Optimization in Drug Discovery

'1. Small Molecule Formulation Screening Strategies in Drug DiscoveryGary W. Caldwell, Becki Hasting, John Masucci, and Zhengyin Yan2. Assessment of Drug Plasma Protein Binding in Drug DiscoveryDennis Kalamaridis and Nayan Patel3. Drug Partition in Red Blood CellsDennis Kalamaridis and Karen DiLoreto4. Permeability Assessment Using 5-Day Cultured Caco-2 Cell MonolayersGary W. Caldwell, Chrissa Ferguson, Robyn Buerger, Lovonia Kulp, and Zhengyin Yan5. In Situ Single Pass Perfused Rat Intestinal ModelMaria Markowska and L. Mark Kao6. Metabolic Stability Assessed by Liver Microsomes and HepatocytesKevin J. Coe and Tatiana Koudriakova7. Metabolic Assessment in Alamethicin-Activated Liver Microsomes: Co-Activating CYPs and UGTsGary W. Caldwell and Zhengyin Yan8. Phenotyping UDP-Glucuronosyltransferases (UGTs) Involved in Human Drug Metabolism: An UpdateMichael H. Court9. In Vitro CYP/FMO Reaction PhenotypingCarlo Sensenhauser10. Human Pregnane X Receptor (hPXR) Activation Assay in Stable Cell LinesJudy L. Raucy11. Characterization of Constitutive Androstane Receptor (CAR) ActivationCaitlin Lynch, Haishan Li, and Hongbing Wang12. DNA Binding (Gel Retardation Assay) Analysis for Identification of Aryl Hydrocarbon (Ah) Receptor Agonists and AntagonistsAnatoly A. Soshilov and Michael S. Denison13. Cell-Based Assays for Identification of Aryl Hydrocarbon Receptor (AhR) ActivatorsGuochun He, Jing Zhao, Jennifer C. Brennan, Alessandra A. Affatato, Bin Zhao, Robert H. Rice, and Michael S. Denison14. In Vitro CYP Induction Using Human HepatocytesMonica Singer, Carlo Sensenhauser, and Shannon Dallas15. Assessment of CYP3A4 Time-Dependent Inhibition in Plated and Suspended Human HepatocytesJ. George Zhang and David M. Stresser16. Evaluation of Time-Dependent CYP3A4 Inhibition Using Human HepatocytesYuan Chen and Adrian J. Fretland17. Rapidly Distinguishing Reversible and Time-Dependent CYP450 Inhibition Using Human Liver Microsomes, Co-Incubation, and Continuous Fluorometric Kinetic AnalysesGary W. Caldwell and Zhengyin Yan18. Identification of Time-Dependent CYP Inhibitors Using Human Liver Microsomes (HLM)Kevin J. Coe, Judith Skaptason, and Tatiana Koudriakova19. CYP Time-Dependent Inhibition (TDI) Using an IC 50 Shift Assay with Stable Isotopic Labeled Substrate Probes to Facilitate Liquid Chromatography/Mass Spectrometry AnalysesGary W. Caldwell and Zhengyin Yan20. Screening for P-Glycoprotein (Pgp) Substrates and InhibitorsQing Wang and Tina M. Sauerwald21. In Vitro Characterization of Intestinal Transporter, Breast Cancer Resistance Protein (BCRP)Chris Bode and Li-Bin Li22. In Vitro Characterization of Intestinal and Hepatic Transporters: MRP2Ravindra Varma Alluri, Peter Ward, Jeevan Kunta, Brian C. Ferslew, Dhiren R. Thakker, and Shannon Dallas23. In Vitro Characterization of Hepatic Transporters OATP1B1 and OATP1B3Blair Miezeiewski and Allison McLaughlin24. In Vitro Characterization of Renal Transporters OAT1, OAT3, and OCT2Ying Wang and Nicole Behler25. General Guidelines for Setting Up an In Vitro LC/MS/MS AssayJohn A. Masucci and Gary W. Caldwell26. Metabolite Identification in Drug DiscoveryWing W. Lam, Jie Chen, Rongfang Fran Xu, Jose Silva, and Heng-Keang Lim27. Drug, Lipid, and Acylcarnitine Profiling Using Dried Blood Spot (DBS) Technology in Drug DiscoveryWensheng Lang, Jenson Qi, and Gary W. Caldwell28. In Vitro Trapping and Screening of Reactive Metabolites Using Liquid Chromatography-Mass SpectrometryZhengyin Yan and Gary W. Caldwell29. Quantitative Assessment of Reactive MetabolitesJie Chen, Rongfang Fran Xu, Wing W. Lam, Jose Silva, and Heng Keang Lim30. In Vitro Assessment of the Reactivity of Acyl GlucuronidesRongfang Fran Xu, Wing W. Lam, Jie Chen, Michael McMillian, Jose Silva, and Hen... Mehr