Enzyme Inhibition/Inactivation

Automated 384-Well Cell-Based Cytochrome P450 Inhibition Assays using Cryopreserved Hepatocytes in Suspension
Bradley R. Larson, BioTek Instruments; Peter Banks, BioTek Instruments; Timothy A. Moeller, Celsis In Vitro Technologies; Tracy Worzella, Promega Corporation; Mary Sobol, Promega Corporation; Dongping Ma, Promega Corporation
Can Ki values for direct inhibition of CYP enzymes can be reliably estimated from IC50 values?
Lois J. Haupt, XenoTech, LLC; Faraz Kazmi, XenoTech, LLC; Brian Smith, XenoTech, LLC; Sarah Leatherman, XenoTech, LLC; Andrew Parkinson, XenoTech, LLC
Choice Of Solvent For Fluorimetric IC50 Assays With Bactosomes Can Influence The End Result
Caroline F. Peet, Cypex Ltd; Anna W Kaaz, Cypex Ltd; Michael W Voice, Cypex Ltd; Michael P Pritchard, Cypex Ltd
Dichloroacetate-dependent inactivation of GSTZ1 in human liver cytosol is modulated by physiologically important anions in a GSTZ1 haplotype-dependent manner
Margaret O. James, University of Florida; Wenjun Li, University of Florida; Yuan Gu, University of Florida; Taimour Langaee, University of Florida; Peter W. Stacpoole, University of Florida
Esomeprazole and omeprazole sulfone are in vitro metabolism-dependent inactivators of CYP2C19: Determination of KI and kinact values
Brian W. Ogilvie, XenoTech, LLC; Paul Toren, XenoTech, LLC; Faraz Kazmi, XenoTech, LLC; Andrew Parkinson, XenoTech, LLC
Evaluation of Mechanism Based CYP 450 3A Drug Interaction in Rats
Vishwottam Kandikere, Suven Life Sciences Ltd; Gopinadh Bhyrapuneni, Suven Life Sciences Ltd; Nageswararao Muddana, Suven Life Sciences Ltd; Veera Raghava Chowdary Palacharla, Suven Life Sciences Ltd; Nilkanth Naik, Suven Life Sciences Ltd; Ramoji Kosuru, Suven Life Sciences Ltd; Shantaveer Irappanavar, Suven Life Sciences Ltd; Ramakrishna Nirogi, Suven Life Sciences Ltd
Evaluation of dilution, dialysis and ultracentrifugation methods to assess the reversibility of metabolism-dependent inhibitors (MDIs) of cytochrome P450 (CYP) enzymes
David B. Buckley, XenoTech, LLC; Faraz Kazmi, XenoTech, LLC; Phyllis Yerino, XenoTech, LLC; Brian Ogilivie, XenoTech, LLC; Andrew Parkinson, XenoTech, LLC
Inhibitory Effect of Chinese Herbal Extracts on the Activities of Human Cytochrome P450 Enzymes In Vitro
Yan Li, Institute of Materia Medica, Chinese Academy of Medical Sciences; Jiangong Shi, Institute of Materia Medica, Chinese Academy of Medical Sciences; Shen Lin, Institute of Materia Medica, Chinese Academy of Medical Sciences; Qinghao Zhang, Institute of Materia Medica, Chinese Academy of Medical Sciences; Baolian Wang, Institute of Materia Medica, Chinese Academy of Medical Sciences; Caroline A. Lee, Pfizer Inc.; R. Scott Obach, Pfizer Inc.; Teresa A. Smolarek, Pfizer Inc.; Jenny Y. Zheng, Pfizer (China)
Studies to Further Investigate the Inhibition of Human Liver Microsomal Cytochrome P450 2C8 (CYP2C8) by the Acyl--Glucuronide of Gemfibrozil
Susan M. Jenkins, Bristol-Myers Squibb Company; Tatyana Zvyaga, Bristol-Myers Squibb Company; Stephen Johnson, Bristol-Myers Squibb Company; Jeremy Hurley, Bristol-Myers Squibb Company; Andrew Wagner, Bristol-Myers Squibb Company; Richard Burrell, Bristol-Myers Squibb Company; Wesley Turley, Bristol-Myers Squibb Company; John E. Leet, Bristol-Myers Squibb Company; Thomas Philip, Bristol-Myers Squibb Company; A. David Rodrigues, Bristol-Myers Squibb Company
The Length of Preincubation Times in Abbreviated Cytochrome P450 Time-Dependent Inhibition Studies: One size fits all?
David M. Stresser, BD Biosciences Discovery Labware; Andrew K Mason, BD Biosciences Discovery Labware; Charles L. Crespi, BD Biosciences Discovery Labware; Elke S. Perloff, BD Gentest SM Contract Research Services
Use of dialysis to differentiate between reversible and mechanism-based CYP inhibition
Stephen Madden, Charles River Laboratories; Jon Welch, Charles River Laboratories; Alison Meechan, Charles River Laboratories