R. Kiplin Guy, PhD

R. Kiplin Guy, PhD

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

Departments

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

Education

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


Research Interests

  • Orphan Diseases: malaria, sleeping sickness, retinoblastoma, ependymoma
  • Medicinal chemistry: parallel chemistry, peptidomimetics, hormone antagonists, protease inhibitors
  • Cellular biology: chemical target validation, lipid homeostasis, nuclear hormone receptors, protein interactions
  • High throughput screening: quantitative assays, data analysis methods

Research Lab

Selected Publications

Mallari JP, Shelat AA, O’Brien T, Caffrey CR, Kosinski A, Connelly M, McKerrow JH, Guy RK. Development of Potent Purine-Derived Nitrile Inhibitors of the Trypanosomal Protease TbCatB. J Med Chem 51(3), 545-552, 2008.

Estebanez-Perpina E, Jouravel N, Arnold A, Togashi M, Blethrow J, Mar E, Nguyen P, Baxter JD, Webb P, Guy RK, Fletterick RJ. Structural Insight into the Mode of Action of a Direct Inhibitor of Thyroid Hormone Receptor Coregulator Binding. Mol Endocrin 21(12), 2919-2928, 2007.

Madrid PB, Liou AL, DeRisi JL, Guy RK. Incorporation of an Intramolecular Hydrogen-bonding Motif in the Side-Chain of 4-Aminoquinolines Enhances Activity against Drug-Resistant P. falciparum. J Med Chem 49(15), 4535-4543, 2006.

Mills NL, Daugherty MD, Frankel AD, Guy RK. An a-helical inhibitor of the HIV-1 Rev-RRE Interaction. J Am Chem Soc128(11), 3496-7, 2006.

Arnold LA, Estebanez-Perpina E, Togashi M, Jouravel N, Shelat A, McReynolds AC, Mar E, Nguyen P, Baxter JD, Fletterick RJ, Webb P, Guy RK. Discovery of small molecule inhibitors of the interaction of thyroid hormone receptor with transcriptional coregulators. J Biol Chem 280(52), 43048-55, 2005.

Feng BY, Shelat AA, Doman TN, Guy RK, Shoichet BK. High-Throughput Assays for Promiscuous Inhibitors. Nature Chemical Biology 1: 146-148, 2005.

Anderson MA, Shelat AS, Moser J, Guy RK. A Novel Solid-phase Approach to the Phallotoxins: Total Synthesis of [Ala7]-Phalloidin. J Org Chem 70: 4578-4584, 2005.

Krylova IN, Sablin EP, Williams JD, Williams SP, Moore JMR, Xu RX, Waitt GM, Juzumiene D, Bynum JM, Montana V, Guy RK, Thornton JW, Fletterick RJ, Willson TM, Ingraham HA. Structural analyses of NR5 orphan receptors reveal a potential role as nuclear phospholipid sensors. Cell 120: 343-55, 2005.

Estébanez-Perpiñá E, Moore JMR, Mar E, Nguyen P, Delgado-Rodrigues E, Baxter J, Buehrer BM, Webb P, Fletterick RJ, Guy RK. The Mechanism of Ligand Dependent Transactivation by the Androgen Receptor. J Biol Chem 280: 8060-8, 2005.

Moore JMR, Galicia SL, McReynolds A, Ha NG, Scanlan TS, Guy RK. Quantitative Proteomics of the Thyroid Hormone Receptor Coactivator Interaction. J Biol Chem 279(26): 27584-27590, 2004.

Evans WE, Guy RK. Gene Expression as a Drug Discovery Tool. Nature Genetics 36: 214-215, 2004.

Fujii N, Haresco JJ, Pendola-Novak KA, Stokoe D, Kuntz ID, Guy RK. A Selective Irreversible Inhibitor Targeting a PDZ Protein Interaction Domain. J Am Chem Soc 125: 12074-12075, 2003.

Geistlinger TR, Guy RK. Novel Selective Inhibitors of the Interaction of Individual Nuclear Hormone Receptors with a Mutually Shared Steroid Receptor Coactivator 2. J Am Chem Soc 125: 6852-6853, 2003.

Harris BZ, Lau FW, Fujii N, Guy RK, Lim WA. Role of Electrostatic Interactions in PDZ Domain Ligand Recognition. Biochemistry 42: 2797-2805, 2003.

Geistlinger TR, Guy RK. An inhibitor of the interaction of thyroid hormone receptor beta and glucocorticoid interacting protein 1. J Am Chem Soc 123: 1525-6, 2001.

Last update: May 2008

 

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