Our goal is to deliver libraries of diverse, targeted and biased compounds with leadlike and druglike properties to help our clients generate hits and chemical probes for their therapeutic discovery, chemical biology and agrochemical programs. We rely on publications in peer-reviewed journals as one measure of our clients’ success, and since 1999 our products have been cited as part of many successful research programs in both academic
and industrial laboratories. A partial list of citations is provided below.
For information on publications in a specific research area, please contact your ChemBridge representative or sales@chembridge.com.
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Rozenfeld, R.; Devi, L. A.; Regulation of CB1 cannabinoid receptor trafficking by the adaptor protein AP-3. FASEB 2008. |
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Takabe, K.; Paugh, S. W.; Milstien, S.; Spiegel, S.; "Inside-Out" Signaling of Sphingosine-1-Phosphate: Therapeutic Targets. Pharmacol Rev. 2008. |
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Tegos, G. P.; Masago, K.; Aziz, F.; Higginbotham, A.; Stermitz, F. R.; Hamblin, M. R.; Inhibitors of bacterial multidrug efflux pumps potentiate antimicrobial photoinactivation. AAC 2008. |
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Lisk, G.; Pain, M.; Gluzman, I. Y.; Kambhampati, S.; Furuya, T.; Su, X.; Fay, M. P.; Goldberg, D. E.; Desai, S. A.; Changes in PSAC Reduce Leupeptin Uptake and Can Confer Drug Resistance in P. falciparum-Infected Erythrocytes. PNAS 2008. |
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Christian, M.; Hannah, W. B.; Lüthen, H.; Jones, A. M.; Identification of auxins by a chemical genomics approach. J. Exp. Botany 2008. |
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Kostka, M.; Högen, T.; Danzer, K. M.; Levin, J.; Habeck, M.; Wirth, A.; Wagner, R.; Glabe, C. G.; Finger, S.; Heinzelmann, U.; Garidel, P.; Duan, W.; Ross, C. A.; Kretzschmar, H.; Giese, A.; Single-particle characterization of iron-induced pore-forming a-synuclein oligomers. J. of Bio. Chem. 2008. |
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Yu, P. B.; Hong, C. C.; Sachidanandan, C.; Babitt, J. L.; Deng, D. Y.; Hoyng, S. A.; Lin, H. Y.; Bloch, K. D.; Peterson, R. T.; Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nature Chem. Bio. 2008, 4, 33-41. |
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Chen, X.; Zhong, S.; Zhu, X.; Dziegielewska, B.; Ellenberger, T.; Wilson, G. M.; Mackerell, Jr., A. D.; Tomkinson, A. E.; Rational Design of Human DNA Ligase Inhibitors that Target Cellular DNA Replication and Repair. Cancer Res. 2008, 68, 3169-3177. |
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Kravchenko, J. E.; Ilyinskaya, G. V.; Komarov, P. G.; Agapova, L. S.; Kochetkov, D. V.; Strom, E.; Frolova, E. I.; Kovriga, I.; Gudkov, A. V.; Feinstein, E.; Chumakov, P. M.; Small-molecule RETRA suppresses mutant p53-bearing cancer cells through a p73-dependent salvage pathway. PNAS 2008, 105 (17), 6302-6307. |
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Wang, Q.; Li, L.; Ye, Y.; Inhibition of p97-dependent Protein Degradation by Eeyarestatin I. J. Biol. Chem. 2008, 283 (12), 7445-7454. |
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Sadek, H.; Hannack, B.; Choe, E.; Wang, E.; Latif, S.; Garry, M. G.; Garry, D. J.; Longgood, J.; Frantz, D. E.; Olson, E. N.; Hsieh, J.; Schneider, J. W.; Cardiogenic small molecules that enhance myocardial repair by stem cells. PNAS 2008, 105 (16), 6063-6068. |
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Neugebauer, R. C.; Uchiechowska, U.; Meier, R.; Hruby, H.; Valkov, V.; Verdin, E.; Sippl, W.; Jung, M.; Structure-Activity Studies on Splitomicin Derivatives as Sirtuin Inhibitors and Computational Prediction of Binding Mode. J. Med Chem. 2008, 51, 1203-1213. |
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Dupré, A.; Boyer-Chatenet, L.; Sattler, R. M.; Modi, A. P.; Lee, J.; Nicolette, M. L.; Kopelovich, L.; Jasin, M.; Baer, R.; Paull, T. T.; Gautier, J.; A forward chemical genetic screen reveals an inhibitor of the Mre11-Rad50-Nbs1 complex. Nature Chem. Bio. 2008, 4 (2), 119-125. |
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Handeli, S.; Simon, J. A.; A small-molecule inhibitor of Tcf/ß-catenin signaling down-regulates PPAR and PPAR activities. Mol. Cancer Therap. 2008, 7, 521-529. |
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Montes, M.; Braud, E.; Miteva, M. A.; Goddard, M.; Mondésert, O.; Kolb, S.; Brun, M.; Ducommun, B.; Garbay, C.; Villoutreix, B. O.; Receptor-Based Virtual Ligand Screening for the Identification of Novel CDC25 Phosphatase Inhibitors. J. Chem. Inf. Model. 2008, 48, 157-165. |
