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To download a PDF version of the paper or supplemental materials, click on the link.
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| Geistlinger, T. R.; Guy, R. K. "An inhibitor of the interaction of thyroid hormone receptor beta and glucocorticoid interacting protein 1," J Am Chem Soc 2001 , 123 , 1525-6. |
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| Novak, K.; Fujii, N.; Guy, R. K. "Investigation of the PDZ domain ligand binding site using chemically modified peptides," Bioorg Med Chem Lett 2002 , 12 , 2471. |
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Harris, B. Z.; Lau, F. W.; Fujii, N.; Guy, R. K.; Lim, W. A. “Role of Electrostatic Interactions in PDZ Domain Ligand Recognition,” Biochemistry , 2003 , 42 , 2797-2805. |
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| Geistlinger, T. R.; Guy, R. K. “Novel Selective Inhibitors of the Interaction of Individual Nuclear Hormone Receptors with a Mutually Shared Steroid Receptor Coactivator 2,” J. Am. Chem. Soc. 2003 , 125 , 6852-6853 |
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| Springsteel, M. F; Galietta, L. J. V.; Ma, T.; By, K.; Berger, G. O.; Yang, H.; Dicus, C. W.; Choung, W.; Quan, C.; Shelat, A. A.; Guy, R. K.; Verkman, A. S.; Kurth, M. J.; Nantz, M. H. “Benzoflavone Activators of the Cystic Fibrosis Transmembrane Conductance Regulator: A Pharmacophorme Model of Flavone-CFTR Binding,” Bioorg Med Chem , 2003 , 11 , 4113-4120. |
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| Yang, H; Shelat, A. A.; Guy, R. K.; Gopinath, V. S.; Ma, T.; Du, K.; Lukacs, G. L.; Taddei, A.; Folli, C.; Pedemonte, N.; Galietta, L. J. V.; Verkman, A. S. “Nanomolar Affinity Small-Molecule Correctors of Defective dF508-CFTR Chloride Channel Gating,” J. Biol. Chem. 2003 , 278 , 35079-35085. |
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| Fujii, N.; Haresco, J. J.; Pendola-Novak, K. A.; Stokoe, D.; Kuntz, I. D.; Guy, R. K., “A Selective Irreversible Inhibitor Targeting a PDZ Protein Interaction Domain,” J Am Chem Soc , 2003 , 125 , 12074-12075. |
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| Gochin, M.; Guy, R. K.; Case, M.; “A metallo-peptide assembly in fluorescence detection of ligand binding to the HIV-1 gp41 coiled coil,” Angew. Chem. Int. Ed. Engl. 2003 , 5325-5328 |
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| Collins, C; Schilling, B.; Young, M.; Dollinger, G.; Guy, R. K. “Isotopically Labeled Crosslinking Reagents: Resolution of Mass Degeneracy in the Identification of Crosslinked Peptides,” Bioorg Med Chem , 2003 , 13 , 4023-4026. |
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Geistlinger, T. R.; Guy, R. K. “Selective inhibitors of nuclear hormone receptor coactivator binding,” Methods Enzymol. 2003 , 364, 223-46. |
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| Fujii, N.; Haresco, J. J.; Pendola-Novak, K. A.; Stokoe, D.; Gage, M.; Von Zastrow, M.; Kuntz, I. D.; Guy, R. K. “Design and Synthesis of Inhibitors of the PDZ Protein Interaction Domain,” Innov. Persp. Solid Phase Synth. & Combi. Chem. Lib. 2004 , 8 , 163-166. |
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| Fujii, N.; Jacobsen, R. B.; Wood, N. L.; Schoeniger, J. S.; Guy, R. K. “A Novel Protein Crosslinking Reagent for the Determination of Moderate Resolution Protein Structures by Mass Spectrometry (MS3D),” Bioorg Med Chem Lett. 2004 , 14 , 427-429. |
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| Geistlinger, T. L.; McReynolds, A.; Guy, R. K. “Ligand Selective Inhibition of the Interaction of Steroid Receptor Coactivators and the Estrogen Receptor,” Chem. Biol. 2004 , 11 , 273-281. |
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| Evans, W. E.; Guy, R. K. “Gene Expression as a Drug Discovery Tool,” Nature Genetics , 2004 , 36 , 214-215. |
