R. Kiplin Guy, PhD

    R. Kiplin Guy, PhD

    Member, St. Jude Faculty
    Chair, Chemical Biology & Therapeutics


    Chemical Biology & Therapeutics

    Contact Information

    R. Kiplin Guy, PhD
    Chemical Biology & Therapeutics
    MS 1000, Room E9050
    St. Jude Children's Research Hospital
    262 Danny Thomas Place
    Memphis, TN 38105-3678
    Email: kip.guy@stjude.org
    Phone: (901) 595-5714
    FAX: (901) 595-5715


    PhD - The Scripps Research Institute, La Jolla, California (1996)

    Research Interests

    Research Lab

    Selected Publications

    Zhang Y, Clark JA, Connelly MC, Zhu F, Min J, Guiguemde WA, Pradhan A, Iyer L, Furimsky A, Gow J, Parman T, El Mazouni F, Phillips MA, Kyle DE, Mirsalis J, Guy RK. Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials. J Med Chem 55(9): 4205-4219, 2012.

    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.

    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.

    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.

    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. 106(17):7233-7238, 2009. PMCID: PMC2678452. http://www.ncbi.nlm.nih.gov/pubmed

    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. 51(3): 545-552, 2008. http://www.ncbi.nlm.nih.gov/pubmed/18173229

    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. D63: 1198-1200, 2007. http://www.ncbi.nlm.nih.gov/pubmed

    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. 21(12): 2919-2928, 2007. http://www.ncbi.nlm.nih.gov/pubmed/17823305

    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 104(41): 16074-16079, 2007. http://www.ncbi.nlm.nih.gov/pubmed

    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. 50(23): 5727-5734, 2007. http://www.ncbi.nlm.nih.gov/pubmed

    Guy, R. K. "Cures for Neglected Diseases: Alternative Strategies for Finding Drugs," Curr. Op. Chem. Biol. 11(4): 10-11, 2007.

    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. 50(22): 5269-5280, 2007. http://www.ncbi.nlm.nih.gov/pubmed

    Mills, N. L.; Shelat, A. A.; Guy, R. K. "Assay Optimization and Screening of RNA:Protein Interactions by Alphascreen," J. Biomol. Screen. 12(7): 946-955, 2007. http://www.ncbi.nlm.nih.gov/pubmed

    Shelat, A.; Guy, R. K. "The Role of Scaffolds in Defining Functional Diversity of Screening Collections in Biologically Relevant Space," Nat. Chem. Biol. 3(8): 442-446, 2007. http://www.ncbi.nlm.nih.gov/sites/entrez

    Shelat, A.; Guy, R. K. "The Interdependence between Screening Methods and Screening Libraries," Curr. Op. Chem. Biol. 11(3): 244-251, 2007.http://www.ncbi.nlm.nih.gov/pubmed

    Inglese, J.; Shamu, C. E.; Guy, R. K. "Reporting Data from High Throughput Screening of Small Molecule Libraries," Nat. Chem. Biol. 3(8): 438-441, 2007.http://www.ncbi.nlm.nih.gov/pubmed/17637769

    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. 73(12): 1910-1926, 2007. http://www.ncbi.nlm.nih.gov/pubmed

    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 67(2): 573-579, 2007. http://www.ncbi.nlm.nih.gov/pubmed/17234765

    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, 444(7115): 66-69, 2006. http://www.ncbi.nlm.nih.gov/pubmed/17080083

    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. 17(2): 546-548, 2006. http://www.ncbi.nlm.nih.gov/pubmed

    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. 17(2): 549-552, 2006. http://www.ncbi.nlm.nih.gov/pubmed

    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. 8(5): 784-90, 2006. http://www.ncbi.nlm.nih.gov/pubmed

    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. 13(9): 993-1000, 2006. http://www.ncbi.nlm.nih.gov/pubmed/16984889

    Arnold, A.; Guy, R. K. "Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors," Bioorg. Med. Chem. Lett. in press, 2006. http://www.ncbi.nlm.nih.gov/pubmed/16890431

    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. 67(5): 409-416, 2006.http://www.ncbi.nlm.nih.gov/pubmed

    Last update: June 2012