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David J. Augeri, PhD

Selected Publications

(14 out of a total of 63)

  1. 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, submitted  to Cancer Cell, April 2014.
  2. Salojin Konstantin V; Hamman Brian D; Chang Wei Chun; Jhaver Kanchan G; Al-Shami Amin; Crisostomo Jeannette; Wilkins Carrie; Digeorge-Foushee Ann Marie; Allen Jason; Patel Nita; Gopinathan Suma; Zhou Julia; Nouraldeen Amr; Jessop Theodore C; Bagdanoff Jeffrey T; Augeri David J; Read Robert; Vogel Peter; Swaffield Jonathan; Wilson Alan; Platt Kenneth A; Carson Kenneth G; Main Alan; Zambrowicz Brian P; Oravecz Tamas, Genetic Deletion of Mst1 Alters T Cell Function and Protects against Autoimmunity PLoS ONE, 2014, 9(5), 98151.
  3. 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]
  4. 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.
  5. Bagdanoff, Jeffrey T.; Donoviel, Michael S.; Nouraldeen, Amr; Tarver, James; Fu, Qinghong; Carlsen, Marianne; Jessop, Tad; Zhang, Haiming; Hazelwood, Jill; Nguyen, Huy; Baugh, Simon D. P.; Gardyan, Michael; Terranova, Kristen M.; Barbosa, Joseph; Yan, Jack; Bednarz, Mark; Layek, Suman; Taylor, Jerry; Digeorge-Foushee, Ann Marie; Gopinathan, Suma; Bruce, Debra; Smith, Traci; Moran, Liam; O'Neill, Emily; Kramer, Jeff; Lai, Zhong; Kimball, S. David; Liu, Qingyun; Sun, Weimei; Yu, Sean; Swaffield, Jonathan; Wilson, Alan; Main, Alan; Carson, Kenneth G.; Oravecz, Tamas; Augeri, David J. * Inhibition of sphingosine-1-phosphate lyase for the treatment of autoimmune disorders.    Journal of Medicinal Chemistry 2009, 52(13), 3941-3953.
  6. Simpkins, Ligaya M.; Bolton, Scott; Pi, Zulan; Sutton, James C.; Kwon, Chet; Zhao, Guohua; Magnin, David R.; Augeri, David J.; Gungor, Timur; Rotella, David P.; Sun, Zhong; Liu, Yajun; Slusarchyk, William S.; Marcinkeviciene, Jovita; Robertson, James G.; Wang, Aiying; Robl, Jeffrey A.; Atwal, Karnail S.; Zahler, Robert L.; Parker, Rex A.; Kirby, Mark S.; Hamann, Lawrence G.   Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.    Bioorganic & Medicinal Chemistry Letters  200717(23),  6476-6480.
  7. Petros, Andrew M.; Dinges, Jurgen; Augeri, David J.; Baumeister, Steven A.; Betebenner, David A.; Bures, Mark G.; Elmore, Steven W.; Hajduk, Philip J.; Joseph, Mary K.; Landis, Shelley K.; Nettesheim, David G.; Rosenberg, Saul H.; Wang, Shen; Thomas, Sheela; Wang, Xilu; Zanze, Irini; Zhang, Haichao; Fesik, Stephen W.  Discovery of a Potent Inhibitor of the Antiapoptotic Protein Bcl-xL from NMR and Parallel Synthesis.    J. Med. Chem, 2006, 49(2), 656-663.
  8. 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.
  9. 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.
  10. Hajduk, Philip J.; Augeri, David J.; Mack, Jamey; Mendoza, Renaldo; Yang, Jianguo; Betz, Stephen F.; Fesik, Stephen W.  NMR-Based Screening of Proteins Containing 13C-Labeled Methyl Groups.    J. Am. Chem. Soc. 2000122, 7898-7904.
  11. Augeri, David J*.; O'Connor, Stephen J.*; Janowick, Dave; Szczepankiewicz, Bruce; Sullivan, Gerry; Larsen, John; Kalvin, Douglas; Cohen, Jerry; Devine, Edward; Zhang, Haichao; Cherian, Sajeev; Saeed, Badr; Ng, Shi-Chung; Rosenberg, Saul.  Potent and Selective Non-Cysteine-Containing Inhibitors of Protein Farnesyltransferase.    J. Med. Chem.  1998, 41, 4288-4300.
  12. Kim, Soong Hoon; Augeri, David; Yang, Dan; Kahne, Daniel.  Concise Synthesis of the Calicheamicin Oligosaccharide Using the Sulfoxide Glycosylation Method    J. Am. Chem. Soc. 1994, 116, 1766-75.
  13. Newhouse, Bradley J.; Bordner, Jon; Augeri, David J.; Litts, Christopher S.; Kleinman, Edward F.  Novel [3+2] and [3+3] 4-Quinolone Annulations by a Tandem Claisen-Cope Amidoalkylation Reaction J. Org. Chem. 199257, 6991-5.
  14. Augeri, David J.; Fray, Andrew H.; Kleinman, Edward F.  Synthesis and Antibacterial Activity of 2,3-Dehydroofloxacin.   J. Heterocycl. Chem. 1990, 27, 1509.