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Herschhorn, A.; Oz-Gleenberg, I.; Hizi, A.; Mechanism of Inhibition of HIV-1 Reverse Transcriptase by the Novel Broad-Range DNA Polymerase Inhibitor N-{2-[4-(Aminosulfonyl)phenyl]ethyl}-2-(2-thienyl)acetamide.; Biochemistry 2008, 47, 490-502. |
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Mao, H.; Thakur, C. S.; Chattopadhyay, S.; Silverman, R. H.; Gudkov, A.; Banerjee, A. K.; Inhibition of human parainfluenza virus type 3 infection by novel small molecules. Antiviral Res. 2008, 77 (2), 83-94. |
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Boyce, M.; Py, B. F.; Ryazanov, A. G.; Minden, J. S.; Long, K.; Ma, D.; Yuan, J.; A pharmacoproteomic approach implicates eukaryotic elongation factor 2 kinase in ER stress-induced cell death. Cell Death and Differentiation 2008, 15, 589-599. |
2007
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Outeiro, T. F.; Kontopoulos, E.; Altman, S.; Kufareva, I.; Strathearn, K. E.; Amore, A. M.; Volk, C. B.; Maxwell, M. M.; Rochet, J. C.; McLean, P. J.; Young, A. B.; Abagyan, R.; Feany, M. B.; Hyman, B. T.; Kazantsev, A.; Sirtuin 2 inhibitors rescue a-synuclein-mediated toxicity in models of Parkinson’s disease. hScience 2007, 317, 516-519. |
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Xiong, Q.; Sun, H.; Li, M.; Zinc pyrithione-mediated activation of voltage-gated KCNQ potassium channels rescues epileptogenic mutants. Nature Chem. Bio. 2007, 3, 287-296. |
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Garske, A. L.; Smith, B. C.; Denu, J. M.; Linking SIRT2 to Parkinson’s Disease. ACS Chem. Bio. 2007, 2 (8), 529-532. |
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Denault, J.; Drag, M.; Salvesen, G. S.; Alves, J.; Heidt, A. B.; Deveraux, Q.; Harris, J. L.; Small molecules not direct activators of caspases. Nature Chem. Bio. 2007, 3 (9), 519. |
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Shirey, J.K.; Xiang, Z.; Orton, D.; Brady, A.E.; Johnson, K.A.; Williams, R.; Ayala, J.E.; Rodriguez, A.L.; Wess, J.; Weaver, D.; Niswender, C.M.; Conn, P.J.; An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nature Chem. Bio. 2007, 4 (1), 42-50. |
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Zhao, Y.; Chow, T.F.; Puckrin, R.S.; Alfred, S.E.; Korir, A.K.; Larive, C.K.; Cutler, S.R.; Chemical genetic interrogation of natural variation uncovers a molecule that is glycoactivated. Nature Chem. Bio. 2007, 3 (11), 716-721. |
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Hu, Q.; Shattock, R.; Novel Antiviral Agents Targeting HIV Entry and Transmission. Virologica Sinica 2007, 22 (6), 451-461. |
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Yang, Y.; Kitagaki, J.; Dai, R.; Tsai, Y. C.; Lorick, K. L.; Ludwig, R. L.; Pierre, S. A.; Jensen, J. P.; Davydov, I. V.; Oberoi, P.; Li, C. H.; Kenten, J. H.; Beutler, J. A.; Vousden, K. H.; Weissman, A. M.; Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of Potential Cancer Therapeutics. Cancer Res. 2007, 67 (19), 9472-9481. |
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Richardson, R. D.; Smith, J. W.; Novel antagonists of the thioesterase domain of human fatty acid synthase.; Mol Cancer Ther. 2007, 6 (7), 2120- 2126. |
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Hirayama, K.; Aoki, S.; Nishikawa, K.; Matsumoto, T.; Wada, K.; Identification of novel chemical inhibitors for ubiquitin C-terminal hydrolase-L3 by virtual screening. Bioorg. Med. Chem. 2007, 15, 6810-6818. |
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Huang, M.; Xie, S.; Ma, Z.; Huang, Q.; Nan, F.; Ye, Q.; Inhibition of Monometalated Methionine Aminopeptidase: Inhibitor Discovery and Crystallographic Analysis.; J. Med. Chem. 2007, 50, 5735-5742. |
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McNamara, C. R.; Mandel-Brehm, J.; Bautista, D. M.; Siemens, J.; Deranian, K. L.; Zhao, M.; Hayward, N. J.; Chong, J. A.; Julius, D.; Moran, M. M.; Fanger, C. M.; TRPA1 mediates formalin-induced pain. PNAS 2007, 104 (33), 13525-13530. |
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Lemaire, G.; Benod, C.; Nahoum, V.; Pillon, A.; Boussioux, A.; Guichou, J.; Subra, G.; Pascussi, J.; Bourguet, W.; Chavanieu, A.; Balaguer, P.; Discovery of a Highly Active Ligand of Human Pregnane X Receptor: A Case Study from Pharmacophore Modeling and Virtual Screening to "In Vivo" Biological Activity. Mol Pharm 2007, 72 (3), 572-581. |
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Kimple, A. J.; Willard, F. S.; Giguère, P. M.; Johnston, C. A.; Mocanu, V.; Siderovski, D. P.; The RGS protein inhibitor CCG-4986 is a covalent modifier of the RGS4 Ga-interaction face. BBA-Proteins & Proteomics 2007, 1774 (9), 1213-1220. |
