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2000
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Herradura, P. S.; Pendola, K. A.; Guy, R. K. "Copper-Mediated Cross-Coupling of Aryl Boronic Acids and Alkyl Thiols," Org. Lett. 2000 , 2 , 2019-22.
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2001
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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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2002
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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.
2003
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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.
2004
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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
2005
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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 Mechanism of 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.
2006
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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.
STKE, 2006, pl3.
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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.
2007
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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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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.
2008
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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. 2008, 51(3):545-552.
2009
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Jones JO, Bolton EC, Huang Y, Feau C, Guy RK, Yamamoto KR, Hann B, Diamond MI. "Ligand independent androgen receptor inhibition in vitro and in vivo," Proc Natl Acad Sci USA. 2009, 106(17):7233-7238, PMCID: PMC2678452.
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Reed D, Ying S, Shelat A, Mills N, Smithson D, Arnold A, Otieno S, Regni C, Zhu F, Kriwacki R, Schulman B, Guy RK, Dyer MA. "Identification and characterization of a small molecule inhibitor of MDMX," J Biol Chem. 2009, in press. J PMCID: PMC Journal.
2010
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Reed D, Ying S, Shelat A, Mills N, Smithson D, Arnold A, Otieno S, Regni C, Zhu F, Kriwacki R, Schulman B, Guy RK, Dyer MA. "Identification and characterization of a small molecule inhibitor of MDMX," J Biol Chem 285(14):10786-10796, 2010.
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Guiguemde WA, Shelat AA, Bouck D, Duffy S, Crowther GJ, Davis PH, Smithson DC, Connelly M, Clark J, Zhu F, Jimenez-Diaz MB, Martinez MS, Wilson EB, Tripathi AK, Gut J, Sharlow ER, Bathurst I, El Mazouni F, Fowble JW, Forquer I, McGinley PL, Castro S, Angulo-Barturen I, Ferrer S, Rosenthal PJ, Derisi JL, Sullivan DJ, Lazo JS, Roos DS, Riscoe MK, Phillips MA, Rathod PK, Van Voorhis WC, Avery VM, Guy RK. Chemical genetics of Plasmodium falciparum Nature 465(7296):311-315, 2010.
2011
Lowes DJ, Guiguemde WA, Connelly MC, Zhu F, Sigal MS, Clark JA, Lemoff AS, Derisi JL, Wilson EB, Guy RK. Optimization of propafenone analogues as antimalarial leads. J Med Chem 54(21):7477-85, 2011.
Zhang F, Tagen M, Throm S, Mallari J, Miller L, Guy RK, Dyer MA, Williams RT, Roussel MF, Nemeth K, Zhu F, Zhang J, Lu M, Panetta JC, Boulos N, Stewart CF. Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration Drug Metab Dispos 39(1):15-21, 2011.