Foreword: Combinatorial Chemistry at a Crossroads |
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ix | (8) |
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Walter H. Moos, MitoKor, San Diego, California |
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Preface |
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xvii | (4) |
Contributors |
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PART I. Combinatorial Chemistry and Molecular Diversity: An Introduction |
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1 | (178) |
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1. Historical Overview of the Developing Field of Molecular Diversity |
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John C. Chabala, Pharmacopeia Inc., Princeton, New Jersey |
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2. Strategies in the Design and Synthesis of Chemical Libraries |
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17 | (22) |
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Eric M. Gordon, Versicor, Inc., Fremont, California |
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3. Solid-Phase Peptide Synthesis, Lead Generation, and Optimization |
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39 | (72) |
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Bruce Seligman, SIDDCO, Tucson, Arizona |
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Michael Lebl, Trega Biosciences, San Diego, California |
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Kit S. Lam, Arizona Cancer Center, Tucson, Arizona |
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4. Light-Directed Chemical Synthesis of Positionally Encoded Peptide Arrays |
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111 | (22) |
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Zhengyu Yuan, Versicor, Inc., Fremont, California |
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John Schullek, Affymax Research Institute, Palo Alto, California |
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Steven A. Sundberg, Affymax Research Institute, Santa Clara, California |
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5. Conformationally Restricted Peptide and Peptidomimetic Libraries |
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133 | (18) |
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Jonathan A. Ellman, Department of Chemistry, University of California at Berkeley, Berkeley, California |
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6. Submonomer Approaches for the Generation of Molecular Diversity: Nonnatural Oligomer and Organic Template Libraries |
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151 | (14) |
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Ronald N. Zuckermann, Chiron Corporation, Emeryville, California |
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7. Oligonucleotide Libraries as a Source of Molecular Diversity |
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165 | (14) |
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Houng-Yau Mei, Parke - Davis Pharmaceutical Research, Division of Warner - Lambert Company, Ann Arbor, Michigan |
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Anthony Czarnik, IRORI, La Jolla, California |
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PART II. Small Molecule Libraries |
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179 | (158) |
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8. Small Molecule Libraries: Overview of Issues and Strategies in Library Design |
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181 | (8) |
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John J. Baldwin, Pharmacopeia, Inc., Princeton, New Jersey |
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9. Protease Inhibitor Libraries |
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189 | (12) |
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Dinesh V. Patel, Versicor, Inc., Fremont, California |
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David A. Campbell, Affymax Research Institute, Santa Clara, California |
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10. Heterocyclic Combinatorial Chemistry: Azine and Diazepine Pharmacophores |
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201 | (12) |
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Dinesh V. Patel, Versicor, Inc., Fremont, California |
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11. Scaffolds for Small Molecule Libraries |
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213 | (14) |
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Michael R. Pavia, Millenium Pharmaceuticals Inc., Cambridge, Massachusetts |
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12. Application of Combinatorial Chemistry to Biopolymers |
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227 | (16) |
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Edmund J. Moran, Ontogen Corp., Carlsbad, California |
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13. Oligosaccharide and Glycoconjugate Solid-Phase Synthesis Technologies for Drug Discovery |
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243 | (28) |
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Michael J. Sofia, Transcell Technologies, Inc., Cranbury, New Jersey |
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14. Encoded Combinatorial Chemistry |
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271 | (20) |
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Zhi-Jie Ni, Versicor, Inc., Fremont, California |
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15. Parallel Organic Synthesis in Array Format |
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291 | (16) |
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Steven E. Hall, Sphinx Pharmaceuticals, A Division of Eli Lilly & Co., Durham, North Carolina |
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16. Synthetic Organic Chemistry on Solid Support |
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307 | (30) |
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Miles G. Siegel, Lilly Research Laboratories, A Division of Eli Lilly & Company, Indianapolis, Indiana |
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PART III. Automation, Analytical, and Computational Methods |
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337 | (50) |
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17. Automation of Combinatorial Chemistry for Large Libraries |
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339 | (10) |
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Jeffrey Sugarman, Affymax Research Institute, Palo Alto, California |
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18. Analytical Chemistry Issues in Combinatorial Organic Synthesis |
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349 | (20) |
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George Detre, Affymax Research Institute, Santa Clara, California |
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19. Quantifying Diversity |
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369 | (18) |
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Mark G. Bures, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois |
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PART IV. Biological Diversity |
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387 | (32) |
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20. Protein Scaffolds for Peptide Libraries |
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389 | (12) |
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Ronald H. Hoess, Dupont-Merck Pharmaceutical Company, Wilmington, Delaware |
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21. Combinatorial Biosynthesis of "Unnatural" Natural Products |
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401 | (18) |
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Chaitan Khosla, Departments of Chemistry and Chemical Engineering, Stanford University, Stanford, California |
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PART V. Screening |
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419 | (26) |
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22. Strategies for Screening Combinatorial Libraries |
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421 | (12) |
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Bruce A. Beutel, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois |
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23. Approaches and Technologies for Screening Large Combinatorial Libraries |
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433 | (12) |
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Daniel Chelsky, Pharmacopeia, Inc., Princeton, New Jersey |
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PART VI. Combinatorial Drug Screening and Development |
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445 | (54) |
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24. Combinatorial Drug Discovery: Concepts |
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447 | (6) |
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Judd Berman, Glaxo Wellcome Research Institute, Research Triangle Park, North Carolina |
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Russell J. Howard, Affymax Research Institute, Santa Clara, California |
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25. ADME/PK Assays in Screening for Orally Active Drug Candidates |
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453 | (22) |
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Rene A. Braeckman, Chiron Corporation, Emeryville, California |
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26. Combinatorial Technologies: Prospects and Future Issues |
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475 | (8) |
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James F. Kerwin, Jr., Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois |
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27. Appendix: Combinatorial Chemistry Information Management |
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483 | (16) |
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David Weininger, Daylight Chemical Information Systems, Inc., Santa Fe, New Mexico |
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Index |
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