Screening Publications

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The publications listed below describe screens carried out in the ICCB/ICG Screening Facility between 1997 and April 2005. During that time the facility was supported by funds from Harvard Medical School, Merck & Co., Inc., Merck KGaA (Germany), W.M.Keck Foundation, and the National Institutes of Health (NIGMS and NCI). Initiative for Chemical Genetics (ICG) funding was provided by the NCI.

Review of bioprobes discovered at the ICCB/ICG:

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

Flaumenhaft, R., Sim, D.S. (2003). The platelet as a model for chemical genetics. Chem. Biol. 10(6): 481-6.

Kau, T.R., Silver, P.A. (2003). Nuclear transport as a target for cell growth. Drug Discov. Today. 8(2): 78-85.

Kau, T.R., Way, J.C., Silver, P.A. (2004).Nuclear transport and cancer: from mechanism to intervention. Nature Reviews Cancer. 4(2):1-12.

Mitchison, T.J. (2005). Small-Molecule Screening and Profiling by Using Automated Microscopy. Chembiochem. 6(1):33-39.

Research Articles :

2008

Brass, A,L., Dykxhoorn, D,M., Benita, Y., Yan, N., Engelman, A., Xavier, R, J., Lieberman, J., Elledge, S, J. (2008). Identification of Host Proteins Required for HIV Infection Through a Functional Genomic Screen. Science 2008 Feb 15;319(5865):921-926.

Cassidy-Stone, A., Chipuk, J.E., Ingerman, E., Song, C., Yoo, C., Kuwana, T., Kurth, M.J., Hinshaw, J.E., Green, D.R., Nunnari, J. (2008) Chemical inhibition of the mitochondrial division dynamin reveals its role in bax/bak-dependent mitochondrial outer membrane permeabilization. Dev.Cell. 2008 Feb; 14(2):193-204.

Umejiego, N.N., Gollapalii, D., Sharling, L., Volftsun, A., Lu, J., Benjamin, N.N., Stroupe, A., Riera, T.V., Striepen, B., Hedstrom, L. (2008) Targeting a Prokaryotic Protein in a Eukaryotic Pathogen: Identification of Lead Compounds against Cryptosporidiosis. Chembiol. 2008 Jan;15(1):70-77.

2007

Breger, J., Fuchs, B.B., Aperis, G., Moy, T.I., Ausubel, F.M., Mylonakis, E. (2007). Antifungal chemical compounds identified using a C. elegans pathogenicity assay. PLoS Pathog. 2007 Feb;3(2):e18.

Cheng, B., Liu, I.F., Tse-Dinh, Y.C. (2007). Compounds with antibacterial activity that enhance DNA cleavage by bacterial DNA topoisomerase I. J Antimicrob Chemother. 2007 Apr;59(4):640-5. Epub 2007 Feb 22.

Dodson, A.W., Taylor, T.J., Knipe, D.M., Coen, D.M. (2007) Inhibitors of the sodium potassium ATPase that impair herpes simplex virus replication identified via a chemical screening approach. Virology. 2007 Jun 1; [Epub ahead of print].

Falk, S.P., Ulijasz, A.T., Weisblum, B. (2007) Differential Assay for High-Throughput Screening of Antibacterial Compounds. J. Biomol. Screen. 2007; 12; 1102-08.

Junker, L.M., Clardy, J. (2007) High-Throughput Screens for Small-Molecule Inhibitors of Pseudomonas aeruginosa Biofilm Development. Antimicrob Agents Chemother. 2007 Oct;51(10):3582-90. Epub 2007 Jul 30.

Lee VT, Pukatzki S, Sato H, Kikawada E, Kazimirova AA, Huang J, Li X, Arm JP, Frank DW, Lory S. (2007) Pseudolipasin A is a specific inhibitor for phospholipase A2 activity of Pseudomonas aeruginosa cytotoxin ExoU.Infect Immun. Mar;75(3):1089-98.

Maresso, A.W., Wu, R., Kern, J.W., Zhang, R., Janik, D., Missiakas, D.M., Duban, M.E., Joachimiak, A., Schneewind, O. (2007) Activation of inhibitors by sortase triggers irreversible modification of the active site. J Biol Chem. 2007 Jun 1; [Epub ahead of print]

Moerke, N.J., Aktas, H., Chen, H., Cantel, S., Reibarkh, M.Y., Fahmy, A., Gross, J.D., Degterev, A., Yuan, J., Chorev, M., Halperin, J.A., and Wagner, G. (2007). Small- Molecule Inhibition of the Interaction between the Translation Initiation Factors eIF4E and eIF4G. Cell. 2007 Jan 26;128(2):257-67.

