Education
Ph.D., University of California, Irvine
Research Interests
Since joining SLU and the Center for World Health and Medicine in 2010 my research interests have focused on neglected diseases and diseases of poverty. These include childrenŐs diarrhea, malaria, tuberculosis and a number of filarial infections including River Blindness, African sleeping sickness, and Chagas disease. Some of the mechanisms being pursued for these disorders are inhibitors of Hsp90, NEP, and MetAP. Here my major focus as a chemist will to help repurpose advanced clinical agents towards these diseases or carry out focused medicinal chemistry and structure-based drug design approaches based on advanced leads to find compounds that may offer a viable treatment.
Recent Publications
  • Chrencik JE, Patny A, Leung IK, Korniski B, Emmons TL, Hall T, Weinberg RA, Gormley JA, Williams JM, Day E, Hirsch JL, Kiefer JR, Leone JW, Fischer HD, Sommers CD, Huang H-C, Jacobsen EJ, TenBrink RE, Tomasselli AG, Benson TE. Structural and Thermodynamic Characterization of the Tyk2 and JAK3 Kinase Domains in Complex with CP-690550 and CMP6. J Mol Biol 2010, 400:413-433.
  • Tollefson MB, Acker BA, Jacobsen EJ, Hughes RO, Walker JK, Fox DA, Palmer MJ, Freeman SK, Yu Y, Bond BR. 1-(2-(2,2,2-Trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as Potent Phosphodiesterase 5 (PDE5) Inhibitors. Bioorg Med Chem Lett. 2010, 20:3125-3128.
  • Tollefson MB, Acker BA, Jacobsen EJ, Hughes RO, Walker JK, Fox DA, Palmer MJ, Freeman SK, Yu Y, Bond BR. 1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as Potent Phosphodiesterase 5 (PDE5) Inhibitors. Bioorg Med Chem Lett 2010, 20:3120-3124.
  • Hughes RO, Rogier DJ, Jacobsen EJ, Walker JK, MacInnes A, Bond BR, Zhang LL, Yu Y, Zheng Y, Rumsey JM, Walgren JLE, Curtis SW, Fobian YM, Heasley SE, Cubbage JW, Moon JB, Brown L, Acker BA, Maddux TM, Tollefson MB, Mischke BV, Owen DF, Freskos JN, Molyneaux JM, Benson AG, Blevis-Bal RM. Design, Synthesis and Biological Evaluation of 3-[4-(2-Hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a Potent, Orally Active, Brain Penetrant Inhibitor of PDE5. J Med Chem 2010, 53:2656-2660.
  • Hughes RO, Walker JK, Cubbage JW, Fobian YM, Rogier DJ, Heasley SE, Blevis-Bal RM, Benson AG, Owen DR, Jacobsen EJ, Freskos JN, Molyneaux JM, Brown DL, Stallings WC, Acker BA, Maddux TM, Tollefson MB, Williams JM, Moon JB, Mischke BV, Rumsey JM, Zheng Y, MacInnes A, Bond BR, Yu Y. Investigation of Aminopyridiopyrazinones as PDE5 Inhibitors: Evaluation of Modifications to the Central Ring System. Bioorg Med Chem Lett 2009, 19:4092-4096.