S
Stephen J. Gardell
Researcher at United States Military Academy
Publications - 55
Citations - 3679
Stephen J. Gardell is an academic researcher from United States Military Academy. The author has contributed to research in topics: Thrombin & Discovery and development of direct thrombin inhibitors. The author has an hindex of 28, co-authored 48 publications receiving 3542 citations.
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Journal ArticleDOI
Photoactivated γ-secretase inhibitors directed to the active site covalently label presenilin 1
Yueming Li,Min Xu,Ming-Tain Lai,Qian Huang,José L. Castro,Jillian DiMuzio-Mower,T. Harrison,C Lellis,Alan Nadin,Joseph G. Neduvelil,R B Register,Mohinder K. Sardana,Mark S. Shearman,Adrian L. Smith,Xiao Ping Shi,Kuo-Chang Yin,Jules A. Shafer,Stephen J. Gardell +17 more
TL;DR: In this paper, photoaffinity labeling of presenilin 1 and 2 (PS1 and PS2) was performed by potent gamma-secretase inhibitors that were designed to function as transition state analogue inhibitors directed to the active site of an aspartyl protease.
Journal ArticleDOI
Presenilin 1 is linked with gamma-secretase activity in the detergent solubilized state.
Yueming Li,Ming-Tain Lai,Min Xu,Qian Huang,Jillian DiMuzio-Mower,Mohinder K. Sardana,Xiao-Ping Shi,Kuo-Chang Yin,Jules A. Shafer,Stephen J. Gardell +9 more
TL;DR: The detergent solubilization and partial characterization of gamma-secretase suggest that gamma- secretase activity is catalyzed by a PS1-containing macromolecular complex.
Journal ArticleDOI
Presenilin-1 and Presenilin-2 Exhibit Distinct yet Overlapping γ-Secretase Activities
Ming-Tain Lai,Elizabeth Chen,Ming-Chih Crouthamel,Jillian DiMuzio-Mower,Min Xu,Qian Huang,Eric A. Price,R. Bruce Register,Xiao-Ping Shi,Dorit B. Donoviel,Alan Bernstein,Daria J. Hazuda,Stephen J. Gardell,Yueming Li +13 more
TL;DR: The distinct yet overlapping enzymatic properties of the PS1 γ-secretase complex and the PS2 γ/substantially higher specific activity imply that these two putative aspartyl class proteases may contribute to different biological processes.
Journal ArticleDOI
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
Joachim Rudolph,William P. Esler,Stephen O'connor,Philip Coish,Philip Wickens,Michael Brands,Donald Bierer,Brian T. Bloomquist,Georgiy Bondar,Libing Chen,Chih-Yuan Chuang,Thomas H. Claus,Zahra Fathi,Wenlang Fu,Uday Khire,James A. Kristie,Xiao-Gao Liu,Derek B. Lowe,Andrea Mcclure,Martin Michels,Astrid A. Ortiz,Philip D. Ramsden,Robert Schoenleber,Tatiana E. Shelekhin,Alexandros Vakalopoulos,Weifeng Tang,Lei Wang,Lin Yi,Stephen J. Gardell,James N. Livingston,Laurel Sweet,Bullock William H +31 more
TL;DR: Piperidine-substituted quinazolinone derivatives were identified as a new class of small-molecule GHS-R1a antagonists and revealed suppression of food intake and body weight reduction as well as glucose-lowering effects mediated by glucose-dependent insulin secretion.
Journal ArticleDOI
The Pro Domain of β-Secretase Does Not Confer Strict Zymogen-like Properties but Does Assist Proper Folding of the Protease Domain *
Xiao-Ping Shi,Elizabeth Chen,Kuo-Chang Yin,Sang Na,Victor M. Garsky,Ming-Tain Lai,Yue-Ming Li,Michael Platchek,R. Bruce Register,Mohinder K. Sardana,Mei-Jy Tang,James Thiebeau,Theresa Wood,Jules A. Shafer,Stephen J. Gardell +14 more
TL;DR: Findings show that the Pro domain in ProBACE460 does not suppress activity as in a strict zymogen but does appear to facilitate proper folding of an active protease domain.