Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology
Min Lu(Merck & Co., Inc., Rahway, NJ, USA (United States)), Hongjun Zhang(Merck & Co., Inc., Rahway, NJ, USA (United States)), Derun Li(Merck & Co., Inc., Rahway, NJ, USA (United States)), Matthew C. Childers(Merck & Co., Inc., Rahway, NJ, USA (United States)), Qinglin Pu(Merck & Co., Inc., Rahway, NJ, USA (United States)), R.L. Palte(Merck & Co., Inc., Rahway, NJ, USA (United States)), Symon Gathiaka(Merck & Co., Inc., Rahway, NJ, USA (United States)), Thomas W. Lyons(Merck & Co., Inc., Rahway, NJ, USA (United States)), Anandan Palani(Merck & Co., Inc., Rahway, NJ, USA (United States)), Peter W. Fan(Merck & Co., Inc., Rahway, NJ, USA (United States)), Peter Spacciapoli(Quantitative BioSciences), J. Richard Miller(Quantitative BioSciences), Hyelim Cho(Quantitative BioSciences), Mangeng Cheng(Quantitative BioSciences), Kalyan Chakravarthy(Quantitative BioSciences), Jennifer O’Neil(Merck & Co., Inc., Rahway, NJ, USA (United States)), Padmanabhan Eangoor(Merck & Co., Inc., Rahway, NJ, USA (United States)), Adam Beard(Merck & Co., Inc., Rahway, NJ, USA (United States)), Hai‐Young Kim(Merck & Co., Inc., Rahway, NJ, USA (United States)), Josep Saurí(Merck & Co., Inc., Rahway, NJ, USA (United States)), Hakan Günaydin(Merck & Co., Inc., Rahway, NJ, USA (United States)), David L. Sloman(Merck & Co., Inc., Rahway, NJ, USA (United States)), Phieng Siliphaivanh(Merck & Co., Inc., Rahway, NJ, USA (United States)), Jared N. Cumming(Merck & Co., Inc., Rahway, NJ, USA (United States)), Christian Fischer(Merck & Co., Inc., Rahway, NJ, USA (United States))
Cited by 25Open Access
Abstract
was well tolerated following multiple days of dosing at concentrations that exceed those required for serum arginase inhibition and concomitant arginine elevation in a syngeneic mouse carcinoma model.
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