Pan, N., Lee, C., Goguen, J. (2007) High throughput screening for small-molecule inhibitors of type III secretion in Yersinia pestis. Adv Exp Med Biol. 603:367-75.

Park, J.Y., Arnaout, M.A., Gupta, V. (2007). A Simple, No-Wash Cell Adhesion-Based High-Throughput Assay for the Discovery of Small Molecule Regulators of the Integrin CD11b/CD18. J Biomol Screen 2007 Apr 12(3): 406-17.

Saenz, J.B., Doggett, T.A, Haslam, D.B. (2007). Identification and characterization of small molecules that inhibit intracellular toxin transport. Infect Immun. 2007 Jun 18; [Epub ahead of print].

Shakhnovich, E.A., Hung, D.T., Pierson, E., Lee, K., Mekalanos, J.J. (2007) Virstatin inhibits dimerization of the transcriptional activator ToxT. Proc Natl Acad Sci USA 2007 Feb 13;104(7):2372-7.

 

2006

Chirnomas, D., Taniguchi, T., de la Vega, M., Vaidya, A.P., Vasserman, M., Hartman, A.R., Kennedy, R., Foster, R., Mahoney, J., Seiden, M.V., D'Andrea, A.D. (2006). Chemosensitization to cisplatin by inhibitors of the Fanconi anemia/BRCA pathway. Mol Cancer Ther. 2006 Apr;5(4):952-61.

De Wall, S.L., Painter, C., Stone, J.D., Bandaranayake, R., Wiley, D.C., Mitchison, T.J., Stern, L.J., and DeDecker, B.S. (2006). Noble metals strip peptides from class II MHC proteins. Nature Chem. Biol. 2006 Apr;2(4):178-9.

Frey, G., Rits-Vollach, S., Zhang, X.-Q., Schooley, R.T., Chen, B., Harrison, S. (2006). Small molecules that bind the inner core of gp41 and inhibit HIV envelope-mediated fusion. Proc, Nat. Acad. US 103, 13938-13943.

Loregian, A., Coen, D.M. (2006). Selective anti-cytomegalovirus compounds discovered by screening for inhibitors of subunit interactions of the viral polymerase. Chem Biol. 2006 Feb;13(2):191-200.

Macia, E., Ehrlich, M., Massol, R., Boucrot, E., Brunner, C., Kirchhausen, T. (2006). Dynasore, a cell-permeable inhibitor of dynamin. Dev Cell. 2006 Jun;10(6):839-50.

Peterson, J.R., Lebensohn, A.M., Pelish, H.E., Kirschner, M.W. (2006) Biochemical suppression of small-molecule inhibitors: a strategy to identify inhibitor targets and signaling pathway components.Chem Biol. 2006 Apr;13(4):443-52.

Smith, P.L., Maloney, K.N., Pothen, R.G., Clardy, J., and Clapham, D.E. (2006) Bisandrographolide from Andrographis paniculata Activates TRPV4 Channels. J. Biol. Chem. 2006 281: 29897-29904.

Wetli, H.A., Buckett, P.D., Wessling-Resnick, M. (2006) Small-Molecule Screening Identifies the Selanazal Drug Ebselen as a Potent Inhibitor of DMT1-Mediated Iron Uptake. Chem Biol. 2006 Sep;13(9):965-72.

Zaarur, N., Gabai, V.L., Porco, J.A. Jr., Calderwood, S., Sherman, M.Y. (2006) Targeting heat shock response to sensitize cancer cells to proteasome and Hsp90 inhibitors. Cancer Res. 2006 Feb 1;66(3):1783-91.

2005

Boyce, M., Bryant, K.F., Jousse, C., Long, K., Harding, H.P., Scheuner, D., Kaufman, R.J., Ma, D., Coen, D.M., Ron, D., Yuan, J. (2005). A Selective Inhibitor of eIF2a Dephosphorylation Protects Cells from ER Stress. Science 307(5711):935-9.

Degterev, A., Huang, Z., Boyce, M., Li, Y., Jagtap, P., Mizushima, N., Cuny, G.D., Mitchison, T.J., Moskowitz, M., Yuan, J. (2005). Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nature Chemical Biology. 1(2):112-119.

