKeyser, M Shou - Encyclopedia of drug metabolism and …, 2011 - Wiley Online Library
The prediction of human pharmacokinetics, efficacy, and toxicity from preclinical data
remains an important goal in the drug discovery and development process to minimize risk to …

Enzyme Induction Studies in Drug Discovery and Development

JG Dekeyser, JL Wahlstrom - Handbook of Drug Metabolism, Third …, 2019 - taylorfrancis.com
Changes in the expression of absorption, distribution, metabolism and excretion (ADME)
genes can impact the pharmacokinetics of many small molecule drugs. This chapter aims to …

[PDF][PDF] CAR2 displays unique ligand binding and RXRα heterodimerization characteristics

JG Dekeyser, SS Auerbach, MA Stoner, CJ Omiecinski - 2007 - Citeseer
The constitutive androstane receptor (CAR, NR1I3) regulates the expression of genes involved
in all phases of xenobiotic metabolism. Alternative splicing of the human CAR transcript …