Issued Patents

Augeri, David John; Bagdanoff, Jeffrey Thomas; Baugh, Simon David Peter; Carlsen, Marianne; Carson, Kenneth Gordon; Gilleran, John Anthony; He, Wei; Oravecz, Tamas; Salojin, Konstantin; Sung, Leonard.  Preparation of benzenesulfonamides as Mst-1 inhibitors U.S. Pat. Appl. Publ. (2012), US 20120225857 

Augeri, David J.; Bagdanoff, Jeffrey; Baugh, Simon D. P.; Carson, Kenneth G.; Jessop, Theodore C.; Tarver, James E.   Preparation of azolylimidazolylbutanetetraols as sphingosine-1-phosphate (S1P) modulators for treatment of autoimmune and inflammatory disorders U.S. Pat. 7,598,280

Augeri, David J.; Steven A. Baumeister, Milan Brunko, Daniel A. Dickman, Hong Ding, Jurgen Dinges, Stephen W. Fesik, Philip J. Hajduk, Aaron R. Kunzer, David G. Nettesheim, Thorsten Oost, Andrew Petros, Saul H. Rosenberg, Wang Shen, Sheela A. Thomas, Xilu Wang, Michael D. Wendt. N-acylsulfonamide Apoptosis Promoters, 7,504,512

Vu, Truc Chi; Brzozowski, David B.; Fox, Rita; Godfrey, Jollie Duaine, Jr.; Hanson, Ronald L.; Kolotuchin, Sergei V.; Mazzullo, John A., Jr.; Patel, Ramesh N.; Wang, Jianji; Wong, Kwok; Yu, Jurong; Zhu, Jason; Magnin, David R.; Augeri, David J.; Hamann, Lawrence G. Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates US 7,420,079

Augeri, David J.; Baumeister, Steven A.; Bruncko, Milan; Dickman, Daniel A.; Ding, Hong; Dinges, Jurgen; Fesik, Stephen W.; Hajduk, Philip J.; Kunzer, Aaron R.; McClellan, William; Nettesheim, David G.; Oost, Thorsten; Petros, Andrew M.; Rosenberg, Saul H.; Wang, Shen; Thomas, Sheela A.; Wang, Xilu; Wendt, Michael D.  N- Preparation of N-Arylcarbonyl- and Heteroarylcarbonyl Benzenesulfonamide Inhibitors of Bcl-Xl and Bcl-2 as Promoters of Apoptosis  United States Patent  6,720,338

David J. Augeri,  Steven A. Baumeister,  Daniel A. Dickman, Hong Ding, Jurgen Dinges, Stephen W. Fesik , Philip J. Hajduk,  William McClellan,  David G. Nettesheim,   Thorsten Oost, Andrew M. Petros,   Saul H. Rosenberg, Wang Shen,  Sheela A. Thomas, Xilu Wang,  Michael D. Wendt  N-acylsulfonamide apoptosis promoters; U.S. 6,720,338

Robl, Jeffrey A.; Sulsky, Richard B.; Augeri, David J.; Magnin, David R.; Hamann, Lawrence G. Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV    United States Patent  6,395,767

Sebti, Said M.; Hamilton, Andrew D.; Augeri, David J.; Barr, Kenneth J.; Fakhoury, Stephen A.; Janowick, David A.; Kalvin, Douglas M.; O'connor, Stephen J.; Rosenberg, Saul H.; Shen, Wang; Swenson, Rolf E.; Sorenson, Bryan K.; Sullivan, Gerard M.; Tasker, Andrew S.; Wasicak, James T.; Nelson, Lissa T. J.; Henry, Kenneth J.; Wang, Le.  Preparation of methionine derivatives as inhibitors of protein isoprenyl transferases. United States Patent  6,310,095