Dorer, R.K., Zhong, S., Tallarico, J.A., Wong, W.H., Mitchison, T.J., Murray, A.W. (2005). A Small-Molecule Inhibitor of Mps1 Blocks the Spindle-Checkpoint Response to a Lack of Tension on Mitotic Chromosomes. Curr Biol. 2005 Jun 7;15(11):1070-1076.

Gross, B.J., Kraybill, B.C., Walker, S. (2005). Discovery of O-GlcNAc Transferase Inhibitors. J. Am. Chem. Soc.127(42):14588-9.

Hung, D.T., Shakhnovich, E.A., Pierson, E., Mekalanos, J.J. (2005) Small-Molecule Inhibitor of Vibrio cholerae Virulence and Intestinal Colonization. Science. 310(5748):670-4.

Kang, S., Li, H.,  Rao, A., Hogan, P.G. (2005)  Inhibition of the Calcineurin-NFAT Interaction by Small Organic Molecules Reflects Binding at an Allosteric Site. J. Biol. Chem. 280(45):37698-706.

Nieland, T.J., Ehrlich, M., Krieger, M., Kirchhausen, T (2005). Endocytosis is not required for the selective lipid uptake mediated by murine SR-BI. Biochem Biophys Acta. 1734(1):44-51.

Perlman, Z.E., Mitchison, T.J., Mayer, T.U. (2005) High-Content Screening and Profiling of Drug Activity in an Automated Centrosome-Duplication Assay. Chembiochem. 6(1):145-151.

Stern, H.M., Murphey, R.D., Shepard, J.L., Amatruda, J.F., Straub, C.T., Pfaff, K.L., Weber, G., Tallarico, J.A., King, R.W., Zon, L.I. (2005) Small molecules that delay S phase suppress a zebrafish bmyb mutant. Nat Chem Biol. 1(7):366-70.

Surpin, M., Rojas-Pierce, M., Carter, C., Hicks, G.R., Vasquez, J., Raikhel, N.V. (2005). The power of chemical genomics to study the link between endomembrane system components and the gravitropic response. PNAS 102(13):4902-7.

Yarrow, J.C., Totsukawa, G., Charras, G.T., Mitchison, T.J (2005). Screening for cell migration inhibitors via automated microscopy reveals a Rho-kinase inhibitor. Chem Biol. 12(3):385-95.

2004

Brown, J.X., Buckett, P.D., Wessling-Resnick, M. (2004). Identification of small molecule inhibitors that distinguish between non-transferrin bound iron uptake and transferrin-mediated iron transport. Chem Biol. 11(3):407-16.

Butcher, R. and Schreiber, S.L. (2004). Identification of Ald6p as the target of a class of small-molecule suppressors of FK506 and their use in network dissection. Proc. Natl. Acad. Sci. USA. 101(21):7868-73.

Carey, K.L., Westwood, N.J., Carey, K.L., Mitchison, T.J., Ward, G.E. A small molecule approach to studying invasive mechanisms of Toxoplasma gondii. Proc. Natl. Acad. Sci. USA. 101:7433-38.

Cerny, J., Feng, Y., Yu, A., Miyake, K., Borgonovo, B., Klumperman, J., Meldolesi, J., McNeil, P.L., Kirchhausen, T. (2004). The small chemical vacuolin-1 inhibits Ca(2+)-dependent lysosomal exocytosis but not cell resealing. EMBO Rep. 5(9):883-8.

Cheng, D., Yadav, N., King, R.W., Swanson, M.S., Weinstein, E.J., Bedford, M.T. (2004). Small molecule regulators of protein arginine methyltransferases. J. Biol. Chem. 279(23):23892-9.

Corcoran, L.J., Mitchison, T.J., Liu, Q. (2004). A novel action of histone deacetylase inhibitors in a protein aggresome disease model. Curr. Biol. 23;14(6):488-92.

Eggert,  U.S., Kiger, A.A., Richter, C., Perlman, Z.E., Perrimon, N., Mitchison, T.J., Field, C.M. (2004).  Parallel Chemical Genetic and Genome-Wide RNAi Screens Identify Cytokinesis Inhibitors and Targets. PLoS Biol. 2(12):379.

Feng, Y., Jadhav, A.P., Rodighiero, C., Fujinaga, Y., Kirchhausen, T., Lencer, W.I. (2004) Retrograde transport of cholera toxin from the plasma membrane to the endoplasmic reticulum requires the trans-Golgi network but not the Golgi apparatus in Exo2-treated cells. EMBO Rep. 5(6):596-601. Epub 2004 May 21.