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Vidal, D.; Blobel, J.; Pérez, Y.; Thormann, M.; Pons, M.; Structure-based discovery of new small molecule inhibitors of low molecular weight protein tyrosine phosphatase. Eur. J. of Med. Chem. 2007, 42, 1-7. |
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Viaud, J.; Zeghouf, M.; Barelli, H.; Zeeh, J.; Padilla, A.; Guibert, B.; Chardin, P.; Royer, C. A.; Cherfils, J.; Chavanieu, A.; Structure-based discovery of an inhibitor of Arf activation by Sec7 domains through targeting of protein-protein complexes. PNAS 2007, 104 (25), 10370-10375. |
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Roman, D. L.; Talbot, J. N.; Roof, R. A.; Sunahara, R. K.; Traynor, J. R.; Neubig, R. R.; Identification of Small-Molecule Inhibitors of RGS4 Using a High-Throughput Flow Cytometry Protein Interaction Assay. Mol. Pharmacol. 2007, 71 (1), 169-175. |
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Schiffer, N. W.; Broadley, S. A.; Hirschberger, T.; Tavan, P.; Kretschmar, H. A.; Giese, A.; Haass, C.; Hartl, F. U.; Schmid, B.; Identification of Anti-prion Compounds as Efficient Inhibitors of Polyglutamine Protein Aggregation in a Zebrafish Model. J. of Bio. Chem. 2007, 282 (12), 9195-9203. |
2006
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Li, R.; Xue, L.; Zhu, T.; Jiang, Q.; Cui, X.; Yan, Z.; McGee, D.; Wang, J.; Gantla, V. R.; Pickens, J. C.; McGrath, D.; Chucholowski, A.; Morris, S. W.; Webb, T. R.; Design and Synthesis of 5-Aryl-pyridone-carboxamides as Inhibitors of Anaplastic Lymphoma Kinase. J. Med. Chem. 2006, 49, 1006-1015. |
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Watanabe, M.; Houten, S. M.; Mataki, C.; Christoffolete, M. A.; Kim, B. W.; Sato, H.; Messaddeq, N.; Harney, J. W.; Ezaki, O.; Kodama, T.; Schoonjans, K.; Bianco, A. C.; Auwerx, J.; Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation. Nature 2006, 439, 484-489. |
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Bodner, R. A.; Outeiro, T. F.; Altmann, S.; Maxwell, M. M.; Cho, S. H.; Hyman, B. T.; McLean, P. J.; Young, A. B.; Housman, D. E.; Kazantsev, A. G.; Pharmacological promotion of inclusion formation: a therapeutic approach for Huntington’s and Parkinson’s diseases. PNAS 2006, 103 (11), 4246-4251. |
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Kwok, T. C. Y.; Ricker, N.; Fraser, R.; Chan, A. W.; Burns, A.; Stanley, E. F.; McCourt, P.; Cutler, S. R.; Roy, P. J. ; A small-molecule screen in C. elegans yields a new calcium channel antagonist. Nature 2006, 441, 91-95. |
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Kim, S.; Henry, E. C.; Kim, D.; Kim, Y.; Shin, K. J.; Han, M. S.; Lee, T. G.; Kang, J.; Gasiewicz, T. A.; Ryu, S. H.; Suh, P.; Novel Compound 2-Methyl-2H-pyrazole-3-carboxylic Acid (2-methyl-4-o-tolylazo-phenyl)-amide (CH-223191) Prevents 2,3,7,8-TCDD-Induced Toxicity by Antagonizing the Aryl Hydrocarbon Receptor. Mol. Pharmacol. 2006, 69, 1871-1878. |
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Williamson, L.; Raess, N. A.; Caldelari, R.; Zakher, A.; de Bruin, A.; Posthaus, H.; Bolli, R.; Hunziker, T.; Suter, M. M.; Müller, E. J.; Pemphigus vulgaris identifies plakoglobin as key suppressor of c-Myc in the skin. EMBO 2006, 25, 3298-3309. |
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Salvador-Recatala, V.; Kim, Y.; Zaks-Makhina, E.; Levitan, E. S.; Voltage-Gated K+ Channel Block by Catechol Derivatives: Defining Nonselective and Selective Pharmacophores. J. Pharmacol. Exp. Therap. 2006, 319, 758-764. |
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Schön, A.; Madani, N.; Klein, J. C.; Hubicki, A.; Ng, D.; Yang, X.; Smith, III, A. B.; Sodroski, J.; Freire, E.; Thermodynamics of Binding of a Low-Molecular-Weight CD4 Mimetic to HIV-1 gp120. Biochemistry 2006, 45 (36), 10973-10980. |
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De La Fuente, R.; Sonawane, N. D.; Arumainayegam, D.; Verkman, A. S.; Small molecules with antimicrobial activity against E. coli and P. aeruginosa identified by high-throughput screening. British J. of Pharmacol. 2006, 149, 551-559. |
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Söderberg, O., Gullberg, M.; Jarvius, M.; Ridderstråle, K.; Leuchowius, K.; Jarvius, J.; Wester, K.; Hydbring, P.; Bahram, F.; Larsson, L.; Landegren, U.; Direct observation of individual endogenous protein complexes in situ by proximity ligation. Nature Methods 2006, 3, 995-1000. |
