Eli Chapman, PhD

Associate Professor, Pharmacology and Toxicology

The Chapman lab is a chemical biology lab. They are primarily focused on finding synthetic small molecules or natural probes and leads through targeted approaches, on understanding the mechanisms and modes of action of these molecules, and on improving the molecules through medicinal chemistry. We use contemporary molecular biology and protein biochemistry procedures to produce the desired target proteins and then develop assays amenable to moderate to high throughput screening. Through development, we use cellular amenable to understand the modes of action, biophysics to understand the mechanisms of action, structural biology to guide molecular improvements, and synthetic chemistry to optimize hit compounds. We often simultaneously probe families of enzymes in a parallel fashion in an effort to pre-program specificity, mitigating downstream off-target liabilities and aiding development. Currently, we have several programs in the lab including antibiotics targeting bacterial HSP60 (GroEL); anti-cancer targeting specific HSP70s, elF4A, and NRF2; and anti-type 2 diabetes targeting PTP1B. 

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Education & Post Graduate Training: 

BS, Chemistry, University of California at Berkeley, 1996
MA, Chemistry, Columbia University (New York), 1998
PhD, Chemistry, Scripps Research Institute (California), 2003

Select Publications

2017

Tillotson, J., M. Kedzior, L. Guimarães, A. B. Ross, T. L. Peters, A. J. Ambrose, C. J. Schmidlin, D. D. Zhang, L. V. Costa-Lotufo, A. D. Rodríguez, et al., "ATP-competitive, marine derived natural products that target the DEAD box helicase, eIF4A.", Bioorg Med Chem Lett, vol. 27, issue 17, pp. 4082-4085, 2017 09 01. PMCID: PMC5593424  PMID: 28757063
Tillotson, J., C. J. Zerio, B. Harder, A. J. Ambrose, K. S. Jung, MJ. Kang, D. D. Zhang, and E. Chapman, "Arsenic Compromises Both p97 and Proteasome Functions.", Chem Res Toxicol, vol. 30, issue 7, pp. 1508-1514, 2017 Jul 17. PMCID: PMC5687067  PMID: 28636814
Tao, S., P. Liu, G. Luo, M. Rojo de la Vega, H. Chen, T. Wu, J. Tillotson, E. Chapman, and D. D. Zhang, "p97 Negatively Regulates NRF2 by Extracting Ubiquitylated NRF2 from the KEAP1-CUL3 E3 Complex.", Mol Cell Biol, vol. 37, issue 8, 2017 Apr 15. PMCID: PMC5376629  PMID: 28115426
Ambrose, A. J., E. A. Santos, P. C. Jimenez, D. D. Rocha, D. V. Wilke, P. Beuzer, J. Axelrod, A. Kumar Kanduluru, P. L. Fuchs, H. Cang, et al., "Ritterostatin GN 1N , a Cephalostatin-Ritterazine Bis-steroidal Pyrazine Hybrid, Selectively Targets GRP78.", Chembiochem, vol. 18, issue 6, pp. 506-510, 2017 Mar 16. PMCID: PMC5562448  PMID: 28074539

2016

Tillotson, J., B. P. Bashyal, MJ. Kang, T. Shi, F. De La Cruz, A. A. Leslie Gunatilaka, and E. Chapman, "Selective inhibition of p97 by chlorinated analogues of dehydrocurvularin.", Org Biomol Chem, vol. 14, issue 25, pp. 5918-21, 2016 Jul 07. PMCID: PMC5466822  PMID: 27223265