Jon Jacobsen, Ph.D.
Director of Chemistry
Center for World Health and Medicine
Research on neglected diseases and diseases of poverty, including childrenŐs diarrhea, malaria, tuberculosis and a number of filarial infections such as River Blindness, African sleeping sickness, and Chagas disease.
Office: DRC, Room 317
Voice: (314) 977-5139
Ph.D., University of California, Irvine
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.
- 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.
Peter Ruminski, M.S.
Center for World Health and Medicine
Translate basic research discoveries and developed leads into viable drug candidates for neglected diseases of the poor, orphan diseases and other unmet medical needs.
Office: DRC, Room 313
Voice: (314) 977-5126
M.S., Washington University in St. Louis
Current goal is to lead the Center's talented and highly skilled pharmaceutical scientists to translate basic research discoveries and developed leads into viable drug candidates for neglected diseases of the poor, orphan diseases and other unmet medical needs. Some of these current targets include anti-secretory agents for the treatment of childhood diarrhea, malaria and other parasitic diseases, sickle cell disease, pulmonary fibrosis, retinopathies and TB.
- Nagarajan SR, Devadas B, Malecha JW, Lu HF, Ruminski PG, Rico JG, Rogers TE, Marrufo LD, Collins JT, Kleine HP, Lantz MK, Zhu J, Green NF, Russell MA, Landis BG, Miller LM, Meyer DM, Duffin TD, Engleman VW, Finn MB, Freeman SK, Griggs DW, Williams ML, Nickols MA, Pegg JA, Shannon KE, Steininger C, Westlin MM, Nickols GA, Keene JL. R-isomers of Arg-Gly-Asp (RGD) mimics as potent avb3 inhibitors. Bioorg Med Chem 2007, 15:3783-3800.
- Shannon KE, Keene JL, Settle SL, Duffin TD, Nickols MA, Westlin M, Schroeter S, Ruminski PG, Griggs DW. Anti-metastatic properties of RGD-peptidomimetic agents S137 and S247. Clin Exp Metastasis 2004, 21:129-138.
- Hippenmeyer PJ, Ruminski PG, Rico JG, Lu HS, Griggs DW. Adenovirus inhibition by peptidomimetic integrin antagonists. Antiviral Res 2002, 55:169-178.
- Carron CP, Meyer DM, Engleman VW, Rico JG, Ruminski PG, Ornberg RL, Westlin WF, Nickols GA. Peptidomimetic antagonists of avb3inhibit bone resorption by inhibiting osteoclast bone resorptive activity, not osteoclast adhesion to b one. J Endocrinol 2000, 165:587-598.
- Carron CP, Meyer DM, Pegg JA, Engleman VW, Nickols MA, Settle SL, Westlin WF, Ruminski PG, Nickols GA. A peptidomimetic antagonist of the integrin avb3 inhibits Leydig cell tumor growth and the development of hypercalcemia of malignancy. Cancer Res 1998, 58:1930-1935.
- Wong NC, Mueller BM, Barbas CF, Ruminski PG, Quaranta V, Lin EC, Smith JW. av Integrins mediate adhesion and migration of breast carcinoma cell lines. Clin Exp Metastasis 1998, 16:50-61.
- Engleman VW, Nickols GA, Ross FP, Horton MA, DGriggs DW, Settle SL, Ruminski PG, Teitelbaum SL. A peptidomimetic antagonist of the avb3 integrin inhibits bone resorption in vitro and prevents osteoporosis in vivo. J Clin Invest 1997, 99:2284-2292.