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Burns, A. R.; Kwok, T. C. Y.; Howard, A.; Houston, E.; Johanson, K.; Chan, A.; Cutler, S. R.; McCourt, P.; Roy, P. J.; High-throughput screening of small molecules for bioactivity and target identification in Caenorhabditis elegans. Nature Protocols 2006, 1 (4), 1906-1914. |
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Huang, C.; Harootunian, A.; Maher, M. P.; Quan, C.; Raj, C. D.; McCormack, K.; Numann, R.; Negulescu, P. A.; González, J. E.; Characterization of voltage-gated sodium-channel blockers by electrical stimulation and fluorescence detection of membrane potential. Nature Bio. 2006, 24, 439-446. |
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Putt, K. S.; Chen, G. W.; Pearson, J. M.; Sandhorst, J. S.; Hoagland, M. S.; Kwon, J.; Hwang, S.; Jin, H.; Churchwell, M. I.; Cho, M.; Doerge, D. R.; Helferich, W. G.; Hergenrother, P. J.; Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nature Chem. Bio. 2006, 2 (10), 543-550. |
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Murphy, G. J.; Mostoslavsky, G.; Kotton, D. N.; Mulligan, R. C.; Exogenous control of mammalian gene expression via modulation of translational termination. Nature Med. 2006, 12 (9), 1093-1099. |
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Ducker, C. E.; Griffel, L. K.; Smith, R. A.; Keller, S. N.; Zhuang, Y.; Xia, Z.; Diller, J. D.; Smith, C. D.; Discovery and characterization of inhibitors of human palmitoyl acyltransferases. Mol. Cancer Ther. 2006, 5 (7), 1647-1659. |
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Strom, E.; Sathe, S.; Komarov, P. G.; Chernova, O. B.; Pavlovska, I.; Shyshynova, I.; Bosykh, D. A.; Burdelya, L. G.; Macklis, R. M.; Skaliter, R.; Komarova, E. A.; Gudkov, A. V.; Small-molecule inhibitor p53 binding to mitochondria protects mice from gamma radiation. Nature Chem. Bio. 2006. |
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Verheij, H. J.; Leadlikeness and structural diversity of synthetic screening libraries. Mol. Diversity 2006, 10 (3), 377-388. |
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Robert, F.; Kapp, L. D.; Khan, S. N.; Acker, M. G.; Kolitz, S.; Kazemi, S.; Kaufman, R. J.; Merrick, W. C.; Koromilas, A. E.; Lorsch, J. R.; Pelletier, J.; Initiation of Protein Synthesis by Hepatitis C Virus is Refractory to Reduced eIF2 · GTP · Met-tRNAiMet Ternary Complex Availability. Mol. Biol. Cell. 2006, 17, 4632-4644. |
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Macia, E.; Ehrlich, M.; Massol, R.; Boucrot, E.; Brunner, C.; Kirchhausen, T.; Dynasore, a Cell-Permeable Inhibitor of Dynamin. Dev. Cell. 2006, 10 (6), 839-850. |
2005
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Kang, M.; Lisk, G.; Hollingworth, S.; Baylor, S. M.; Desai, S. A.; Malaria Parasites Are Rapidly Killed by Dantrolene Derivatives Specific for the Plasmodial Surface Anion Channel. Mol. Pharmacol. 2005, 68, 34-40. |
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Zhaoa, Q.; Maa, L.; Jiangb, S.; Lub, H.; Liub, S.; Heb, Y.; Strickc, N.; Neamatid, N.; Debnatha, A. K.; Identification of N-phenyl-N'-(2,2,6,6-tetramethyl-piperidin-4-yl)-oxalamides as a new class of HIV-1 entry inhibitors that prevent gp120 binding to CD4. Virology 2005, 339 (2), 213-225. |
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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.; Small molecules that delay S phase suppress a zebrafish bmyb mutant. Nature Chem. Bio. 2005, 1 (7), 366-370. |
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Gilmour, R.; Foster, J. E.; Sheng, Q.; McClain, J. R.; Riley, A.; Sun, P.; Ng, W.; Yan, D.; Nicas, T. I.; Henry, K.; Winkler, M. E.; New Class of Competitive Inhibitor of Bacterial Histidine Kinases. J. of Bacteriology 2005, 187 (23), 8196-8200. |
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Gurova, K. V.; Hill, J. E.; Guo, C.; Prokvolit, A.; Burdelya, L. G.; Samoylova, E.; Khodyakova, A. V.; Ganapathi, R.; Ganapathi, M.; Tararova, N. D.; Bosykh, D.; Lvovskiy, D.; Webb, T. R.; Stark, G. R.; Gudkov, A. V.; Small molecules that reactivate p53 in renal cell carcinoma reveal a NF-kB-dependent mechanism of p53 suppression in tumors. PNAS 2005, 102 (48), 17448-17453. |
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Kang, S.; Li, H.; Rao, A.; Hogan, P. G.; Inhibition of the Calcineurin-NFAT Interaction by Small Organic Molecules Reflects Binding at an Allosteric Site. J. of Biological Chemistry 2005, 280 (45), 37698-37706. |
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Hung, D. T.; Shakhnovich, E. A.; Pierson, E.; Mekalanos, J. J.; Small-Molecule Inhibitor of Vibrio Cholerae Virulence and Intestinal Colonization. Science 2005, 310, 670-674. |
