Work in Dr. Kerns’ lab is directed toward the design and synthesis of new pharmaceutical agents to treat disease. His research group is involved in numerous interdisciplinary translational research programs focused on the design, synthesis, and evaluation of novel bioactive small molecule therapeutics. Ongoing projects include optimizing lead structures as chemical probes to validate new drug targets and as lead compounds for further development as new therapeutics for the treatment of diseases including cancer, heart disease, drug-resistant infections, and diabetes. The Kerns lab is also working to develop new mitochondria-targeted molecular probes and therapeutic agents.

Current Positions

• Professor of Pharmaceutical Sciences and Experimental Therapeutics

Education

• BS in Chemistry, Iowa State University, Ames, Iowa, United States
• PhD in Medicinal & Natural Products Chemistry, University of Iowa, Iowa City, Iowa
• Postdoctoral Fellow in Organic Chemistry and Molecular Recognition, Princeton University, Princeton, New Jersey, United States

Research Interest

• Drug Discovery

Selected Publications

• Carter, H. E., Wildman, B., Schwanz, H. A., Kerns, R. J. & Aldred, K. J. (2023). Role of the Water-Metal Ion Bridge in Quinolone Interactions with Escherichia coli Gyrase. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES 24 (3). DOI: 10.3390/ijms24032879.
• Gruenwald, H. K. & Kerns, R. J. (2022). Stability of Phenyl-Modified Triphenylphosphonium Conjugates and Interactions with DTPA. ACS OMEGA 7 (51) 48332-48339. DOI: 10.1021/acsomega.2c06525.
• Chheda, P. R., Nieto, N., Kaur, S., Beck, J. M., Beck, J. R., Honzatko, R., Kerns, R. J. & Nelson, S. W. (2022). Promising antimalarials targeting apicoplast DNA polymerase from Plasmodium falciparum. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 243. DOI: 10.1016/j.ejmech.2022.114751.
• Fosdick, M. G., Chheda, P. R., Tran, P. M., Wolff, A., Peralta, R., Zhang, M. Y., Kerns, R. & Houtman, Jon C. D. (2021). Suppression of human T cell activation by derivatives of glycerol monolaurate. SCIENTIFIC REPORTS 11 (1). DOI: 10.1038/s41598-021-88584-y.
• Fink, B. D., Yu, L., Coppey, L., Obrosov, A., Shevalye, H., Kerns, R. J., Yorek, M. A. & Sivitz, William, I (2021). Effect of mitoquinone on liver metabolism and steatosis in obese and diabetic rats. Pharmacology research & perspectives 9 (1) e00701. DOI: 10.1002/prp2.701. PMID: 33547885. PMCID: PMC7866483.
• Kulkarni, C. A., Fink, B. D., Gibbs, B. E., Chheda, P. R., Wu, M., Sivitz, William, I & Kerns, R. J. (2021). A Novel Triphenylphosphonium Carrier to Target Mitochondria without Uncoupling Oxidative Phosphorylation. Journal of medicinal chemistry 64 (1) 662-676. DOI: 10.1021/acs.jmedchem.0c01671. PMID: 33395531.
• Aguirre, A. L., Chheda, P. R., Lentz SRC, Held, H. A., Groves, N. P., Hiasa, H. & Kerns, R. J. (2020). Identification of an ethyl 5,6-dihydropyrazolo[1,5-c]quinazoline-1-carboxylate as a catalytic inhibitor of DNA gyrase. Bioorganic & medicinal chemistry 28 (10) 115439. DOI: 10.1016/j.bmc.2020.115439. PMID: 32234278. PMCID: PMC7331940.
• Delgado, J. L., Lentz SRC, Kulkarni, C. A., Chheda, P. R., Held, H. A., Hiasa, H. & Kerns, R. J. (2019). Probing structural requirements for human topoisomerase I inhibition by a novel N1-Biphenyl fluoroquinolone. European journal of medicinal chemistry 172 109-130. DOI: 10.1016/j.ejmech.2019.03.040. PMID: 30959322. PMCID: PMC6499389.
• Lentz SRC, Chheda, P. R., Oppegard, L. M., Towle, T. R., Kerns, R. J. & Hiasa, H. (2019). The C7-aminomethylpyrrolidine group rescues the activity of a thio-fluoroquinolone. Biochimie 160 24-27. DOI: 10.1016/j.biochi.2019.02.002. PMID: 30763638. PMCID: PMC6462232.
• Oppegard, L. M., Delgado, J. L., Kulkarni, C. A., Towle, T. R., Hart, D. E., Williams, B. P., Lentz SRC, Norris, B. J., Flory, C. M., Schumacher, R. J., Murry, D. J., Kerns, R. J. & Hiasa, H. (2019). Novel N-1 substituted fluoroquinolones inhibit human topoisomerase I activity and exhibit anti-proliferative activity. Investigational new drugs 37 (2) 378-383. DOI: 10.1007/s10637-018-0666-x. PMID: 30198058. PMCID: PMC6409185.
• Towle, T. R., Kulkarni, C. A., Oppegard, L. M., Williams, B. P., Picha, T. A., Hiasa, H. & Kerns, R. J. (2018). Design, synthesis, and evaluation of novel N-1 fluoroquinolone derivatives: Probing for binding contact with the active site tyrosine of gyrase. Bioorganic & medicinal chemistry letters 28 (10) 1903-1910. DOI: 10.1016/j.bmcl.2018.03.085. PMID: 29661533. PMCID: PMC5938125.
• Imai, Y., Fink, B. D., Promes, J. A., Kulkarni, C. A., Kerns, R. J. & Sivitz, W. I. (2018). Effect of a mitochondrial-targeted coenzyme Q analog on pancreatic β-cell function and energetics in high fat fed obese mice. Pharmacology research & perspectives 6 (3) e00393. DOI: 10.1002/prp2.393. PMID: 29864244. PMCID: PMC5980123.
• Ashley, R. E., Lindsey, Jr, R. H., McPherson, S. A., Turnbough, Jr, C. L., Kerns, R. J. & Osheroff, N. (2017). Interactions between Quinolones and Bacillus anthracis Gyrase and the Basis of Drug Resistance. Biochemistry 56 (32) 4191-4200. DOI: 10.1021/acs.biochem.7b00203. PMID: 28708938. PMCID: PMC5560241.
• Fink, B. D., Guo, D. F., Kulkarni, C. A., Rahmouni, K., Kerns, R. J. & Sivitz, W. I. (2017). Metabolic effects of a mitochondrial-targeted coenzyme Q analog in high fat fed obese mice. Pharmacology research & perspectives 5 (2) e00301. DOI: 10.1002/prp2.301. PMID: 28357127. PMCID: PMC5368965.
• Malik, M., Mustaev, A., Schwanz, H. A., Luan, G., Shah, N., Oppegard, L. M., de Souza, E. C., Hiasa, H., Zhao, X., Kerns, R. J. & Drlica, K. (2016). Suppression of gyrase-mediated resistance by C7 aryl fluoroquinolones. Nucleic acids research 44 (7) 3304-16. DOI: 10.1093/nar/gkw161. PMID: 26984528. PMCID: PMC4838383.