Broad Institute Chemical Biology Program

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2003 | 2004 | 2005

2003

The small-molecule approach to biology: Chemical genetics and diversity-oriented organic synthesis make possible the systematic exploration of biology" Stuart L. Schreiber, Chem. & Eng. News, 2003, 81, 51-61.

From knowing to controlling: a path from genomics to drugs using small molecule probes" Robert L. Strausberg and Stuart L. Schreiber, Science, 2003, 300, 294-295.

Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation" S.J. Haggarty, K.M. Koeller, J.C. Wong, C.M. Grozinger, S.L. Schreiber, Proc. Natl. Acad. Soc., 2003, 100, 4389-4394.

Structural biasing elements for in-cell histone deacetylase paralog selectivity" Jason C. Wong, Roger Hong, Stuart L. Schreiber, J. Am. Chem. Soc., 2003, 125, 5586-5587.

Mulitdimensional chemical genetic analysis of a combinatorial library of deacetylase inhibitors using cell-based assays" Stephen J. Haggarty, Kathryn M. Koeller, Jason C. Wong, Rebeccca A. Butcher, Stuart L. Schreiber, Chem. Biol., 2003, 10, 383-396.

Chemical genetic modifier screens: Small molecule trichostatin suppressors as probes of acetylation in transcription, cell cycle progression, and stability of the cytoskeleton" Kathryn M. Koeller, Stephen J. Haggarty, Brian D. Perkins, Igor Leykin, Jason C. Wong, Ming-Chih J. Kao, Stuart L. Schreiber, Chem. & Biol., 2003, 10, 397-410.

Expanding the Functinal Group Compatibility of Small-Molecule Microarrays: Discovery of Novel Calmodulin Ligands" David Barnes-Seeman, Seung Bum Park, Angela N. Koehler, and Stuart L. Schreiber, Angewandte Chemie, 2003, 42, 2376-2379.

Development and validation of a T7 based linear amplicifation for genomic DNA" Chih Long Liu, Stuart L. Schreiber, Bradley E. Bernstein, BMC Genomics, 2003, 4, 19-29.

3Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis" Angela N. Koehler, Alykhan F. Shamji, Stuart L. Schreiber, J. Am. Chem. Soc., 2003, 125, 8420-8421.

Catalytic Asymmetric [3+2] Cycloaddition of Azomethine Ylides. Development of a Versatile Stepwise, Three-Component Reaction for Diversity-Oriented Synthesis" Chuo Chen, Xiaodong Li, Stuart L. Schreiber, J. Am. Chem. Soc., 2003, 125, 10174-10175.

A small molecule suppressor of FK506 that targets the mitochondria and modulates ionic balance in Saccharomyces cerevisiae" Rebecca Butcher, Stuart L. Schreiber, Chem. & Biol., 2003, 10, 521-531.

Chemical Genomic Profiling of Biological Networks Using Graph Theory and Combinations of Small Molecule Perturbations" Stephen J. Haggarty, Paul A. Clemons, Stuart L. Schreiber, J. Am. Chem. Soc., 2003, 125, 10543-10545.

SIR1, an Upstream Component in Auxin Signaling Identified by Chemical Genetics" Yunde Zhao, Xinhua Dai, Helen E. Blackwell, Stuart L. Schreiber, Joanne Chory, Science, 2003, 301, 1107-1110.

Integration of Growth Factor and Nutrient Signaling: Implications for Cancer Biology" Alykhan F. Shamji, Paul Nghiem, and Stuart L. Schreiber, Molecular Cell, 2003, 12, 271-280.

Generating diverse skeletons of small molecules combinatoriallyî Martin D. Burke, Eric M. Berger, Stuart L. Schreiber, Science, 2003, 302, 613-616.

Stereochemical control of skeletal diversityî Jason K. Sello, Peter R. Andreana, Daesung Lee, Stuart L. Schreiber, Org. Lett, 2003, 5, 4125-4127.

Methylation of Histone H3 K4 Mediates Association of the Isw1p ATPase with Chromatin" Helena Santos-Rosa, Robert Schneider, Bradley E. Bernstein, Nickoletta Karabesou, Antonin Morillon, Christoph Weisse, Stuart L. Schreiber, Jane Mellor, Tony Kouzarides, Molecular Cell, 2003, 12, 1325-1332.

Small Molecule Modulation of the Human Chromatid Decatenation Checkpoint" Stephen J. Haggarty, Kathryn M. Koeller, Tweeny R. Kau, Pamela A. Silver, Michel Roberge, Stuart L. Schrieber, Chem. Biol., 2003, 10, 1267-1279.

2004

A planning strategy for diversity-oriented synthesis" Martin D. Burke, Stuart L. Schreiber, Angewandte Chemie, 2004, 43, 46-58.

Macrolactones in Diversity-Oriented Synthesis: Preparation of a Pilot Library and Exploration of Factors Controlling Macrocyclization" Darby R. Schmidt, Ohyum Kwon, and Stuart L. Schreiber, J Comb Chem, 2004, 6, 286-292.

Synthetic Strategy toward Skeletal Diversity via Solid-Supported, Otherwise Unstable Reactive Intermediates" Steven J. Taylor, Alexander M. Taylor, Stuart L. Schreiber, Angewandte Chemie, 2004, 43, 1681-1685.

