Faculty
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Kerwin, Sean
Associate Professor in Pharmacy G. D. Searle Fellow
E-mail Website Main Office: BME 6.202C Phone: 471-5074 Alternate Office: BME 6.302 Phone: 471-7546 Mailing Address: The University of Texas at Austin - ICMB 1 University Station C0850 Austin, TX 78712-1095
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Research Lab Students:
Graduate Student
- David, Wendi - Graduate Student
- Feng, Liping - Graduate Student
- Kern, Jonathan - Graduate Student
- Marriner, Wendy - Graduate Student
- McPhee, Mark - Graduate Student
- Nadipuram, Asha - Graduate Student
- Rodriguez, Mireya - Graduate Student
- Tuesuwan, Bodin - Graduate Student
Research Summary:
The long-term goal of our research is the development of selective strategies for the treatment of cancer, inflammation, and infectious diseases. Our work takes place at the interface of computational chemistry, synthesis, biochemistry, and molecular biology. The targets of current interest include certain nucleic acid sequences and their associated structures, such as G-quadruplexes, kinases implicated in cancer and inflammation, and as yet undefined targets of structurally and functionally interesting anti-cancer and anti-inflammitory natural products . Structural and biochemical characterization of these targets enables us to use computational and combinatorial chemistry techniques to discover compounds that combine recognition of the targets with the desired biological effects.
Research Images: Complex of Human Telomeric G-Quadruplex DNA with TEL01 - The perylenediimide TEL01 was designed to bind to the four-stranded G-qaudruplex form (G4) of the Human telomeric repeat sequence [d(TAGGGTTA)]4. In this NMR-based model of the Tel01-G4 complex, the ligand is stacked on the 3’ G-tetrad face with the morpholinopropyl sidearms positioned in the grooves of the DNA. The DNA thymine residues are shown in aqua, adenines in purple, and guanosines in yellow. The ligand is CPK rendered with carbons in green, oxygen in red, and nitrogen in blue. |
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Publications:| 2010 | Wang X, Stavchansky S, Kerwin SM, Bowman PD, Structure-activity relationships in the cytoprotective effect of caffeic acid phenethyl ester (CAPE) and fluorinated derivatives: effects on heme oxygenase-1 induction and antioxidant activities, Eur J Pharmacol. 635:16-22. | | 2010 | Laroche C, Li J, Gonzales C, David WM, Kerwin SM., Cyclization kinetics and biological evaluation of an anticancer 1,2-dialkynylimidazole., Org Biomol Chem. 8:1535-9. | | 2009 | Li J, Kaoud TS, Laroche C, Dalby KN, Kerwin SM., Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles, Bioorg Med Chem Lett. 19:6293-7. | | 2008 | McKee ML, Kerwin SM., Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1., Bioorg Med Chem. 16:1775-83. | | 2008 | Tuesuwan B, Kern JT, Thomas PW, Rodriguez M, Li J, David WM, Kerwin SM., Simian virus 40 large T-antigen G-quadruplex DNA helicase inhibition by G-quadruplex DNA-interactive agents., Biochemistry 47:1896-909. |
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