John E. Munroe
Eli Lilly and Company
39 Papers
351 Citations
John E. Munroe is an academic researcher from Eli Lilly and Company. The author has contributed to research in topics: Protease & Lactam. The author has an hindex of 13, co-authored 39 publications.
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Papers
Patent
HIV protease inhibitors
Bruce A. Dressman,James E. Fritz,Marlys Hammond,William Joseph Hornback,Stephen W. Kaldor,Vincent J. Kalish,John E. Munroe,Reich Siegfried Heinz,Tatlock John H,Timothy Alan Shepherd,Rodriguez Michael J,Louis Nickolaus Jungheim +11 more
- 07 Oct 1994
TL;DR: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the virus to terminate as discussed by the authors, and are thus suitable for the treatment of HIV virus known to cause AIDS.
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Discovery of a novel bicycloproline P2 bearing peptidyl α-ketoamide LY514962 as HCV protease inhibitor
Yip Yvonne Yee Mai,Frantz Victor,Jason Eric Lamar,Robert B. Johnson,Q. May Wang,Donna Barket,John I. Glass,Ling Jin,Lifei Liu,Daryl Venable,Mark Wakulchik,Congping Xie,Beverly A. Heinz,Elcira C. Villarreal,Joe Colacino,Nathan Yumibe,Mark Joseph Tebbe,John E. Munroe,Shu-Hui Chen +18 more
TL;DR: The design, syntheses and evaluation of a number of bicycloproline P2 bearing HCV protease inhibitors endowed with impressive enzyme potency, enzyme selectivity, cellular activity and favorable ADME profiles are described.
82
Cryptophycins-309, 249 and other cryptophycin analogs: preclinical efficacy studies with mouse and human tumors.
Jian Liang,Richard E. Moore,Eric D. Moher,John E. Munroe,Rima S. Al-awar,David A. Hay,Varie David Lee,Tony Y. Zhang,James Abraham Aikins,Michael J. Martinelli,Chuan Shih,James Edward Ray,Lowell Lee Gibson,Vasu Vasudevan,Lisa Polin,Kathryn White,Juiwanna Kushner,Chiab Simpson,Susan Pugh,Thomas H. Corbett +19 more
TL;DR: After the examination of 81 different Cryptophycin analogs in tumor bearing animals, C-309 has emerged as superior to all others and is being considered as second-generation clinical candidates.
79
P4 and P1′ optimization of bicycloproline P2 bearing tetrapeptidyl α-ketoamides as HCV protease inhibitors
Yip Yvonne Yee Mai,Frantz Victor,Jason Eric Lamar,Robert B. Johnson,Q. May Wang,John I. Glass,Nathan Yumibe,Mark Wakulchik,John E. Munroe,Shu-Hui Chen +9 more
TL;DR: It is found that replacement of the P4 valine as seen in 1a with cyclohexylglycine (Chg) resulted in the discovery of 5a, 5c, and 5e endowed with improved cellular activity in comparison to 1a.
67
Inhibition of Influenza Virus Hemagglutinin-Mediated Membrane Fusion by a Compound Related to Podocarpic Acid
Kirk A. Staschke,S. D. Hatch,J.C. Tang,William Joseph Hornback,John E. Munroe,Joseph M. Colacino,Mark A. Muesing +6 more
TL;DR: Results suggest that 180299 interacts with the neutral pH conformation of influenza A HA and prevents the low-pH-induced change of HA to its fusogenic conformation.
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