<p>Although parallel synthesis combined with high-throughput screening has made it easier to generate highly potent drug candidates, many of these compounds never make the grade because they either prove to be unsafe or lack the necessary physicochemical and pharmacokinetic properties. In Optimizati
Optimization in drug discovery: in vitro methods
β Scribed by Caldwell, Gary;Yan, Zhengyin
- Publisher
- Humana Press
- Year
- 2004
- Tongue
- English
- Leaves
- 425
- Series
- Methods in pharmacology and toxicology
- Category
- Library
No coin nor oath required. For personal study only.
β¦ Synopsis
Isothermal titration calorimetry characterization of drug-binding energetics to blood proteins / Gary W. Caldwell and Zhengyin Yan -- Metabolic stability assessed by liver microsomes and hepatocytes / David C. Ackley, Kevin T. Rockich, and Timothy R. Baker -- In vitro drug metabolite profiling using hepatic S9 and human liver microsomes / Wu-Nan Wu and Linda A. McKown.;In vitro identification of UDP-glucuronosyltransferases involved in drug metabolism / Michael H. Court -- In vitro CYP induction in human hepatocytes / Daniel R. Mudra and Andrew Parkinson -- High-throughput screening of human cytochrome P450 inhibitors using fluorometric substrates: methodology for 25 enzyme/substrate pairs / David M. Stresser -- Evaluation of cytochrome P450 inhibition in human liver microsomes / Zhengyin Yan and Gary W. Caldwell -- Identification of CYP mechanism-based inhibitors / Amin A. Nomeir, Jairam Palamanda, and Leonard Favreau.;pKa, solubility and lipophilicity: assessing physicochemical properties of lead compounds / Yushen Guo and Hong Shen -- Use of caco-2 cell monolayers to study drug absorption and metabolism / Ming Hu [and others] -- Absorption screening using the PAMPA approach / Jeffrey A. Ruell and Alex Avdeef -- In situ single-pass perfused rat intestinal model for absorption and metabolism / Eun Ju Jeong [and others] -- In vitro permeation study with bovine brain microvessel endothelial cells / Sung-Hack Lee [and others] -- An enzymatic microplate assay for testing P-glycoprotein substrates and inhibitors / S. Orlowski, J. Nugier and Eric Ezan -- Evaluation of drug-transporter interactions using in vitro cell models / Yaming Su and Patrick J. Sinko -- Plasma protein-binding methods in drug discovery / Lucinda H. Cohen.;Detection of DNA adducts by 32P-postlabeling analysis / Naomi Suzuki, Padmaja M. Prabhu, and Shinya Shibutani -- Covalent DNA adduct formation mediated by cytochrome P450 / Marie StiborovΓ‘ -- Application of in vitro comet assay for genotoxicity testing / Bojana Zegura and Metka Filipic -- Assessing DNA damage using a reporter gene system / Xuming Jia and Wei Xiao -- Improvement of the Ames test using human liver S9 preparation / Atsushi Hakura, Satoshi Suzuki, and Tetsuo Satoh -- Screening for chemical mutagens using the mouse lymphoma assay / Tao Chen and Martha M. Moore -- A high throughput binding assay for HERG / Keith Finlayson and John Sharkey -- In vitro drug metabolism: thiol conjugation / Wei Tang and Randy R. Miller -- In vitro screening assay of the reactivity of acyl glucuronides / SΓ©bastien Bolze.
β¦ Table of Contents
pKa, solubility and lipophilicity: assessing physicochemical properties of lead compounds / Yushen Guo and Hong Shen --
Use of caco-2 cell monolayers to study drug absorption and metabolism / Ming Hu [and others] --
Absorption screening using the PAMPA approach / Jeffrey A. Ruell and Alex Avdeef --
In situ single-pass perfused rat intestinal model for absorption and metabolism / Eun Ju Jeong [and others] --
In vitro permeation study with bovine brain microvessel endothelial cells / Sung-Hack Lee [and others] --
An enzymatic microplate assay for testing P-glycoprotein substrates and inhibitors / S. Orlowski, J. Nugier and Eric Ezan --
Evaluation of drug-transporter interactions using in vitro cell models / Yaming Su and Patrick J. Sinko --
Plasma protein-binding methods in drug discovery / Lucinda H. Cohen. Isothermal titration calorimetry characterization of drug-binding energetics to blood proteins / Gary W. Caldwell and Zhengyin Yan --
Metabolic stability assessed by liver microsomes and hepatocytes / David C. Ackley, Kevin T. Rockich, and Timothy R. Baker --
In vitro drug metabolite profiling using hepatic S9 and human liver microsomes / Wu-Nan Wu and Linda A. McKown. In vitro identification of UDP-glucuronosyltransferases involved in drug metabolism / Michael H. Court --
In vitro CYP induction in human hepatocytes / Daniel R. Mudra and Andrew Parkinson --
High-throughput screening of human cytochrome P450 inhibitors using fluorometric substrates: methodology for 25 enzyme/substrate pairs / David M. Stresser --
Evaluation of cytochrome P450 inhibition in human liver microsomes / Zhengyin Yan and Gary W. Caldwell --
Identification of CYP mechanism-based inhibitors / Amin A. Nomeir, Jairam Palamanda, and Leonard Favreau. Detection of DNA adducts by 32P-postlabeling analysis / Naomi Suzuki, Padmaja M. Prabhu, and Shinya Shibutani --
Covalent DNA adduct formation mediated by cytochrome P450 / Marie StiborovaΜ --
Application of in vitro comet assay for genotoxicity testing / Bojana Zegura and Metka Filipic --
Assessing DNA damage using a reporter gene system / Xuming Jia and Wei Xiao --
Improvement of the Ames test using human liver S9 preparation / Atsushi Hakura, Satoshi Suzuki, and Tetsuo Satoh --
Screening for chemical mutagens using the mouse lymphoma assay / Tao Chen and Martha M. Moore --
A high throughput binding assay for HERG / Keith Finlayson and John Sharkey --
In vitro drug metabolism: thiol conjugation / Wei Tang and Randy R. Miller --
In vitro screening assay of the reactivity of acyl glucuronides / SeΜbastien Bolze.
β¦ Subjects
Biochimie physique;Chimie pharmaceutique;Drug Evaluation, Preclinical--methods;Drugs--Testing;MΓ©dicaments--Essais cliniques;Pharmaceutical chemistry;Physical biochemistry;Laboratory manuals;Pharmaceutical chemistry -- Laboratory manuals;Physical biochemistry -- Laboratory manuals;Drugs -- Testing -- Laboratory manuals;Drug Evaluation, Preclinical -- methods;Chimie pharmaceutique -- Manuels de laboratoire;Biochimie physique -- Manuels de laboratoire;MeΜdicaments -- Essais cliniques -- Manuels de
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