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Bertsch, U.; Winklhofer, K. F.; Hirschberger, T.; Bieschke, J.; Weber, P.; Hartl, F. U.; Tavan, P.; Tatzelt, J.; Kretzschmar, H. A.; Giese, A.; Systematic Identification of Antiprion Drugs by High-Throughput Screening Based on Scanning for Intensely Fluorescent Targets. J. of Virology 2005, 79 (12), 7785-7791. |
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Zhang, X.; Smith, D. L.; Meriin, A. B.; Engemann, S.; Russel, D. E.; Roark, M.; Washington, S. L.; Maxwell, M. M.; Marsh, J. L.; Thompson, L. M.; Wanker, E. E.; Young, A. B.; Housman, D. E.; Bates, G. P.; Sherman, M. Y.; Kazantsev, A. G.; A potent small molecule inhibits polyglutamine aggregation in Huntington's disease neurons and suppresses neurodegeneration in vivo. PNAS 2005, 102 (3), 892-897. |
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Ason, B.; Knauss, D. J.; Balke, A. M.; Merkel, G.; Skalka, A.; Reznikoff, W. S.; Targeting Tn5 Transposase Identifies Human Immunodeficiency Virus Type 1 Inhibitors. Antimicrobial Agents and Chemotherapy 2005, 49 (5), 2035-2043. |
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Surpin, M.; Rojas-Pierce, M.; Carter, C.; Hicks, G. R.; Vasquez, J.; Raikhel, N. V.; The power of chemical genomics to study the link between endomembrane system components and the gravitropic response. PNAS 2005, 102 (13), 4902-4907. |
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Huynh, C.; Andrews, N. W.; The small chemical vacuolin-1 alters the morphology of lysomes without inhibiting Ca²+-regulated exocytosis. EMBO 2005, 6 (9), 843-847. |
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Dai, X.; Hayashi, K.; Nozaki, H.; Cheng, Y.; Zhao, Y.; Genetic and chemical analyses of the action mechanisms of sirtinol in Arabidopsis. PNAS 2005, 102 (8), 3129-3134. |
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Degterev, A.; Huang, Z.; Boyce, M.; Li, Y.; Jagtap, P.; Mizushima, N.; Cuny, G. D.; Mitchison, T. J.; Moskowitz, M. A.; Yuan, J.; Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nature Chem. Bio. 2005, 1 (2), 112-119. |
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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; A Selective Inhibitor of eIF2α Dephosphorylation Protects Cells from ER Stress. Science 2005, 307, 935-939. |
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Zon, L. I.; Peterson, R. T.; In Vivo Drug Discovery in the Zebrafish. Nature Reviews Drug Discovery 2005, 4, 35-44. |
2004
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Im, I.; Webb, T. R.; Gong, Y.; Kim, J.; Kim, Y.; Solid-Phase Synthesis of Tetrahydro-1,4-benzodiazepine-2-one Derivatives as a â-Turn Peptidomimetic Library. J. Comb. Chem. 2004, 6, 207-213. |
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Zaks-Makhina, E.; Kim, Y.; Aizenman, E.; Levitan, E. S.; Novel Neuroprotective K+ Channel Inhibitor Identified by High-Throughput Screening in Yeast. Mol. Pharmacol. 2004, 65, 214-219. |
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Wu, S.; Zhu, H.; Gu, J.; Zhang, L.; Teraishi, F.; Davis, J. J.; Jacob, D. A.; Fang, B.; Induction of Apoptosis and Down-Regulation of Bcl-XL in Cancer Cells by a Novel Small Molecule, 2[[3-(2,3-Dichlorophenoxy)propyl]amino]ethanol. Cancer Res. 2004, 64, 1110-1113. |
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Zhu, H.; Zhang, L.; Wu, S.; Teraishi, F.; Davis, J. J.; Jacob, D.; Fang, B.; Induction of S-phase arrest and p21 overexpression by a small molecule 2[[3-(2,3-dichlorophenoxy)propyl] amino]ethanol in correlation with activation of ERK. Oncogene 2004, 23, 4984-4992. |
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Peterson, J. R.; Bickford, L. C.; Morgan, D.; Kim, A. S.; Ouerfelli, O.; Kirschner, M. W.; Rosen, M. K.; Chemical inhibition of N-WASP by stabilization of a native autoinhibited conformation. Nat. Struct. Mol. Biol. 2004, 11 (8), 747-755. |
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Jiang, S.; Lu, H.; Liu, S.; Zhao, Q.; He, Y.; Debnath, A. K.; N-Substituted Pyrrole Derivatives as Novel Human Immunodeficiency Virus Type 1 Entry Inhibitors That Interfere with the gp41 Six-Helix Bundle Formation and Block Virus Fusion. Antimicrobial Agents and Chemotherapy 2004, 48 (11), 4349-4359. |
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Desai, P. V.; Patny, A.; Sabnis, Y.; Tekwani, B.; Gut, J.; Rosenthal, P.; Srivastava, A.; Avery, M.; Identification of Novel Parasitic Cysteine Protease Inhibitors Using Virtual Screening. 1. The ChemBridge Database. Journal of Medicinal Chemistry 2004, 47 (26), 6609-6615. |
