Pharmaceutical profiling in drug discovery for lead selection:
Gespeichert in:
| Format: | Buch |
|---|---|
| Sprache: | English |
| Veröffentlicht: |
Arlington, VA
AAPS Press
2004
|
| Schriftenreihe: | Biotechnology: pharmaceutical aspects ;1
1 |
| Schlagworte: | |
| Online-Zugang: | Publisher description Inhaltsverzeichnis |
| Beschreibung: | Includes bibliographical references and index |
| Beschreibung: | XIII, 482 S. Ill., graph. Darst. 26 cm |
| ISBN: | 0971176795 |
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Datensatz im Suchindex
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| adam_text | PHARMACEUTICAL PROFILING IN DRUG DISCOVERY FOR LEAD SELECTION RONALD T.
BORCHARDT UNIVERSITY OF KANSAS EDWARD H. KERNS WYETH RESEARCH
CHRISTOPHER A. LIPINSKI PFIZER GLOBAL R&D (RETIRED) DHIREN R. THAKKER
UNIVERSITY OF NORTH CAROLINA BINGHE WANG GEORGIA STATE UNIVERSITY
AMERICAN ASSOCIATION OF PHARMACEUTICAL SCIENTISTS ARLINGTON, VA CONTENTS
PREFACE XI PARTI IN SILICO TOOLS 1 1. ABSORPTION PREDICTION 3 PER
ARTURSSON AND PAR MATSSON 2. PREDICTING MOLECULAR PHYSICAL PROPERTIES 27
ROBERT S. DEWITTE AND ED KOLOVANOV 3. IN SILICO TRANSPORTER MODELING AND
ITS APPLICATION IN DRUG DISCOVERY 53 ANNE HERSEY, CHRIS LUSCOMBE, AND
SANDEEP MODI 4. MODELS FOR CYTOCHROME P450-MEDIATED METABOLISM 69 K.R.
KORZEKWA, T.J. EWING, J.P. KOCHER, AND T.J. CARLSON 5. FUTURE OF IN
SILICO METHODS IN TOXICOLOGY 81 DAVID E. PATTERSON AND MICHAEL R.
BERTHOLD PART II PHYSICOCHEMICAL TOOLS 91 1. SOLUBILITY IN WATER AND
DMSO: ISSUES AND POTENTIAL SOLUTIONS 93 CHRISTOPHER A. LIPINSKI 2.
MEASUREMENTS OF LIPOPHILICITY AND ACID/BASE CHARACTER USING HPLC METHODS
127 KLDRA VALKO 3. HOW DO WE STUDY OXIDATIVE CHEMICAL STABILITY IN
DISCOVERY? SOME IDEAS, TRIALS, AND OUTCOMES 183 FRANCO LOMBARDO AND GUS
CAMPOS VU VIII CONTENTS PART III PERMEABILITY TOOLS 195 1.
PHYSICOCHEMICAL METHODS FOR ESTIMATING PERMEABILITY AND RELATED
PROPERTIES 197 M. KANSY, H. FISCHER, $. BENDELS, B. WAGNER, F SENNER, I.
PARRILLA, AND V. MICALLEF 2. CULTURED EPITHELIAL CELL ASSAYS USED TO
ESTIMATE INTESTINAL ABSORPTION POTENTIAL 217 ISMAEL J. HIDALGO, KATHRYN
WEINSTEIN, PAULA KARDOS, AND ROBERT STRAB 3. IN VITRO CELL-BASED ASSAYS
FOR ESTIMATING THE EFFECTS OF EFFLUX TRANSPORTERS ON CELL PERMEATION 235
JOSEPH W. POLLI AND COSETTE J. SERABJIT-SINGH PART IV ABSORPTION,
DISTRIBUTION, METABOLISM, AND EXCRETION TOOLS 257 1. IN VITRO MODELS FOR
ESTIMATING HEPATOBILIARY CLEARANCE 259 MADE] J. ZAMEK-GHSZCZYNSKI AND
KIM L.R. BROUWER 2. CHALLENGES IN DRUG DISCOVERY; LEAD OPTIMIZATION AND
PREDICTION OF HUMAN PHARMACOKINETICS 293 JIUNN H. LIN 3. FREE DRUG! THE
CRITICAL IMPORTANCE OF PLASMA PROTEIN BINDING IN NEW DRUG DISCOVERY 327
DAVID D. CHRIST AND GEORGE L. TRAINOR PARTV APPLICATIONS OF PROPERTY
INFORMATION TO LEAD SELECTION 337 1. USE OF IN VITRO ADME SCREENS TO
DEVELOP ORALLY BIOAVAILABLE AND CNS-PERMEABLE NEUROPEPTIDE Y Y5
ANTAGONISTS 339 DENNIS HEYER, ALEJANDRO J. DANIELS, AND THIMYSTA C.
