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David J. Augeri
Researcher at Lexicon Pharmaceuticals
Publications - 68
Citations - 5589
David J. Augeri is an academic researcher from Lexicon Pharmaceuticals. The author has contributed to research in topics: Dipeptidyl peptidase & Farnesyltransferase. The author has an hindex of 19, co-authored 68 publications receiving 5354 citations. Previous affiliations of David J. Augeri include University of Pittsburgh & Bristol-Myers Squibb.
Papers
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Journal ArticleDOI
An inhibitor of Bcl-2 family proteins induces regression of solid tumours
Tilman Oltersdorf,Steven W. Elmore,Alexander R. Shoemaker,Robert C. Armstrong,David J. Augeri,Barbara A. Belli,Milan Bruncko,Thomas L. Deckwerth,Jürgen Dinges,Philip J. Hajduk,Mary K. Joseph,Shinichi Kitada,Stanley J. Korsmeyer,Stanley J. Korsmeyer,Kunzer Aaron R,Anthony Letai,Chi Li,Michael J. Mitten,David G. Nettesheim,Shi Chung Ng,Paul Nimmer,Jacqueline M. O'Connor,Anatol Oleksijew,Andrew M. Petros,John C. Reed,Wang Shen,Stephen K. Tahir,Craig B. Thompson,Kevin J. Tomaselli,Baole Wang,Wendt Michael D,Haichao Zhang,Stephen W. Fesik,Saul H. Rosenberg +33 more
TL;DR: Mechanistic studies reveal that ABT-737 does not directly initiate the apoptotic process, but enhances the effects of death signals, displaying synergistic cytotoxicity with chemotherapeutics and radiation.
Journal ArticleDOI
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
David J. Augeri,Jeffrey A. Robl,David A. Betebenner,David R. Magnin,Ashish Khanna,James G. Robertson,Aiying Wang,Ligaya M. Simpkins,Prakash Taunk,Qi Huang,Songping Han,B.E. Abboa-Offei,Michael Cap,Li Xin,Li Tao,Effie Tozzo,Gustav E Welzel,Donald Egan,Jovita Marcinkeviciene,Shu Y Chang,Scott A. Biller,Mark S. Kirby,Rex A. Parker,Lawrence G. Hamann +23 more
TL;DR: Extension of this approach to adamantylglycine-derived inhibitors led to the discovery of highly potent inhibitors, including hydroxyadamantyl compound BMS-477118 (saxagliptin), a highly efficacious, stable, and long-acting DPP-IV inhibitor, which is currently undergoing clinical trials for treatment of type 2 diabetes.
Journal ArticleDOI
Discovery of a Potent Inhibitor of the Antiapoptotic Protein Bcl-xL from NMR and Parallel Synthesis
Andrew M. Petros,Jürgen Dinges,David J. Augeri,Steven A. Baumeister,David A. Betebenner,Mark G. Bures,Steven W. Elmore,Philip J. Hajduk,Mary K. Joseph,Shelley K. Landis,David G. Nettesheim,Saul H. Rosenberg,Wang Shen,Sheela A. Thomas,Wang Xilu,Irini Zanze,Haichao Zhang,Stephen W. Fesik +17 more
TL;DR: From NMR-based structural studies and parallel synthesis, a potent ligand was obtained, which binds to Bcl-x(L) with an inhibition constant (K(i)) of 36 +/- 2 nM, which represents the binding site for BH3 peptides from proapoptotic B cl-2 family members such as Bak and Bad.
Patent
Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
Jeffrey A. Robl,Sulsky Richard B,David J. Augeri,David R. Magnin,Lawrence G. Hamann,David A. Betebenner +5 more
TL;DR: In this paper, a method for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out in this paper, employing a DP 4 inhibitor or a combination of such DP 4 inhibitors and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitaxone, rosiglitaze, and/or insulin, and one of a hypolipidemic agent.
Journal ArticleDOI
NMR-Based Screening of Proteins Containing 13C-Labeled Methyl Groups
Philip J. Hajduk,David J. Augeri,Jamey Mack,Renaldo Mendoza,Jianguo Yang,and Stephen F. Betz,Stephen W. Fesik +6 more
TL;DR: A method is described for NMR-based screening that involves monitoring the 13C/1H chemical shift changes of a protein selectively labeled with 13C at the methyl groups of valine, leucine, and isoleucine (δ1 only), increasing the sensitivity by nearly 3-fold.