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Fiebiger, E.; Hirsch, C.; Vyas, J. M.; Gordon, E.; Ploegh, H. L.; Tortorella, D.; Dissection of the Dislocation Pathway for Type I Membrane Proteins with a New Small Molecule Inhibitor, Eeyarestatin. Molecular Biology of the Cell 2004, 15, 1635-1646. |
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Harrison, B. C.; Roberts, C. R.; Hood, D. B.; Sweeney, M.; Gould, J. M.; Bush, E. W.; McKinsey, T. A.; The CRM1 Nuclear Export Receptor Controls Pathological Cardiac Gene Expression. Molecular and Cellular Biology 2004, 24 (24), 10636-10649. |
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Min, D.; Tan, W.; Mrksich, M.; Chemical Screening by mass spectrometry to identify inhibitors of anthrax lethal factor. Nature Biotechnology 2004, 22 (6), 717-723. |
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Margolis, J.; Plowman, G. D.; Overcoming the gridlock in discovery research. Nature Biotechnology 2004, 22 (5), 522-524. |
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Peterson, R.T.; Shaw, S. Y.; Peterson, T. A.; Milan, D. J.; Zhong, T. P.; Schreiber, S. L.; MacRae, C. A.; Fishman, M. C.; Chemical suppression of a genetic mutation in a zebrafish model of aortic coarctation. Nature Biotechnology 2004, 22 (5), 595-599. |
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Kao, R. Y.; Tsui, W. H.W.; Lee, T. S.W.; Tanner, J. A.; Watt, R. M.; Huang, J.; Hu, L.; Chen, G.; Chen, Z.; Zhang, L.; He, T.; Chan, K.; Tse, H.; To, A. P.C.; Ng, L. W.Y.; Wong, B. C.W.; Tsoi, H.; Yang, D.; Ho, D. D.; Yuen, K.; Identification of Novel Small-Molecule Inhibitors of Severe Acute Respiratory Syndrome-Associated Coronavirus by Chemical Genetics. Chemistry & Biology 2004, 11, 1293-1299. |
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Lee, Y.; Bergson, P.; He, W. S.; Mrksich, M.; Tang, W.; Discovery of a Small Molecule that Inhibits the Interaction of Anthrax Edema Factor with Its Cellular Activator, Calmodulin. Chemistry & Biology 2004, 11, 1139-1146. |
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Armstrong, J. I.; Yuan, S.; Dale, J. M.; Tanner, V. N.; Theologis, A.; Identification of inhibitors of auxin transcriptional activation by means of chemical genetics in Arabidopsis. PNAS 2004, 101 (41), 14978-14983. |
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Margalit, D. N.; Romberg, L.; Mets, R. B.; Hebert, A. M.; Mitchison, T. J.; Kirschner, M. W.; RayChaudhuri, D.; Targeting cell division: Small-molecule inhibitors of FtsZ GTPase perturb cytokinetic ring assembly and induce bacterial lethality. PNAS 2004, 101 (32), 11821-11826. |
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Nieland, T. J. F.; Feng, Y.; Brown, J. X.; Chuang, T. D.; Buckett, P. D.; Wang, J.; Xie, X.; McGraw, T. E.; Kirchhausen, T.; Wessling-Resnick, M.; Chemical Genetic Screening Identifies Sulfonamides That Raise Organellar pH and Interfere with Membrane Traffic. Traffic 2004, 5, 478-492. |
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Won, J.; Chang, S.; Oh, S.; Kim, T. K.; Small-molecule-based identification of dynamic assembly of E2F-pocket protein-histone deacetylase complex for telomerase regulation in human cells. PNAS 2004, 101 (31), 11328-11333. |
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Soltero-Higgin, M.; Carlson, E. E.; Phillips, J. H.; Kiessling, L. L.; Identification of Inhibitors for UDP-Galactopyranose Mutase. J. Am. Chem. Soc. 2004, 126, 15924. |
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Venkatesh, N.; Feng, Y.; DeDecker, B.; Yacono, P.; Golan, D.; Mitchison, T.; McKeon, F.; Chemical genetics to identify NFAT inhibitors: Potential of targeting calcium mobilization in immunosuppression. PNAS 2004, 101 (24), 8969-8974. |
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Cerny, J.; Feng, Y.; Yu, A.; Miyake, K.; Borgonovo, B.; Klumperman, J.; Meldolesi, J.; McNeil, P. L.; Kirchhausen, T.; The small chemical vacuolin-1 inhibits Ca²+-dependent lysosomal exocytosis but not cell resealing. EMBO 2004, 5 (9), 883-888. |
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Cheng, D.; Yadav, N.; King, R. W.; Swanson, M. S.; Weinstein, E. J.; Bedford, M. T.; Small Molecule Regulators of Protein Arginine Methyltransferases. Journal of Biological Chemistry 2004, 279 (23), 23892-23899. |
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Nieland, T. J. F.; Chroni, A.; Fitzgerald, M. L.; Maliga, Z.; Zannis, V. I. Kirchhausen, T.; Krieger, M.; Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide. J. of Lipid Research 2004, 45, 1256-1265. |
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Zouhar, J.; Hicks, G. R.; Raikhel, N. V.; Sorting inhibitors (Sortins): Chemical compounds to study vacuolar sorting in Arabidopsis. PNAS 2004, 101 (25), 9497-9501. |