BURNETTE 2. APPLYING COMPUTATIONAL AND IN VITRO APPROACHES TO LEAD
SELECTION 361 SEAN EKINS, JENNIFER BERBAUM, RICHARD K. HARRISON,
MARIANNE ZECHER, JING YUAN, ALEXEY V. ISHCHENKO, KATYA BEREZIN, VICTOR
CHUBUKOV, J. DAVID LAWSON, AND MAGGIE AZ HUPCEY CONTENTS IX PART VI
INTEGRATION OF PROFILING DATA IN DRUG DISCOVERY 391 1. STRATEGIES FOR IN
SILICO AND EXPERIMENTAL SCREENING OF PHYSICOCHEMICAL PROPERTIES 393
OLAFUR S. GUDMUNDSSON AND SRINI VENKATESH 2. THE CHALLENGE OF QUALITY IN
CANDIDATE OPTIMIZATION 413 SCOTT A. BILLER, LAURA CUSTER, KEN E.
DICKINSON, STEPHEN K. DURHAM, ASHVINIKUMAR V. GAVAI, LAWRENCE G. HAMANN,
JONATHAN L. JOSEPHS, FREDERIC MOULIN, GREG M. PEARL, OLIVER P. FLINT,
MARK SANDERS, ADRIENNE A. TYMIAK, AND ROY VAZ 3. A COMPREHENSIVE
STRATEGY FOR ADME SCREENING IN DRUG DISCOVERY 431 RONALD E. WHITE 4.
SCIENTIFIC, EDUCATIONAL, AND COMMUNICATION ISSUES ASSOCIATED WITH
INTEGRATING AND APPLYING DRUG-LIKE PROPERTIES IN DRUG DISCOVERY 451
RONALD T. BORCHARDT INDEX 467
|
| adam_txt |
PHARMACEUTICAL PROFILING IN DRUG DISCOVERY FOR LEAD SELECTION RONALD T.
BORCHARDT UNIVERSITY OF KANSAS EDWARD H. KERNS WYETH RESEARCH
CHRISTOPHER A. LIPINSKI PFIZER GLOBAL R&D (RETIRED) DHIREN R. THAKKER
UNIVERSITY OF NORTH CAROLINA BINGHE WANG GEORGIA STATE UNIVERSITY
AMERICAN ASSOCIATION OF PHARMACEUTICAL SCIENTISTS ARLINGTON, VA CONTENTS
PREFACE XI PARTI IN SILICO TOOLS 1 1. ABSORPTION PREDICTION 3 PER
ARTURSSON AND PAR MATSSON 2. PREDICTING MOLECULAR PHYSICAL PROPERTIES 27
ROBERT S. DEWITTE AND ED KOLOVANOV 3. IN SILICO TRANSPORTER MODELING AND
ITS APPLICATION IN DRUG DISCOVERY 53 ANNE HERSEY, CHRIS LUSCOMBE, AND
SANDEEP MODI 4. MODELS FOR CYTOCHROME P450-MEDIATED METABOLISM 69 K.R.
KORZEKWA, T.J. EWING, J.P. KOCHER, AND T.J. CARLSON 5. FUTURE OF IN
SILICO METHODS IN TOXICOLOGY 81 DAVID E. PATTERSON AND MICHAEL R.
BERTHOLD PART II PHYSICOCHEMICAL TOOLS 91 1. SOLUBILITY IN WATER AND
DMSO: ISSUES AND POTENTIAL SOLUTIONS 93 CHRISTOPHER A. LIPINSKI 2.
MEASUREMENTS OF LIPOPHILICITY AND ACID/BASE CHARACTER USING HPLC METHODS
127 KLDRA VALKO 3. HOW DO WE STUDY OXIDATIVE CHEMICAL STABILITY IN
DISCOVERY? SOME IDEAS, TRIALS, AND OUTCOMES 183 FRANCO LOMBARDO AND GUS
CAMPOS VU VIII CONTENTS PART III PERMEABILITY TOOLS 195 1.
PHYSICOCHEMICAL METHODS FOR ESTIMATING PERMEABILITY AND RELATED
PROPERTIES 197 M. KANSY, H. FISCHER, $. BENDELS, B. WAGNER, F SENNER, I.