Fiebiger E, Hirsch C, Vyas JM, Gordon E, Ploegh HL, Tortorella D(2004). Dissection of the dislocation pathway for type I membraneproteins with a new small molecule inhibitor, eeyarestatin. MolBiol Cell. 14(4):1635-46.

Hu, Y., Helm, J.S., Chen, L., Ginsberg, C., Gross, B., Kraybill, B., Tiyanont, K., Fang, X., Wu, T., Walker, S. (2004). Identification of selective inhibitors for the glycosyltransferase MurG via high-throughput screening. Chem. Biol. 11(5):703-11.

Kim YK, Arai MA, Arai T, Lamenzo JO, Dean EF 3rd, Patterson N, Clemons PA, Schreiber SL. (2004) Relationship of stereochemical and skeletal diversity of small molecules to cellular measurement space. J Am Chem Soc. 126(45):14740-5.

Li, H., Rao, A., Hogan, P.G. (2004). Structural delineation of the calcineurin-NFAT interaction and its parallels to PP1 targeting interactions. Journal of Molecular Biology 342, 1659-1674.

Limouze, J., Straight, A.F., Mitchison, T., Sellers, J.R. (2004) Specificity of blebbistatin, an inhibitor of myosin II. J Muscle Res Cell Motil. 25(4-5):337-41.

Margalit, D.M., Romberg, L., Mets, R.B., Hebert, A.M., Mitchison, T.J., Kirschner, M.W., RayChaudhuri, D. (2004). Targeting cell division: small-molecule inhibitors of FtsZ GTPase perturb cytokinetic ring assembly and induce bacterial lethality. Proc. Natl. Acad. Sci. USA. 101(32):11821-6.

Misaghi S, Pacold ME, Blom D, Ploegh HL, Korbel GA. (2004). Using a small molecule inhibitor of Peptide: N-glycanase to probe its role in glycoprotein turnover. Chem Biol. (12):1677-87.

Nieland, T.J., Chroni, A., Fitzgerald, M.L., Maliga, Z., Zannis, V.I., Kirchhausen, T., Krieger, M. (2004). Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide. J Lipid Res. 45:1256-65.

Nieland, T.J., Feng, Y., Brown, JX, Chuang, T.D., Buckett, P.D., Wang, J., Xie, X.S., McGraw, T.E., Kirchhausen, T., Wessling-Resnick, M. (2004). Chemical Genetic Screening Identifies Sulfonamides That Raise Organellar pH and Interfere with Membrane Traffic. Traffic. 5(7):478-92.

Perlman, Z.E., Slack, M.D., Feng, Y., Mitchison T.J., Wu, L.F. Altschuler, S.J. (2004) Multidimensional Drug Profiling By Automated Microscopy. Science. 306: 1194-1198.

Peterson, R.T., Shaw, S.Y., Peterson, T.A., Milan, D.J., Zhong, T.P., Schreiber, S.L., MacRae, C.A., Fishman, M.C. (2004). Chemical suppression of a genetic mutation in a zebrafish model of aortic coarctation. Nat. Biotechnol. 22(5):595-9.

Peterson, J.R., Bickford, L.C., Morgan, D., Kim, A.S., Ouerfelli, O., Kirschner, M.W., Rosen, M.K. (2004). Chemical Inhibition of N-WASP by stablization of a native autoinhibited conformation. Nat. Struct. Mol. Biol., in press.

Pilger, B.D., Cui, C., Coen, D.M (2004). Identification of a small molecule that inhibits herpes simplex virus DNA polymerase subunit interactions and viral replication. Chem. Biol., 11(5):647-54.

Roehrl, M.H.A., Kang, S., Aramburu, J., Wagner, G., Rao, A. Hogan, P.G. (2004). Selective inhibition of calcineurin-NFAT signaling by blocking protein-protein interaction with small organic molecules. Proc. Natl. Acad. Sci. USA, 101(20):7554-9.

Sim, D.S., Merrill-Skoloff, G., Furie, B.C., Furie, B., Flaumenhaft, R. (2004). Initial accumulation of platelets during arterial thrombus formation in vivo is inhibited by elevation of basal cAMP levels. Blood. 103(6):2127-34.