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| Madrid, P. B.; Wilson, N.; DeRisi, J. L.; Guy, R. K., “Parallel Synthesis and Antimalarial Screening of a 4-Aminoquinoline Library,” J. Comb. Chem. 2004 , 6(3) , 437-442. |
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| Moore, J. M. R.; Galicia, S. L.; McReynolds, A.; Ha, N. G.; Scanlan, T. S.; Guy, R. K. “Quantitative Proteomics of the Thyroid Hormone Receptor Coactivator Interaction,” J. Biol. Chem. 2004 , 279(26) , 27584-27590. |
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| Arnold, A.; Luo, W.; Guy, R. K. “Synthesis of Medium Ring Heterocycles using an Intramolecular Heck Reaction,” Org. Lett. 2004 , 6(17) , 3005-3007. |
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| Anderson, M.; Moser, J.; Sherrill, J.; Guy, R. K., “A Convenient Procedure for Hydrolysis of Esters in Parallel Syntheses,” Synlett 2004 , 13 , 2391-2399 |
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| Fujii, N. Mallari, J. P.; Hansell, E. J.; Mackey, Z.; Doyle, P.; Zhou, Y. M.; Rosenthal, P. J.; McKerrow, J. H.; Guy, R. K. “Discovery of Potent Thiosemicarbazone Inhibitors of Rhodesain and Cruzain,” Bioorg Med. Chem. Lett. 2005 , 15(1) , 121-123. |
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| Estébanez-Perpiñá, E.; Moore, J. M. R.; Mar, E.; Nguyen, P.; Delgado-Rodrigues, E.; Baxter, J.; Buehrer, B. M.; Webb, P.; Fletterick, R. J.; Guy, R. K. “The Molecular Mechanisms of Coactivator Utilization in Ligand-dependent Transactivation by the Androgen Receptor”, J. Biol. Chem. 2005 , 280 , 8060-8. |
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| Krylova, I. N.; Sablin, E. P.; Williams, J. D.; Williams, S. P.; Moore, J. M. R.; Xu, R. X. Waitt, G. M.; Juzumiene, D.; Bynum, J. M.; Montana, V.; Guy, R. K.; Thornton, J. W.; Fletterick, R. J.; Willson, T. M.; Ingraham, H. A. “Structural analyses of NR5 orphan receptors reveal a potential role as nuclear phospholipid sensors,” Cell , 2005 , 120 , 343-55. |
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| Madrid, P. B.; Liou, A. L.; Sherrill, J.; Weisman, J.; DeRisi, J. L.; Guy, R. K. “Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities,” Bioorg Med. Chem. Lett. 2005 , 15 , 1015-8. |
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| Anderson, M. A.; Shelat, A. A.; Guy, R. K. "A solid-phase approach to the phallotoxins: Total Synthesis of [Ala7]-phalloidin," J. Org. Chem. , 2005 , 70 , 4578-4584. |
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Feng, B. Y.; Shelat, A. A.; Doman, T. N.; Guy, R. K.; Shoichet, B. K. “ High-Throughput Assays for Promiscuous Inhibitors.” Nature Chemical Biology. , 2005 , 1 , 146-148. |
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| Moore, J. M.; Guy, R. K. “Co-regulators of Thyroid Hormone Receptor Signaling,” Clinical Proteomics , 2005 , 4 , 475-482. |
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Anderson, M. O.; Sherrill, J.; Madrid, P. B.; Liou, A. P.; Weisman, J. L.; Derisi, J. L.; and Guy, R. K., "Parallel synthesis of 9-aminoacridines and their evaluation against chloroquine-resistant Plasmodium falciparum , " Bioorg Med Chem , 2006 . 14(2) : 334-43. |
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Arnold, L. A.; Estebanez-Perpina, E.; Togashi, M.; Jouravel, N.; Shelat, A.; McReynolds, A. C.; Mar, E.; Nguyen, P.; Baxter, J. D.; Fletterick, R. J.; Webb, P.; and Guy, R. K., "Discovery of small molecule inhibitors of the interaction of thyroid hormone receptor with transcriptional coregulators , " J Biol Chem , 2005, 280(52) , 43048-55. |
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Lu, F.; Chi, S.-W.; Kim, D.-H.; Han, K.-H.; Kuntz, I. D.; Guy, R. K.; “Proteomimetic Libraries: Design, Synthesis, and Evaluation of p53-MDM2 Inhibitors,” J. Combi. Chem. , 2006, 8(3), 315-325.