PARRILLA, AND V. MICALLEF 2. CULTURED EPITHELIAL CELL ASSAYS USED TO
ESTIMATE INTESTINAL ABSORPTION POTENTIAL 217 ISMAEL J. HIDALGO, KATHRYN
WEINSTEIN, PAULA KARDOS, AND ROBERT STRAB 3. IN VITRO CELL-BASED ASSAYS
FOR ESTIMATING THE EFFECTS OF EFFLUX TRANSPORTERS ON CELL PERMEATION 235
JOSEPH W. POLLI AND COSETTE J. SERABJIT-SINGH PART IV ABSORPTION,
DISTRIBUTION, METABOLISM, AND EXCRETION TOOLS 257 1. IN VITRO MODELS FOR
ESTIMATING HEPATOBILIARY CLEARANCE 259 MADE] J. ZAMEK-GHSZCZYNSKI AND
KIM L.R. BROUWER 2. CHALLENGES IN DRUG DISCOVERY; LEAD OPTIMIZATION AND
PREDICTION OF HUMAN PHARMACOKINETICS 293 JIUNN H. LIN 3. FREE DRUG! THE
CRITICAL IMPORTANCE OF PLASMA PROTEIN BINDING IN NEW DRUG DISCOVERY 327
DAVID D. CHRIST AND GEORGE L. TRAINOR PARTV APPLICATIONS OF PROPERTY
INFORMATION TO LEAD SELECTION 337 1. USE OF IN VITRO ADME SCREENS TO
DEVELOP ORALLY BIOAVAILABLE AND CNS-PERMEABLE NEUROPEPTIDE Y Y5
ANTAGONISTS 339 DENNIS HEYER, ALEJANDRO J. DANIELS, AND THIMYSTA C.
BURNETTE 2. APPLYING COMPUTATIONAL AND IN VITRO APPROACHES TO LEAD
SELECTION 361 SEAN EKINS, JENNIFER BERBAUM, RICHARD K. HARRISON,
MARIANNE ZECHER, JING YUAN, ALEXEY V. ISHCHENKO, KATYA BEREZIN, VICTOR
CHUBUKOV, J. DAVID LAWSON, AND MAGGIE AZ HUPCEY CONTENTS IX PART VI
INTEGRATION OF PROFILING DATA IN DRUG DISCOVERY 391 1. STRATEGIES FOR IN
SILICO AND EXPERIMENTAL SCREENING OF PHYSICOCHEMICAL PROPERTIES 393
OLAFUR S. GUDMUNDSSON AND SRINI VENKATESH 2. THE CHALLENGE OF QUALITY IN
CANDIDATE OPTIMIZATION 413 SCOTT A. BILLER, LAURA CUSTER, KEN E.
DICKINSON, STEPHEN K. DURHAM, ASHVINIKUMAR V. GAVAI, LAWRENCE G. HAMANN,
JONATHAN L. JOSEPHS, FREDERIC MOULIN, GREG M. PEARL, OLIVER P. FLINT,
MARK SANDERS, ADRIENNE A. TYMIAK, AND ROY VAZ 3. A COMPREHENSIVE
STRATEGY FOR ADME SCREENING IN DRUG DISCOVERY 431 RONALD E. WHITE 4.
SCIENTIFIC, EDUCATIONAL, AND COMMUNICATION ISSUES ASSOCIATED WITH
INTEGRATING AND APPLYING DRUG-LIKE PROPERTIES IN DRUG DISCOVERY 451
RONALD T. BORCHARDT INDEX 467 |
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| isbn | 0971176795 |
| language | English |
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| series | Biotechnology: pharmaceutical aspects ;1 |
| series2 | Biotechnology: pharmaceutical aspects ;1 |
| spelling | Pharmaceutical profiling in drug discovery for lead selection Ronald T. Borchardt ... Arlington, VA AAPS Press 2004 XIII, 482 S. Ill., graph. Darst. 26 cm txt rdacontent n rdamedia nc rdacarrier Biotechnology: pharmaceutical aspects ;1 Includes bibliographical references and index Chemistry, Pharmaceutical Drug Design Drug development Pharmaceutical chemistry Borchardt, Ronald T. Sonstige oth Biotechnology: pharmaceutical aspects ;1 1 (DE-604)BV021640956 1 http://www.loc.gov/catdir/enhancements/fy0663/2004046347-d.html Publisher description lizenzfrei GBV Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=016381925&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Pharmaceutical profiling in drug discovery for lead selection Biotechnology: pharmaceutical aspects ;1 Chemistry, Pharmaceutical Drug Design Drug development Pharmaceutical chemistry |
| title | Pharmaceutical profiling in drug discovery for lead selection |
| title_auth | Pharmaceutical profiling in drug discovery for lead selection |
| title_exact_search | Pharmaceutical profiling in drug discovery for lead selection |
| title_exact_search_txtP | Pharmaceutical profiling in drug discovery for lead selection |
| title_full | Pharmaceutical profiling in drug discovery for lead selection Ronald T. Borchardt ... |
| title_fullStr | Pharmaceutical profiling in drug discovery for lead selection Ronald T. Borchardt ... |
| title_full_unstemmed | Pharmaceutical profiling in drug discovery for lead selection Ronald T. Borchardt ... |
| title_short | Pharmaceutical profiling in drug discovery for lead selection |
| title_sort | pharmaceutical profiling in drug discovery for lead selection |
| topic | Chemistry, Pharmaceutical Drug Design Drug development Pharmaceutical chemistry |
| topic_facet | Chemistry, Pharmaceutical Drug Design Drug development Pharmaceutical chemistry |
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