Jon E. Hawkinson, PhD

Associate Program Director, Institute for Therapeutics Discovery and Development (ITDD)

Jon E. Hawkinson

Contact Info

hawkinso@umn.edu

Office Phone 612-626-6326

Fax 612-626-6318

Office Address:
717 Delaware Bldg, Rm 519E

Mailing Address:
University of Minnesota
Institute for Therapeutics Discovery & Development (ITDD)
717 Delaware Street SE
Room 519E
Minneapolis, MN 55414

Associate Program Director, Institute for Therapeutics Discovery and Development (ITDD)

Research Professor, Department of Medicinal Chemistry

Research Professor


Fellowship, University of California (Neurotoxicology)

PhD, University of California (Pharmacology and Toxicology)

BS, University of California (Nutritional Sciences)

Graduate Program, University of California (Physiology and Anatomy)

Summary

I have over 15 years of experience leading in vitro pharmacology groups in drug discovery research. I led assay development, high throughput screening, structure-activity relationship, molecular pharmacology, and phenotypic screening teams at two neuroscience-focused biopharmaceutical companies, CoCensys and Elan Pharmaceuticals. At Elan, my HTS team identified eight Hit series entering medicinal chemistry lead optimization, including three series leading to Development Candidates for Alzheimer’s disease and pain. I have extensive knowledge of several therapeutic areas, particularly pain, neurodegeneration, neuropsychiatric disorders, and autoimmune disease. In the field of pain, I led a multidisciplinary discovery team that identified the bradykinin B1 receptor antagonist Development Candidate ELN441958. In addition, I co-invented the anti-nerve growth factor (NGF) therapeutic monoclonal antibody Development Candidate MEDI-585, which entered Phase 1 clinical trials sponsored by AstraZeneca. I also made seminal contributions to the discovery of the g-secretase development candidate ELN475516 for Alzheimer’s Disease, as well as four GABAA receptor modulator development candidates for anxiety, insomnia, and epilepsy. At Elan, I led drug discovery collaborations with Cambridge Antibody Technology and Ingenium Pharmaceuticals. As a drug discovery consultant, I have advised disease-focused non-profits, research institutes, and biopharmaceutical companies on HTS, pharmacology and research strategy.

Research

Research Summary/Interests

  •  High Thoughput screening
  •  Fragment-Based Screening
  •  Assay development
  •  Neuroscience
  •  Pharmacology
  •  Hit to Lead

Publications

PubMed

E. Amin, E Kurbanov, T.-L. Chiu, J. Solberg, S. Francis, K. Maize, Kimberly, J. Fernandez, R. Johnson, J. Hawkinson, M. Walters, B. Finzel. Probing the S2? Subsite of the Anthrax Toxin Lethal Factor Using Novel N-Alkylated Hydroxamates and Highly Predictive 3D-QSAR Models. J. Med. Chem. 58:8723-33, 2015.

S.S. Syeda, E.J. Carlson, M.R. Miller, R. Francis, D.E. Clapham, P.V. Lishko, J.E. Hawkinson, D. Hook, and G.I. Georg. The Fungal Sexual Pheromone Sirenin Activates the Human CatSper Channel Complex. ACS Chem. Biol. 2015 Dec. 16 (Epub ahead of print).

J. Shetty, R. Sinville, I.A. Shumilin, W Minor, J. Zhang, J.E. Hawkinson, G.I. Georg, C.J. Flickinger, J.C. Herr. Recombinant Production of Enzymatically Active Male Contraceptive Drug Target hTSSK2: Localization of the TSKS Domain Phosphorylated by TSSK2. Protein Expr. Purif. 121:88-96, 2016.

Y. Zhang, D. Tian, H. Matsuyama, T. Hamazaki, T. Shiratsuchi, N. Terada, D.J. Hook, M.A. Walters, G.I. Georg, and J.E. Hawkinson. Human Adenine Nucleotide Translocase (ANT) Modulators Identified by High Throughput Screening of Transgenic Yeast. J. Biomol. Screen. 2016 Jan. 8 (Epub ahead of print).

J.E. Hawkinson, A.J. Ross, S. Parthasarathy, D.J. Scott, E.A. Laramee, L.J. Posecion, W.R. Rekshan, K.E. Sheau, N.D. Njaka, P. J. Bayley, and R.C. deCharms. Quantification of the Adverse Events Associated with Functional MRI and with Real-Time MRI-Based Training. Int J. Behav. Med. 19(3):372, 2012."