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Bush, E.; Fielitz, J.; Melvin, L.; Martinez-Arnold, M.; McKinsey, T. A.; Plichta, R.; Olson, E. N.; A small molecular activity of cardiac hypertrophy uncovered in a chemical screen for modifiers of the calcineurin signaling pathway. PNAS 2004, 101, 2870-2875. |
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Baurin, N.; Baker, R.; Richardson, C.; Chen, I.; Foloppe, N.; Potter, A.; Jordan, A.; Roughley, S.; Parratt, M.; Greaney, P.; Morley, D.; Hubbard, R.E.; Drug-like Annotation and Duplicate Analysis of a 23-Supplier Chemical Database Totalling 2.7 Million Compounds. J. Chem. Inf. Comput. Sci. 2004, 44, 643-651. |
2003
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Chianelli, D.; Kim, Y.; Lvovskiy, D.; Webb, T. R.; Application of a Novel Design Paradigm to Generate General Nonpeptide Combinatorial Scaffolds Mimicking Beta Turns: Synthesis of Ligands for Somatostatin Receptors. Bioorg. & Med. Chem. 2003, 11 (23), 5059-5068. |
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Kau, T. R.; Schroeder, F.; Ramaswamy, S.; Wojciechowski, C. L.; Zhao, J. J.; Roberts, T. M.; Clardy, J.; Sellers, W. R.; Silver, P. A.; A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells. Cancer Cell 2003, 4, 463-476. |
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Fulco, M.; Schlitz, R. L.; Iezzi, S.; King, M. T.; Zhao, P.; Kashiwaya, Y.; Hoffman, E.; Veech, R. L.; Sartorelli, V.; Sir2 Regulates Skeletal Muscle Differentiation as a Potential Sensor of the Redox State. Molecular Cell 2003, 12, 51-62. |
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Koller, K. M.; Haggarty, S. J.; Perkins, B. D.; Leykin, I.; Wong, J. C.; Ming-Chih, J. K.; Schreiber, S. L.; Chemical Genetic Modifier Screens: Small Molecule Trichostatin Suppressors as Probes of Intracellular Histone and Tubulin Acetylation. Chemistry & Biology 2003, 10, 397-410. |
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French, K.J.; Schrecengost, R.S.; Lee, B.D.; Zhuang, Y.; Smith, S.N.; Eberly, J.L.; Yun, J.K.; Smith, C.D.; Discovery and Evaluation of Inhibitors of Human Sphingosine Kinase. Cancer Research 2003, 63, 5962-5969. |
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Jenkins, J. L.; Shapiro, R.; Identification of Small-Molecule Inhibitors of Human Angiogenin and Characterization of Their Binding Interactions Guided by Computational Docking. Biochemistry 2003, 42, 6674-6687. |
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Yin, X.; Giap, C.; Lazo, J. S.; Prochownik, E. V.; Low molecular weight inhibitors of Myc-Max interaction and function. Oncogene 2003, 22, 6151-6159. |
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Bae, Y.; Lee, T. G.; Park, J. C.; Hur, J. H.; Kim, Y.; Heo, K.; Kwak, J.; Suh, P.; Ryu, S. H.; Identification of a Compound That Directly Stimulates Phospholipase C Activity. Molecular Pharmacology 2003, 63, 1043-1050. |
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Feng, Y.; Yu, S.; Lasell, T. K. R.; Jadhav, A. P.; Macia, E.; Chardin, P.; Melancon, P.; Roth, M.; Mitchison, T.; Kirchhausen, T.; Exo1: A new chemical inhibitor of the exocytic pathway. PNAS 2003, 100 (11), 6469-6474. |
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Windsor, B.; Roux, S. J.; Lloyd, A.; Multiherbicide tolerance conferred by AtPgp1 and apyrase overexpression in Arabidopsis thaliana. Nature Biotechnology 2003, 21, 428-433. |
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Webb, T. R.; Lvovskiy, D.; Kim, S. A.; Ji, X.; Melman, N.; Linden, J.; Jacobson, K. A.; Quinazolines as Adenosine Receptor Antagonists: SAR and Selectivity for A(2B) Receptors. Bioorganic & Medicinal Chemistry 2003, 11 (1), 77-85. |
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Jenkins, J. L.; Kao, R. Y.; Shapiro, R.; Virtual Screening to Enrich Hit Lists from High-Throughput Screening: A Case Study on Small-Molecule Inhibitors of Angiogenin. Proteins: Structure, Function, and Genetics 2003, 50 (1), 81-93. |
2002
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Ma, T.; Thiagarajah, J. R.; Yang, H.; Sonawane, N. D.; Folli, C.; Galietta, L. J. V.; Verkman, A. S.; Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. The Journal of Clinical Investigation 2002, 110 (11), 1651-1658. |
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Nieland, T. J. F.; Penman, M.; Dori, L.; Krieger, M.; Kirchhausen, T.; Discovery of chemical inhibitors of the selective transfer of lipids mediated by the HDL receptor SR-BI. PNAS 2002, 99 (24), 15422-15427. |
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Windsor, J. B.; Thomas, C.; Hurley, L.; Roux, S.J.; Lloyd, A.M.; Automated Colorimetric Screen for Apyrase Inhibitors. BioTechniques 2002, 33, 1024-1030. |