Augeri, David J.; Betebenner, David A.; Craig, Richard; Davidsen, Steven K.; Fesik, Stephen W.; Giesler-Stacey, Jamie R.; Guo, Yan; Hajduk, Philip J.; Michaelides, Michael R.; Nettesheim, David G.  Preparation of Naphthalenehydroxamic acids as Matrix Metalloproteinase Inhibitors. United States Patent  6,288,261 

Sebti, Said M.; Hamilton, Andrew D.; Augeri, David J.; Barr, Kenneth J.; Fakhoury, Stephen A.; Janowick, David A.; Kalvin, Douglas M.; O'Connor, Stephen J.; Rosenberg, Saul H.; Shen, Wang; Swenson, Rolf E.; Sorensen, Bryan K.; Sullivan, Gerard M.; Tasker, Andrew S.; Wasicak, James T.; Nelson, Lissa T. J.; Henry, Kenneth J.; Wang, Le; Liu, Gang; Gunawardana, Indrani W.  Inhibitors of protein isoprenyl transferases. United States Patent  6,204,293

Sebti, Said M.; Hamilton, Andrew D.; Augeri, David J.; Barr, Kenneth J.; Fakhoury, Stephen A.; Janowick, David A.; Kalvin, Douglas M.; O'Connor, Stephen J.; Rosenberg, Saul H.; Shen, Wang; Swenson, Rolf E.; Sorensen, Bryan K.; Sullivan, Gerard M.; Tasker, Andrew S.; Wasicak, James T.; Nelson, Lissa T. J.; Henry, Kenneth J.; Wang, Le; Inhibitors of protein isoprenyl transferases. United States Patent  6,310,095

Arendsen , D. L.; Augeri, D. J.; Baker, W. R.; Fakhhoury, S. A.; Fung, A. R.; Garvey, D. S.; McClellan, W. J.; O’Connor, S. J.; Prasad, R. N.; Rockway, T. W.; Rosenberg, S. H.; Stein, H.; Shen, W.; Stout, D. M.; Sullivan, G. M. Inhibitors of Squalene Synthase and Protein Farnesyltransferase.  United States Patent 5, 831,115.

Fesik, Stephen W.; Augeri, David J. Site-Specific 13C/14C-Labeled Proteins, Amino Acids, and Biochemical Precursors US 6,897,337

Sebti, Said M.; Hamilton, Andrew D.; Augeri, David J.; Barr, Kenneth J.; Donner, Bernard G.; Fakhoury, Stephen A.; Janowick, David A.; Kalvin, Douglas M.; Larsen, John J.; Liu, Gang; O'Connor, Stephen J.; Rosenberg, Saul H.; Shen, Wang; Swenson, Rolf E.; Sorensen, Bryan K.; Sullivan, Gerard M.; Szczepankiewicz, Bruce G.; et al.  Inhibitors of Protein Isoprenyl Transferases. US 6,693,123

Sebti, Said M.; Hamilton, Andrew D.; Rosenberg, Saul H.; Augeri, David J.; Barr, Kenneth J.; Donner, Bernard G.; Janowick, David A.; Kalvin, Douglas M.; Larsen, John J.; Liu, Gang; O'Connor, Stephen J.; Shen, Wang; Swenson, Rolf E.; Sorenson, Bryan K.; Sullivan, Gerard M.; Szczepankiewicz, Bruce; Tasker, Andrew S.; Wasicak, James T.; Winn, Martin.  Inhibitors of Protein Isoprenyl Transferases. 1997, US 6,694,104

Invited Lectures, Presentations and Abstracts

The Discovery of Saxagliptin (Onglyza), Bayer Healthcare Science Symposium; Berlin, Germany, 2014, January 24-26.

Inhibition of sphingosine-1-phosphate lyase for the treatment of autoimmune disorders. First Disclosure of LX2931 and LX2932.  Augeri, David J.  Invited Lecture, First Disclosures Forum, 239th ACS National Meeting, San Francisco, CA, United States, 2010, March 21-25, MEDI-36.;

The Discovery of Saxagliptin. Augeri, David J.  Invited Lecture, Burger Award Symposium, ACS MARM, Hershey, Pennsylvania, 2006, June 4-6.