Venkatesh, N., Feng, Y., DeDecker, B., Yacono, P., Golan, D., Mitchison, T., McKeon, F. (2004). Chemical genetics to identify NFAT inhibitors: Potential of targeting calcium mobilization in immunosuppression. Proc Natl Acad Sci U S A. 15;101(24):8969-74.

Verma, R., Peters, N.R., D’Onofrio, M., Tochtrop, G.P., Sakamoto, K.M., Varadan, R., Zhang, M., Coffino, P., Fushman, D., Deshaies, R.J., King, R.W. (2004) Ubistatins inhibit proteasome-dependent degradation by binding the ubiquitin chain. Science 306(5693):117-20.

Yarrow, J.C., Perlman, Z.E., Westwood, N.J., Mitchison, T.J. (2004) A high-throughput cell migration assay using scratch wound healing, a comparison of image-based readout methods. BMC Biotechnol 4: 21.

2003

Barnes-Seeman, D., Park, S.B., Koehler, A.N., Schreiber, S.L. (2003). Expanding the functional group compatibility of small-molecule microarrays: discovery of novel calmodulin ligands. Angewandte Chemie. 42, 2376-79.

Butcher, R., Schreiber, S.L. (2003). A small molecule suppressor of FK506 that targets the mitochondria and modulates ionic balance in Saccharomyces cerevisiae. Chem. Biol. 10, 521-31.

Canman, J.C., Cameron, L.A., Maddox, P.S., Straight, A., Tirnauer, J.S., Mitchison, T.J., Fang, G., Kapoor, T.M., Salmon, E.D. (2003). Determining the position of the cell division plane. Nature. 424, 1074-8.

Feng, Y., Yu, S., Lasell, T.K., Jadhav, A.P., Macia, E., Chardin, P., Melancon, P., Roth, M., Mitchison, T., Kirchhausen, T. (2003). Exo1: a new chemical inhibitor of the exocytic pathway. Proc. Natl. Acad. Sci. USA. 100, 6469-74.

Haggarty, S.J., Clemons, P.A., Schreiber, S.L. (2003). Chemical genomic profiling of biological networks using combinations of small molecules and graph theory. J. Am. Chem. Soc. 125, 10543-5.

Haggarty, S.J., Koeller, K.M., Kau, T.R., Silver, P.A., Roberge, M., Schreiber, S.L. (2003). Small molecule modulation of the human chromatid decatenation checkpoint. Chem. Biol. 10, 1267-79.

Haggarty, S.J., Koeller, K.M., Wong, J.C., Butcher, R.A., Schreiber, S.L. (2003). Multidimensional chemical genetic analysis of a combinatorial library of deacetylase inhibitors using cell-based assays. Chem. Biol. 10, 383-96.

Haggarty, S.J., Koeller, K.M., Wong, J.C., Grozinger, C.M., Schreiber, S.L. (2003). Domain-selective small molecule inhibitor of HDAC-mediated tubulin deacetylation. Proc. Natl. Acad. Sci. USA. 100, 4389-94.

Helm, J. S., Hu, Y., Chen, L., Gross, B., Walker, S. (2003). Identification of active-site inhibitors of MurG using a generalizable, high-throughput glycosyltransferase screen. J. Am. Chem. Soc. 125(37): 11168-9.

Jenkins, J.L., Kao, R.Y.T., Shapiro, R. (2003). Virtual screening to enrich hit lists from high-throughput screening: A case study on small-molecule inhibitors of angiogenin. Structure, Function and Genetics. 50, 81-93.

Kau, T.R., Schroeder, F., Ramazwamy, S., Wojciechowski, C.L., Zhao, J.J., Roberts, T.M., Clardy, J., Sellers, W.R., Silver, P.A. (2003). A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN deficient tumor cells. Cancer Cell. 4(6), 463-76.

Koehler, A.N., Shamji, A.F., Schreiber, S.L. (2003). Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis. J. Am. Chem. Soc. 125, 8420-1.

Koeller, K.M., Haggarty, S.J., Perkins, B.D., Leykin, I., Wong, J.C., Kao, M.C.J., Schreiber, S.L. (2003). Chemical genetic modifier screens: Small molecule trichostatin suppressors as probes of acetylation in transcription, cell cycle progression, and stability of the cytoskeleton. Chem. Biol. 10, 397-410.

Straight, A., Cheung, A., Limouze, J., Chen, I., Westwood, N., Sellers, J., Mitchison, T. (2003). Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science. 299, 1743-7.