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Chen, J. K.; Taipale, J.; Young, K. E.; Maiti, T.; Beachy, P. A.; Small molecule modulation of Smoothened activity. PNAS 2002, 99 (22), 14071-14076. |
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Ma, T.; Vetrivel, L.; Yang, H.; Pedemonte, N.; Zegarra-Moran, O.; Galietta, L. J. V.; Verkman, A. S.; High-affinity Activators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Chloride Conductance Identified by High-throughput Screening. The Journal of Biological Chemistry 2002, 277 (40), 37235-37241. |
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Kao, R. Y. T.; Jenkins, J. L.; Olson, K. A.; Key, M. E.; Fett, J. W.; Shapiro, R.; A small-molecule inhibitor of the ribonucleolytic activity of human angiogenin that possesses antitumor activity. PNAS 2002, 99 (15), 10066-71. |
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Sohn, T. A.; Bansal, R.; Su, G. H.; Murphy, K. M.; Kern, S. E.; High-throughput measurement of the Tp53 response to anticancer drugs and random compounds using a stably integrated. Carcinogenesis 2002, 23 (6), 949-957. |
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Cheung, A.; Dantzig, J. A.; Hollingworth, S.; Baylor, S. M.; Goldman, Y.E.; Mitchison, T. J.; Straight, A. F. A small-molecule inhibitor of skeletal muscle myosin II. Nature Cell Biology 2002, 4, 83-84. |
2001
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Kondratov, R.V.; Komarov, P.G.; Becker, Y.; Ewenson, A.; Gudkov, A. Small molecules that dramatically alter multidrug resistance phenotype by modulating the substrate specificity of P-glycoprotein. PNAS 2001, 98 (24), 14078-83. |
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Peterson, R.T.; Mably, J.D.; Chen, J.; Fishman, M. C. Convergence of distinct pathways to heart patterning revealed by the small molecule concentramide and the mutation heart-and-soul. Current Biology 2001, 11, 1481-1491. |
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Torrance, C.J.; Agrawal, V.; Vogelstein, B.; Kinzler, K. W. Use of Isogenic Human Cancers Cells for High-throughput Screening and Drug Discovery. Nature Biotechnology 2001, 19, 940-945. |
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Sohn, T. A.; Su, G. H.; Ryu, B.; Yeo, C. J.; Kern, S. E.; High-Throughput Drug Screening of the DPC4 Tumor-Suppressor Pathway in Human Pancreatic Cancer Cells. Annals of Surgery 2001, 233 (5), 696-703. |
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Grozinger, C. M.; Chao, E.D.; Blackwell, H.E.; Moazed, D.; Schreiber, S. L. Identification of a Class of Small Molecule Inhibitors of the Sirtuin Family of NAD-dependent Deacetylases by Phenotypic Screening. J. Bio. Chem. 2001, 276 (42), 38837. |
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Degterev, A.; Lugovskoy, A.; Cardone, M.; Mulley, B.; Wagner, G.; Mitchison, T.; Yuan, J. Identification of Small-Molecule Inhibitors of Interaction between the BH3 Domain and Bcl-xL. Nature Cell Biology 2001, 3, 173-82. |
2000
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Peterson, R.; Link, B.A.; Dowling, J.E.; Schreiber, S. L. Small Molecule Developmental Screens Reveal the Logic and Timing of Vertebrate Development. PNAS 2000, 97, 12965-69. |
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Kim, T.; Kim, T.Y.; Lee, W.G.; Yim, J.; Kim; T.K.. Signaling Pathways to the Assembly of an Interferon-B Enhanceosome. J. Biol. Chem. 2000, 275, 16910-17. |
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1999
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Mayer, T. U.; Kapoor, T.M.; Haggarty, S.J.; King, R.W.; Screiber, S.L.; Mitchison, T. J. Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype-based Screen. Science 1999, 286, 971-74. |
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Komarov, P. G.; Komarova, E. A.; Kondratov, R. V.; Christov-Tselkov, K.; Coon, J. S.; Chernov, M. V.; Gudkov, A. V. A Chemical Inhibitor of p53 that Protects Mice from the Side Effects of Cancer Therapy. Science 1999, 285, 1733-37. |
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Markham, P.N.; Westhaus, E.; Klyachko, K.; Johnson, M.E.; Neyfakh, A. A. Multiple Novel Inhibitors of the NorA Multidrug Transporter of Staphylococcus aureus. Antimicrobial Agents and Chemotherapy 1999, 43, 2404-08. |
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Stockwell, B.R.; Hardwick, J.S.; Tong, J.K.; Schreiber, S. L. Chemical genetic and genomic approaches reveal a role for copper in specific gene activation. J. of Amer. Chem. Society 1999, 121, 10662-10663. |
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