Thomas G. Steele
United States Military Academy
9 Papers
56 Citations
Thomas G. Steele is an academic researcher from United States Military Academy. The author has contributed to research in topics: Amyloid precursor protein & Chemistry. The author has an hindex of 8, co-authored 9 publications.
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Papers
In Vitro and in Vivo Evaluation of Dihydropyrimidinone C-5 Amides as Potent and Selective α1A Receptor Antagonists for the Treatment of Benign Prostatic Hyperplasia
James C. Barrow,Philippe G. Nantermet,Harold G. Selnick,Kristen L. Glass,Kenneth E. Rittle,Kevin F. Gilbert,Thomas G. Steele,Carl F. Homnick,Roger M. Freidinger,Rick W. Ransom,Paul J. Kling,Duane R. Reiss,Theodore P. Broten,Terry W. Schorn,Raymond S.L. Chang,Stacey O'Malley,Timothy V. Olah,Joan D. Ellis,A. Barrish,Kelem Kassahun,Paula Leppert,Dhanapalan Nagarathnam,Carlos Forray +22 more
TL;DR: While many of the compounds tested displayed poor pharmacokinetics, compound 48 was found to be more potent than terazosin in both a rat model of prostate tone and a dog model of intra-urethral pressure without significantly affecting blood pressure.
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Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
Ramakanth Sarabu,Fred Thomas Bizzarro,Wendy Lea Corbett,Mark T. Dvorozniak,Wanping Geng,Joseph F. Grippo,Nancy-Ellen Haynes,Stanley D. Hutchings,Lisa M. Garofalo,Kevin Richard Guertin,Darryl W. Hilliard,Marek M. Kabat,Robert Francis Kester,Wang Ka,Zhenmin Liang,Paige Erin Mahaney,Linda Marcus,Franz M. Matschinsky,David J Moore,Jagdish Kumar Racha,Roumen Nikolaev Radinov,Yi Ren,Lida Qi,Michael Pignatello,Cheryl Spence,Thomas G. Steele,John Tengi,Joseph Grimsby +27 more
TL;DR: Piragliatin was found to lower pre- and postprandial glucose levels, improve the insulin secretory profile, increase β-cell sensitivity to glucose, and decrease hepatic glucose output in patients with T2D.
90
BACE-1 inhibition by a series of ψ[CH2NH] reduced amide isosteres
Craig A. Coburn,Shawn J. Stachel,Kristen G. Jones,Thomas G. Steele,Diane M Rush,Jillian DiMuzio,Beth Pietrak,Ming-Tain Lai,Qian Huang,Janet Lineberger,Lixia Jin,Sanjeev Munshi,M. Katharine Holloway,Amy S. Espeseth,Adam J. Simon,Daria J. Hazuda,Samuel L. Graham,Joseph P. Vacca +17 more
TL;DR: A series of β-site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing a ψ(CH 2 NH) reduced amide bond were synthesized and incorporated as a non-cleavable peptide surrogate afforded inhibitors possessing low nanomolar potencies in both an enzymatic and cell-based assay.
60
Biochemical and cell-based assays for characterization of BACE-1 inhibitors.
Beth Pietrak,Ming-Chih Crouthamel,Katherine Tugusheva,Janet Lineberger,Min Xu,Jillian DiMuzio,Thomas G. Steele,Amy S. Espeseth,Shawn J. Stachel,Craig A. Coburn,Samuel L. Graham,Joseph P. Vacca,Xiao-Ping Shi,Adam J. Simon,Daria J. Hazuda,Ming-Tain Lai +15 more
TL;DR: Two novel assays for the characterization of BACE-1 inhibitors are reported, including a sensitive 96-well HPLC biochemical assay that uses a unique substrate containing an optimized peptide cleavage sequence, NFEV, spanning from the P2-P2' positions, permitting the evaluation of inhibitors with subnanomolar potency.
49
Discovery and optimization of 2-pyridinone aminal integrase strand transfer inhibitors for the treatment of HIV
John D. Schreier,Mark Embrey,Izzat T. Raheem,Guillaume Barbe,Louis-Charles Campeau,Dubost David C,Jamie M. McCabe Dunn,Jay A. Grobler,Timothy J. Hartingh,Daria J. Hazuda,Daniel J. Klein,Michael D. Miller,Keith P. Moore,Nguyen Natalie,Natasa Pajkovic,David A. Powell,Rada Vanessa L,John M. Sanders,John T. Sisko,Thomas G. Steele,John S. Wai,Abbas Walji,Min Xu,Paul J. Coleman +23 more
TL;DR: Systematic optimization carried out at the amide and aminal positions on the periphery of the core provided the necessary balance of antiviral activity and physiochemical properties and led to a novel aminal lead compound with the desired virological profile and preclinical pharmacokinetic profile to support a once-daily human dose prediction.
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