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| Mills, N. L.; Daugherty, M. D.; Frankel, A. D.; Guy, R. K. “An a -helical inhibitor of the HIV-1 Rev-RRE Interaction,” J. Am. Chem. Soc. , 2006, 128(11), 3496-7 |
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Mackey, Z. B.; Baca, A. M.; Fujii, N.; Apsel, B.; Shelat, A.; Hansell, E. J.; Chiang, P. K.; Wolff, B.; Guy, R. K.; Williams, J.; McKerrow, J.
"Discovery of trypanocidal compounds by whole cell HTS of live Trypanosoma brucei," Chem. Biol. Drug. Des., 2006, 67(5), 355-367. |
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| Madrid, P. B.; Liou, A. L.; DeRisi, J. L.; Guy, R. K. "Incorporation of an Intramolecular Hydrogen-bonding Motif in the Side-Chain of 4-Aminoquinolines Enhances Activity against Drug-Resistant P. falciparum." J. Med. Chem. 2006, in press. |
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| May, B. C. H.; Witkop, J.; Sherrill, J.; Anderson, M. O.; Madrid, P. B.; Zorn, J. A.; Prusiner, S. B.; Cohen, F. E.; Guy, R. K, "Structure-activity Relationship Study of 9-Aminoacridine Compounds in Scrapie-Infected Neuroblastoma Cells," Bioorg. Med. Chem. Lett. 2006, in press. |
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Arnold, A.; Estébanez-Perpiñá, E; Togashi, M.; Shelat, A.; Ocasio, C.
A.; McReynolds, A. C.; Nguyen, P.; Baxter, J. D.; Fletterick, R. J.; Webb, P.; Guy, R. K. "A High-Throughput Screening Method to Identify Small Molecule Inhibitors of Thyroid Hormone Receptor Coactivator Binding," Sci.
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| Weisman, J. L.; Liou, A. P.; Shelat, A. A.; Cohen, F. E.; Guy, R. K; DeRisi, J. L. "Searching for New Antimalarial Therapeutics amongst Known Drugs," Chem. Biol. Drug. Des., 2006, 67(5), 409-416. |
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| Arnold, A.; Guy, R. K. "Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors,"
Bioorg. Med. Chem. Lett. 2006, in press. |
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Mayer, M.; Lang, P. T.; Gerber, S.; Madrid, P. B.; Gomez-Pinto, I.; Guy, R. K.; James, T. L. “Synthesis and Testing of a Focused Phenothiazine Library for Binding to HIV-1 TAR RNA,” Chem. Biol. 2006, 13(9), 993-1000.
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| Anderson, M. O.; Yu, H.; Penaranda, C.; Maddux, B. A.; Goldfine, I. D.; Youngren, J. F.; Guy, R. K. "Parallel Synthesis of Diarylureas and their Evaluation as Inhibitors of Insulin-Like Growth Factor Receptor," J. Comb. Chem., 2006, 8(5), 784-90. |
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| Fujii, N.; Haresco, J. J.; Novak, K. A. P.; Gage, R. M.; Pedemonte, N.; Stokoe, D.; Kuntz, I. D.; Guy, R. K. "Rational Design of a Nonpeptide General Chemical Scaffold for Reversible Inhibition of PDZ Domain Interactions," Bioorg. Med. Chem. Lett. 2006, 17(2), 549-552. |
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| Fujii, N.; Shelat, A.; Hall, R. A.; Guy, R. K. "Design of a Selective Chemical Probe for Class I PDZ Domains," Bioorg. Med. Chem. Lett. 2006, 17(2), 546-548. |
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| Laurie, N. A.; Donovan, S. L; Shih, C.-S.; Zhang, J.; Mills, N.; Fuller, C.; Teunisse, A.; Lam, S.; Ramos, Y.; Mohan, A.; Johnson, D.; Wilson, M.; Rodriguez-Galindo, C.; Quarto, M.; Francoz, S.; Mendrysa, S. M.; Guy, R. K.; Marine, J.-C.; Jochemsen, A. G.; Dyer, M. A. "Inactivation of the p53 Pathway in Retinoblastoma," Nature, 2006, 444(7115), 66-69. |
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| Fujii, N.; You, L.; Xu, Z.; Uematsu, K.; Shan, J.; He, B.; Mikami, I.; Edmondson, L. R.; Neale, G.; Zheng, J.; Guy, R. K.; Jablons, D. M. "An Antagonist of Dishevelled Protein-Protein Interaction Suppresses b-catenin Dependent Tumor Cell Growth," Cancer Research, 2007, 67(2), 573-579. |