J.E. Hawkinson, B.G. Szoke, A.W. Garofalo, D.S. Hom, H. Zhang, M. Dreyer, J.Y. Fukuda, L. Chen, B. Samant, S. Simmonds, K.P. Zeitz, A. Wadsworth, A. Liao, R.A. Chavez, W. Zmolek, L. Ruslim, M.P. Bova, R. Holcomb, E.R. Butelman, M.-C. Ko, and A.B. Malmberg. Pharmacological, Pharmacokinetic, and Primate Analgesic Efficacy Profile of the Novel Bradykinin B1 Receptor Antagonist ELN441958. J. Pharmacol. Exp. Ther. 322:619-630, 2007.

J.E. Hawkinson, M. Acosta-Burruel, and S.A. Espitia. Opioid activity profiles indicate similarities between the nociceptin/orphanin FQ and opioid receptors. Eur. J. Pharmacol. 389:107-114, 2000.

J.E. Hawkinson, M. Acosta-Burruel, K.C. Yang, D.J. Hogenkamp, J.-S. Chen, N.C. Lan, J.A. Drewe, E.R. Whittemore, R.M. Woodward, R.B. Carter, and R.B. Upasani. Substituted 3-phenylethynyl derivatives of 3-hydroxy-5-pregnan-20-one: Remarkably potent neuroactive steroid modulators of g-aminobutyric acidA receptors. J. Pharm. Exp. Ther. 287: 198 – 207, 1998.
J.E. Hawkinson and S.A. Espitia. Effects of thiocyanate and AMPA receptor ligands on (S)-5-fluorowillardiine, (S)-AMPA and (R,S)-AMPA binding. Eur. J. Pharmacol. 329: 213 – 221, 1997.

J.E. Hawkinson, M. Acosta-Burruel, N.D. Ta, and P.L. Wood. Novel phosphoserine phosphatase inhibitors. Eur. J. Pharmacol. 337: 315 – 324, 1997.

J.E. Hawkinson, K.R. Huber, P.S. Sahota, H.H. Hsu, E. Weber, and M.J. Whitehouse. The N-methyl-D-aspartate (NMDA) receptor glycine site antagonist ACEA 1021 does not produce pathological changes in rat brain. Brain Res. 744: 227 – 234, 1997.

J.E. Hawkinson, M. Acosta-Burruel, and P.L. Wood. The metabotropic glutamate receptor antagonist L-2-amino-3-phoshonopropionic acid inhibits phosphoserine phosphatase. Eur. J. Pharmacol. 307: 219 – 225, 1996.
J.E. Hawkinson, M. Acosta-Burruel, C.L. Kimbrough, D.B. Goodnough, and P.L. Wood. Steroid inhibition of [3H]SR 95531 binding to the GABAA recognition site. Eur. J. Pharmacol. 304: 141 – 146, 1996.

J.E. Hawkinson, J.A. Drewe, C.L. Kimbrough, J.-S. Chen, D.J. Hogenkamp, N.C. Lan, K.W. Gee, K.-Z. Shen, E.R. Whittemore, and R.M. Woodward. 3-Hydroxy-3-trifluoromethyl-5-pregnan-20-one (Co 2-1970): A partial agonist at the neuroactive steroid site of the g-aminobutyric acidA receptor. Molec. Pharmacol. 49: 897 – 906, 1996.

J.E. Hawkinson, C.L. Kimbrough, L.D. McCauley, M.B. Bolger, N.C. Lan, and K.W. Gee. The neuroactive steroid 3-hydroxy-5-pregnan-20-one is a two-component modulator of ligand binding to the GABAA receptor. Eur. J. Pharmacol. Molec. Pharmacol. Sect. 17: 157 – 163, 1994.

J.E. Hawkinson, C.L. Kimbrough, D. Belelli, J.J. Lambert, R.H. Purdy, and N.C. Lan. Correlation of neuroactive steroid modulation of [35S]t-butylbicyclophosphorothionate and [3H]flunitrazepam binding and ? -aminobutyric acidA receptor function. Molec. Pharmacol. 46: 977 – 985, 1994.

J.E. Hawkinson and J.E. Casida. Binding kinetics of ?-aminobutyric acidA receptor noncompetitive antagonists: Trioxabicyclooctane, dithiane, and cyclodiene insecticide-induced slow transition to blocked chloride channel conformation. Molec. Pharmacol. 42: 1069 – 1076, 1993.

J.E. Hawkinson, M.P. Goeldner, C.J. Palmer, and J.E. Casida. Photoaffinity ligands for the [3H]TBOB binding site of the GABAA receptor. J. Receptor Res. 11: 391-405, 1991.

J.E. Hawkinson, L.R. Shull, and R.M. Joy. Effects of lindane on calcium fluxes in synaptosomes. Neurotoxicology 10: 29 – 40, 1989.