ADME/Tox Resources

Get the most out of your hepatic products through our protocols and user guides. Obtain the latest literature published by both Life Technologies scientists and thought leaders in the ADME/Tox research field.

DDI induction | Environmental tox | Toxicology | Drug metabolism |  Hepatocyte cell bio | Co-cultures

DDI induction

• Li Y, Zhou D, Ferguson SS, Dorff P, Simpson TR, Grimm SW. In Vitro Assessment of Metabolic Drug–Drug Interaction Potential of AZD2624, Neurokinin-3 Receptor Antagonist, Through Cytochrome P(450) Enzyme Identification, Inhibition, and Induction Studies. Xenobiotica. 2010 Nov;40(11):721-9.
• Li L, Hassan HE, Tolson AH, Ferguson SS, Eddington ND, Wang H. Differential Activation of Pregnane X Receptor and Constitutive Androstane Receptor by Buprenorphine in Primary Human Hepatocytes and HepG2 Cells. J Pharmacol Exp Ther. 2010 Sep.
• Rana R, Chen Y, Ferguson SS, Kissling GE, Surapureddi S. Hepatocyte Nuclear Factor 4alpha Regulates Rifampicin-Mediated Induction of CYP2C Genes in Primary Cultures of Human Hepatocytes. Drug Metab Dispos. 2010 Apr;38(4):591-9. 
• Lau AJ, Yang G, Rajaraman G, Baucom CC, Chang TK. Differential Effect of Meclizine on the Activity of Human Pregnane X Receptor and Constitutive Androstane Receptor. J Pharmacol Exp Ther. 2010 Dec.
• Lau AJ, Yang G, Rajaraman G, Baucom CC, Chang TK. Human Pregnane X Receptor Agonism by Ginkgo Biloba Extract: Assessment of the Role of Individual Ginkgolides. J Pharmacol Exp Ther. 2010 Dec;335(3):771-80.
• Graham RA, Tyler LO, Krol WL, Silver IS, Webster LO. Temporal Kinetics and Concentration-Response Relationships for Induction of CYP1A, CYP2B, and CYP3A in Primary Cultures of Beagle Dog Hepatocytes. J Biochem Mol Toxicol. 2006;20(2):69-78.
• Faucette SR, Sueyoshi T, Smith CM, Negishi M, Lecluyse EL. Differential Regulation of Hepatic CYP2B6 and CYP3A4 Genes by Constitutive Androstane Receptor but Not Pregnane X Receptor. J Pharmacol Exp Ther. 2006 Jun;317(3):1200-9.
• Ferguson SS, Chen Y, LeCluyse EL, Negishi M, Goldstein JA. Mol Pharmacol. Human CYP2C8 is Transcriptionally Regulated by the Nuclear Receptors Constitutive Androstane Receptor, Pregnane X Receptor, Glucocorticoid Receptor, and Hepatic Nuclear Factor 4alpha. 2005 Sept;68(3):747-57.
• Smith CM, Graham RA, Krol WL, Silver IS, Negishi M. Differential UGT1A1 Induction by Chrysin in Primary Human Hepatocytes and HepG2 Cells. J Pharmacol Exp Ther. 2005 Dec;315(3):1256-64.
• Madan A, Graham RA, Carroll KM, Mudra DR, Burton LA. Effects of Prototypical Microsomal Enzyme Inducers on Cytochrome P450 Expression in Cultured Human Hepatocytes. Drug Metab Dispos. 2003 Apr;31(4):421-31.
• Wang H, LeCluyse EL. Role of Orphan Nuclear Receptors in the Regulation of Drug-Metabolising Enzymes. Clin Pharmacokinet. 2003;42(15):1331-57.
• LeCluyse EL. Pregnane X Receptor: Molecular Basis for Species Differences in CYP3A Induction by Xenobiotics. Chem Biol Interact. 2001 May 16;134(3):283-9.
• LeCluyse E, Madan A, Hamilton G, Carroll K, DeHaan R. Expression and Regulation of Cytochrome P450 Enzymes in Primary Cultures of Human Hepatocytes. J Biochem Mol Toxicol. 2000;14(4):177-88.
• McCune JS, Hawke RL, LeCluyse EL, Gillenwater HH, Hamilton G. In Vivo and In Vitro Induction of Human Cytochrome P4503A4 by Dexamethasone. Clin Pharmacol Ther. 2000 Oct;68(4):356-66.

Environmental tox

• Budinsky RA, LeCluyse EL, Ferguson SS, Rowlands JC, Simon T. Human and Rat Primary Hepatocyte CYP1A1 and 1A2 Induction with 2,3,7,8-Tetrachlorodibenzo-p-dioxin, 2,3,7,8-Tetrachlorodibenzofuran, and 2,3,4,7,8-Pentachlorodibenzofuran. Toxicol Sci. 2010 Nov;118(1):224-35.
• Rotroff D, Beam A, Freeman K, Farmer A, Bondell H. Xenobiotic Metabolizing Enzyme and Transporter Gene Expression in Primary Cultures of Human Hepatocytes Modulated by ToxCast Chemicals. J Toxicol Environ Health B Crit Rev. 2010 Feb;13(2-4):329-46.
• Rotroff DM, Wetmore BA, Dix DJ, Ferguson SS, Clewell HJ. Incorporating Human Dosimetry and Exposure into High-Throughput In Vitro Toxicity Screening. Toxicol Sci. 2010 Oct;117(2):348-58.

Toxicology

• LeCluyse EL, Witek RP, Andersen ME, Powers MJ. Organotypic liver culture models: Meeting current challenges in toxicity testing. Critical Reviews in Toxicology. 2012 Early online 1-48
• Martinez SM, Bradford BU, Soldatow VY, Kosyk O, Sandot A. Evaluation of an In Vitro Toxicogenetic Mouse Model for Hepatotoxicity. Toxicol Appl Pharmacol. 2010 Dec 15;249(3):208-16.

Drug metabolism

• Sahi J, Grepper S, Smith C. Hepatocytes as a Tool in Drug Metabolism, Transport and Safety Evaluations in Drug Discovery. Curr Drug Discov Technol. 2010 Sep;7(3):188-98.
• Hewitt NJ, Lechón MJ, Houston JB, Hallifax D, Brown HS. Primary Hepatocytes: Current Understanding of the Regulation of Metabolic Enzymes and Transporter Proteins, and Pharmaceutical Practice for the Use of Hepatocytes in Metabolism, Enzyme Induction, Transporter, Clearance, and Hepatotoxicity Studies. Drug Metab Rev. 2007;39(1):159-234.

Hepatocyte cell biology

• LeCluyse EL, Alexandre E. Isolation and Culture of Primary Hepatocytes from Resected Human Liver Tissue. Methods Mol Biol. 2010;640:57-82.

Co-cultures

• Sunman JA, Hawke RL, LeCluyse EL, Kashuba AD. Kupffer Cell-Mediated IL-2 Suppression of CYP3A Activity in Human Hepatocytes. Drug Metab Dispos. 2004 Mar;32(3):359-63.