Wong, J.C., Hong, R., Schreiber, S.L. (2003). Structural biasing elements for in-cell histone deacetylase paralog selectivity. J. Am. Chem. Soc. 125, 5586-7.

Yarrow, J., Feng, Y., Perlman, Z., Kirchhausen, T., Mitchison, T. (2003). Phenotypic screening of small molecule libraries by high throughput cell imaging.Comb. Chem. and High Throughput Screening. 6, 79-99.

Zhao, Y., Dai, X., Blackwell, H.E., Schreiber, S.L., Chory, J. (2003). SIR1, an upstream component in auxin signaling identified by chemical genetics. Science. 301, 1107-1110.

2002

Cheung, A., Dantzig, J.A., Hollingworth, S., Baylor, S.M., Goldman, Y.E., Mitchison, T.J., Straight, A.F. (2002). A small-molecule inhibitor of skeletal muscle myosin II. Nat. Cell Biol. 4, 83-7.

Fantin, V., Berardi, M., Scorrano, L., Korsmeyer, S., Leder, P. (2002). A novel mitochondriotoxic small molecule that selectively inhibits tumor cell growth. Cancer Cell. 2, 29-42.

Kao, R.Y.T., Jenkins, J.L., Olson, K.A., Key, M.E., Fett, J.W., Shapiro, R. (2002). A small-molecule inhibitor of the ribonucleolytic activity of human angiogenin that possesses antitumor activity. Proc. Natl. Acad. Sci. USA. 99, 10066-71.

Kuruvilla, F.G., Shamji, A.F., Sternson, S.M., Hergenrother, P.J., Schreiber, S.L. (2002). Dissecting glucose signaling with diversity-oriented synthesis and small molecule microarrays. Nature. 416, 653-6.

Lugovskoy, A.A., Degterev, A.I., Fahmy, A.F., Zhou, P., Gross, J.D., Yuan, J., Wagner, G. (2002). A novel approach for characterizing protein ligand complexes: molecular basis for specificity of small-molecule Bcl-2 inhibitors. J. Am. Chem. Soc. 124, 1234-40.

Nieland, T., Penman, M., Dori, L., Krieger, M., Kirchhausen, T. (2002). Discovery of chemical inhibitors of the selective transfer of lipids mediated by the HDL receptor SR-BI. Proc. Natl. Acad. Sci. USA. 99, 15422-7.

2001

Degterev, A., Lugovskoy, A., Cardone, M., Mulley, B., Wagner, G., Mitchison, T., Yuan, J. (2001). Identification of small-molecule inhibitors of interaction between BH3 domain and Bcl-xL. Nat. Cell Biol. 3, 173-82.

Grozinger, C.M., Chao, E.D., Blackwell, H.E., Moazed, D., Schreiber, S.L. (2001). Identification of a class of small molecule inhibitors of the sirtuin family of NAD-dependent deacteylases by phenotypic screening. J. Biol. Chem. 276, 38837-43.

Pelish, H.E., Westwood, N.J., Feng, Y., Kirchhausen, T., Shair, M.D. (2001). Use of biomimetic diversity-oriented synthesis to discover galanthamine-like molecules with biological properties beyond those of the natural product. J. Am. Chem. Soc. 123, 6740-1.

Peterson, J.R., Lokey, R.S., Mitchison, T.J., Kirschner, M.W. (2001). A chemical inhibitor of N-WASP reveals a new mechanism for targeting protein interactions. Proc. Natl. Acad. Sci. USA. 98, 10624-9.

2000

Haggarty, S.J., Mayer, T.U., Miyamoto, D.T., Fathi, R., King, R.W., Mitchison, T.J., Schreiber, S.L. (2000). Dissecting cellular processes using small molecules: identification of colchicine-like, taxol-like and other small molecules that perturb mitosis. Chem. Biol. 7, 275-86.

Kapoor, T.M., Mayer, T.U., Coughlin, M.L., Mitchison, T.J. (2000). Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5. J. Cell. Biol. 150, 975-88.

Petersen, R.T., Link, B.A., Dowling, B.A., Schreiber, S.L. (2000). Small molecule developmental screens reveal the logic and timing of vertebrate development. Proc. Natl. Acad. Sci. U.S.A. 97, 12965-9.

1999

Mayer, T.U., Kapoor, T.M., Haggarty, S.J., King, R.W., Schreiber, S.L., Mitchison, T.J. (1999). Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science.286, 971-4.