Department of Medicinal Chemistry

David J. Augeri

Research Professor
Department of Medicinal Chemistry
Ph.D. 1992, University of California-Irvine
Phone (848) 445-6493;
fax (732) 445-6312

 

Education

B.S. Chemistry, 1986, University of Connecticut, Storrs
Ph.D Synthetic Organic Chemistry, 1992, University of California, Irvine
NIH Postdoctoral Fellow, Princeton University

Positions Held

Pfizer 1986-1987
Abbott Laboratories, Senior Scientist,1995-1999
Bristol-Myers Squibb, Senior Research Investigator, 1999-2002
Lexicon Pharmaceuticals, Director of Medicinal Chemistry, 2002-1012

Research Interests:

I have 23 years of experience performing drug discovery research in the pharmaceutical industry in the areas of oncology, immunology and metabolic diseases. I played a central role in the discovery of saxagliptin (Onglyza) at Bristol-Myers Squibb that was approved by the FDA in 2009 for type II diabetes. Through research conducted at Abbott Labs, I synthesized an acylsulfonamide “linker” that connected two fragments that showed high affinity for the binding site on the bcl-2 protein. This acylsulfonamide remains a central structural element of ABT-737 and ABT-263, bcl-2/bcl/xL inhibitors. ABT-263 is currently in Phase III trials for the treatment of solid tumors. At Lexicon, I served as director of Immunology Medicinal Chemistry and guided the LX2931 and LX2932 programs that are currently in Phase II clinical trials for the treatment of rheumatoid arthritis. I also led several other programs including kinases, lyases, and GPCRs. I returned to academics to take the position of Research Professor and Director of Molecular Design and Synthesis in Rutgers Translational Sciences in 2012. I collaborate with several CINJ investigators in the areas of mutant p53 reactivators, Bmi-1 inhibitors, BMP-2 inhibitors, MTHD2 inhibitors, and several pilot programs. I also collaborate with Mito Biopharma in the area of metabolic diseases. I have a research group of 4 chemists as well as summer interns and honors research students in the school of pharmacy. I have 74 publications, including 36 patents.

 

Recent publications (representative):

Blanden, A.R., Yu, X., Wolfe, A. J., Gilleran, J. A., Augeri, D. J., O'Dell, R. F., Olson, E.C., Kimball, S. D., Emge, T. J., Movileanu, L., Carpizo, D. R., Loh, S.N., “Synthetic metallochaperone ZMC1 rescues mutant p53 by tranporting Zn2+ into cells and buffering intracellular Zn2+ concentration”Molecular Pharmacology, 2015, 97550.

Xin Yu1, Adam R. Blanden, Sumana Narayanan, Lalithapriya Jayakumar, David Lubin, David Augeri, S. David Kimball, Stewart N. Loh,*, and Darren R. Carpizo Small molecule restoration of wildtype structure and function of mutant p53 using a novel zinc- metallochaperone based mechanism, Oncotarget, 2014, 5(19), 8879.

Oravecz, T.; Augeri, D. Anti-Inflammatory Drug Discovery, contributed chapter entitled  “Tipping the Balance of Sphingosine 1-Phosphate Production: Sphingosine Kinases and Sphingosine 1- Lyase as Immune Therapeutic Targets : Edited by Dr. Jeremy Levin, Prof. Stefan Laufer, Royal Chemistry Society, 2012, 10.1039/[ISBN]

Bagdanoff, J. T;  Donoviel, M.S.; Nouraldeen, A.; Carlsen, M; Jessop, T. C.;Tarver, J.; Aleem, S;  Dong, L.; Zhang, H.;Yan, J.; Bednarz, M.; Layek, S.; Hazelwood, J.; Owusu, I. B.; Gopinathan, S.; Moran, L.; Lai, Z.; Boteju, L.; Kramer, J.;  Kimball, S.D.; Yalamanchili, P.; Heydorn, W.E.;  Frazier, K.E.;  Brooks, B.; Brown, P.;  Wilson, A.; Sonnenburg, W. K.; Main, A.; Carson, K.G.; Oravecz, T.; Augeri, David J.*  Inhibition of Sphingosine 1-Phosphate Lyase for the Treatment of Rheumatoid Arthritis: Discovery of (E)-1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone oxime (LX2931) and (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol (LX2932)  Journal of Medicinal Chemistry 2010, 8650-8662.

Augeri, David J.*; Robl, Jeffrey A.; Betebenner, David A. ; Magnin, David R.; Khanna, Ashish; Robertson, James G.; Wang, Aiying; Simpkins, Ligaya M.; Taunk, Prakash; Huang, Qi; Han, Song-Ping ; Abboa-Offei, Benoni; Cap, Michael;  Xin, Li; Tao, Li ; Tozzo, Effie; Welzel, Gustav E.; Egan, Donald M.; Marcinkeviciene, Jovita; Kirby, Mark S.; Biller, Scott; Parker, Rex A.; Hamann, Lawrence G.* Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes  J. Med. Chem. 2005, 48, 5025-5037.

Oltersdorf, Tilman; Elmore, Steven W.; Shoemaker, Alexander R.; Armstrong, Robert C.; Augeri, David J.; Belli, Barbara A.; Bruncko, Milan; Deckwerth, Thomas L.; Dinges, Jurgen; Hajduk, Philip J.; Joseph, Mary K.; Kitada, Shinichi; Korsmeyer, Stanley J.; Kunzer, Aaron R.; Letai, Anthony; Li, Chi; Mitten, Michael J.; Nettesheim, David G.; Ng, Shi Chung; Nimmer, Paul M.; O'Connor, Jacqueline M.; Oleksijew, Anatol; Petros, Andrew M.; Reed, John C.; Shen, Wang; Tahir, Stephen K.; Thompson, Craig B.; Tomaselli, Kevin J.; Wang, Baole; Wendt, Michael D.; Zhang, Haichao; Fesik, Stephen W.; Rosenberg, Saul H.  An inhibitor of Bcl-2 family proteins induces regression of solid tumours.  Nature, 2005, 435 (7042), 677-681.
 
(top)