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| Warhust, D. C.; Craig, J. C.; Adagu, I. S.; Guy, R. K.; Madrid, P. B.; Fivelman, Q. L. "Activity of Piperaquine and other 4-aminoquinoline Antiplasmodial Drugs against Chloroquine-sensitive and Resistant Blood-stages of Plasmodium Falciparum. Role of beta-haematin inhibition and drug concentration in vacuolar water- and liquid-phases," Biochem. Pharmacol. 2007, 73(12), 1910-1926. |
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| Inglese, J.; Shamu, C. E.; Guy, R. K. "Reporting Data from High Throughput Screening of Small Molecule Libraries," Nat. Chem. Biol. 2007, 3(8) 438-441. |
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| Shelat, A.; Guy, R. K. "The Interdependence between Screening Methods and Screening Libraries," Curr. Op. Chem. Biol. 2007, 11(3), 244-251. |
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| Shelat, A.; Guy, R. K. "The Role of Scaffolds in Defining Functional Diversity of Screening Collections in Biologically Relevant Space," Nat. Chem. Biol. 2007, 3(8), 442-446. |
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| Mills, N. L.; Shelat, A. A.; Guy, R. K. "Assay Optimization and Screening of RNA:Protein Interactions by Alphascreen," J. Biomol. Screen. 2007, 12(7), 946-955. |
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| Arnold, A.; Kosinski, A.; Estebanez-Perpina, E; Fletterick, R. J.; Guy, R. K.; "Inhibitors of the Interaction of Thyroid Hormone Receptor and Coactivators: Preliminary Structure Activity Relationships," J. Med. Chem. 2007, 50(22), 5269-5280. |
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| Guy, R. K. "Cures for Neglected Diseases: Alternative Strategies for Finding Drugs," Curr. Op. Chem. Biol. 2007, 11(4), 10-11. |
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| Hyatt, J. L.; Wadkins, R. M.; Tsurkan, L.; Hicks, L. D.; Hatfield, M. J.; Edwards, C. C.; Ross, C. R.; Cantalupo, S. A.; Crundwell, G.; Guy, R. K.; Potter, P. M. "Planarity and Constraint of the Carbonyl Groups in 1,2-diones are Determinants for Selective Inhibition of Human Carboxylesterase 1," J. Med. Chem., 2007, 50(23), 5727-5734. |
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| Estebanez-Perpina, E.; Arnold, A. Webb, P.; Nguyen, P.; Delgado-Rodrigues, E.; Mar, E.; Bateman, R.; Pallai, P.; Shokat, K. M.; Baxter, J. D.; Guy, R. K.; Fletterick, R. J.; "A surface on the androgen receptor that allosterically regulates coactivator binding.," Proc. Natl. Acad. Sci. USA, 2007, 104(41), 16074-16079. |
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| Estebanez-Perpina, E.; Jouravel, N.; Arnold, A.; Togashi, M.; Blethrow, J.; Mar, E.; Nguyen, P.; Baxter, J. D.; Webb, P.; Guy, R. K.; Fletterick, R. J. "Structural Insight into the Mode of Action of a Direct Inhibitor of Thyroid Hormone Receptor Coregulator Binding," Mol. Endocrin., 2007, 21(12), 2919-2928. |
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| Mallari, J. P.; Shelat, A. A.; O'Brien, T.; Caffrey, C. R.' Kosinski, A.; Connelly, M.; McKerrow, J. H.; Guy, R. K. "Development of Potent Purine-Derived Nitrile Inhibitors of the Trypanosomal Protease TbCatB," J. Med. Chem. 2007, in press. |
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| Jouravel, N.; Sablin, E.; Arnold, L. A.; Guy, R. K.; Fletterick, R. J. "Interaction between the Androgen Receptor and a Segment of its Corepressor SHP," Acta Cryst. 2007, D63, 1198-1200. |
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