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The Resource Optimization in drug discovery : in vitro methods, edited by Zhengyin Yan, Gary W. Caldwell

Optimization in drug discovery : in vitro methods, edited by Zhengyin Yan, Gary W. Caldwell

Label
Optimization in drug discovery : in vitro methods
Title
Optimization in drug discovery
Title remainder
in vitro methods
Statement of responsibility
edited by Zhengyin Yan, Gary W. Caldwell
Contributor
Subject
Genre
Language
eng
Summary
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 Optimization in Drug Discovery: In Vitro Methods, a panel of researchers and experts from leading universities and major pharmaceutical companies from all over the world provide proven solutions to this expensive problem with a collection of cutting-edge experimental protocols for early in vitro evaluation of new chemical entities (NCE). These readily reproducible assays measure such critical parameters as physicochemical properties, adsorption, plasma binding, metabolism, drug interactions, and toxicity. All protocols follow the successful Methods in Molecular Biology{u2122} series format, each one offering step-by-step laboratory instructions, an introduction outlining the principle behind the technique, lists of equipment and reagents, and tips on troubleshooting and avoiding known pitfalls. Comprehensive and highly practical, Optimization in Drug Discovery: In Vitro Methods systematically collects and describes the key methods for uncovering-as early in the discovery stage as possible-those defects that can eliminate candidate drugs from preclinical and clinical development
Member of
Cataloging source
COO
Dewey number
615/.19/0072
Illustrations
illustrations
Index
index present
Language note
English
LC call number
RS407
LC item number
.O66 2004
Literary form
non fiction
Nature of contents
  • dictionaries
  • bibliography
NLM call number
  • 2004 L-127
  • QV 771
NLM item number
O62 2004
http://library.link/vocab/relatedWorkOrContributorDate
1953-
http://library.link/vocab/relatedWorkOrContributorName
  • Yan, Zhengyin
  • Caldwell, Gary
Series statement
Methods in pharmacology and toxicology
http://library.link/vocab/subjectName
  • Pharmaceutical chemistry
  • Physical biochemistry
  • Drugs
  • Drug Evaluation, Preclinical
  • MEDICAL
  • MEDICAL
  • MEDICAL
  • MEDICAL
  • Drugs
  • Pharmaceutical chemistry
  • Physical biochemistry
Label
Optimization in drug discovery : in vitro methods, edited by Zhengyin Yan, Gary W. Caldwell
Instantiates
Publication
Bibliography note
Includes bibliographical references and index
Carrier category
online resource
Carrier category code
  • cr
Carrier MARC source
rdacarrier
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent
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 Stiborová -- 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 / Sébastien Bolze
Control code
61354687
Dimensions
unknown
Extent
1 online resource (xv, 418 pages)
Form of item
online
Isbn
9781588293329
Media category
computer
Media MARC source
rdamedia
Media type code
  • c
Other physical details
illustrations
Specific material designation
remote
System control number
(OCoLC)61354687
Label
Optimization in drug discovery : in vitro methods, edited by Zhengyin Yan, Gary W. Caldwell
Publication
Bibliography note
Includes bibliographical references and index
Carrier category
online resource
Carrier category code
  • cr
Carrier MARC source
rdacarrier
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent
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 Stiborová -- 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 / Sébastien Bolze
Control code
61354687
Dimensions
unknown
Extent
1 online resource (xv, 418 pages)
Form of item
online
Isbn
9781588293329
Media category
computer
Media MARC source
rdamedia
Media type code
  • c
Other physical details
illustrations
Specific material designation
remote
System control number
(OCoLC)61354687

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