Chemical suppression of a genetic mutation in a zebrafish model of aortic coarctation" Randall T. Peterson, Stanley Y. Shaw, Travis A. Peterson, David J. Milan, Tao P. Zhong, Stuart L. Schreiber, Calurn A. MacRae, Mark C. Fishman, Nature Biotech, 2004.

The use of chromatin immunoprecipitation assays in genome-wide analyses of histone modificationsî Bradley E. Bernstein, Emily L. Humphrey, Chih Long Liu and Stuart L. Schreiber. In Allis C.D., Wu C., eds. Methods in Enzymology: Chromatin and Chromatin Remodeling Enzymes 2004, 376, 350-361.

Paul Nghiem, Young-son Kim, Stuart L. Schreiber, "Protein kinases as targets in cancer therapy: Validated and emerging approaches" Chapter 13, Pages 293-315 in Oncogenomics: Molecular Approaches to Cancer, Ed., Charlie Brenner and David Duggan, John Wiley & Sons, 2004.

Rpd3p relocation mediates the transcriptional response to rapamycin in yeastî Emily L. Humphrey, Alykhan F. Shamji, Bradley E. Bernstein, Stuart L. Schreiber, Chem. & Biol., 2004, 11, 295-299.

Questions and Answers: Stuart L. Schreiberî, Curr. Biol., 2004, 14, R292-R293.

Identification of Ald6 as the target of a class of small molecule suppressors of FK506 and their use in network dissectionî Rebecca A. Butcher and Stuart L. Schreiber, Proc. Natl. Acad. Sci., U.S.A., 2004, 101, 7868-7873.

Global determinants of nucleosome occupancy in yeastî Bradley E. Bernstein, Chih Long Liu, Emily L. Humphrey, Stuart L. Schreiber, Genome Biology, 2004, 5:R62.

Modular synthesis and preliminary biological evaluation of stereochemically and skeletally diverse 1,3-dioxanes" Jason C. Wong, Scott M. Sternson, Joseph B. Louca, Roger Hong, Stuart L. Schreiber, Chem. & Biol., 2004, 11, 1279-1291.

Mapping chemical space using molecular descriptors and chemical genetics: Deacetylase inhibitors", Stephen J. Haggarty, Jason C. Wong, Paul A. Clemons, Stuart L. Schreiber, Comb. Chem. High Throughput Screen., 2004, 7, 669-676.

A synthesis strategy yielding skeletally diverse small molecules combinatorially" Martin D. Burke, Eric M. Berger, Stuart L. Schreiber, J. Am. Chem. Soc., 2004, 126, 14095-14104.

Syntheses of stereochemicaly diverse nine-membered ring-containing biaryls" Shyam Krishnan and Stuart L. Schreiber, Org. Lett., 2004, 6, 4021-4024.

Stereochemical control of the Passerini reaction" Peter R. Andreana, Chang C. Liu, Stuart L. Schreiber, Org. Lett., 2004, 6, 4231-4233.

Finding new genetic modifiers of the TOR signaling pathway through chemical genetics and proteome chips" Jing Huang, Heng Zhu, Stephen J. Haggarty, David R. Spring, Heejun Hwang, Fulai Jin, Michael Snyder, Stuart L. Schreiber, Proc. Natl. Acad. Sci., U.S.A., 2004, 101, 16594-16599.

Relationship of stereochemical and skeletal diversity of small molecules to cellular measurement spaceî Young-kwon Kim, Midori A. Arai, Takayoshi Arai, Julia O. Lamenzo, Elton F. Dean, III, Nick Patterson, Paul A. Clemons, Stuart L. Schreiber, J. Am. Chem. Soc.,2004, 126, 14740-14745.

A Library of Spirooxindoles Based on a Stereoselective Three-Component Coupling Reactionî Lo, M.M.-C.; Neumann, C.S.; Nagayama, S.; Perlstein, E.O.; Schreiber, S.L. J. Am. Chem. Soc.,2004, 126, 16077-16086.

2005

Skeletal diversity via a folding pathway: Synthesis of Indole alkaloid-like skeletons" Hiroki Oguri and Stuart L. Schreiber, Org. Lett., 2005, 7, 47-50.

Genomic maps and comparative analysis of histone modifications in human and mouseî Bradley E. Bernstein, Michael Kamal, Kerstin Lindblad-Toh, Stefan Bekiranov, Dione Kampa, Dana J. Huebert, Scott McMahon, Edward J. Kulbokas III, Thomas R. Gingeras, Stuart L. Schreiber, Eric S. Lander, Cell, 2005, 120, 169-181.

Using genome-wide transcriptional profiling to elucidate small-molecule mechanism" Rebecca A. Butcher and Stuart L. Schreiber, Curr. Op. Chem. Biol., 2005, 9, 25-30.

Convergent Diversity-Oriented Synthesis of Small-Molecule Hybrids" Chuo Chen, Xiaodong Li, Christopher Neumann, Michael M.-C. Lo, and Stuart L. Schreiber, Angew. Chem. 2005, 117, 2-4.

 

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