Abstract
A screen of N-alkyl-Gly-boro-Pro DPP inhibitors using an acute murine model revealed that N-adamantyl and N-cycloalkyl groups greater in size than cyclobutyl significantly induced G-CSF. Treatment of neutropenic mice with the most efficacious compound, AX8312 (N-(1-adamantyl)-Gly-boro-Pro), resulted in a faster and greater neutrophil recovery versus vehicle-treated mice.
Keywords: N-alkyl-Gly-boro-Pro, G-CSF, Neutropenia, Cytokine, AX8312
Letters in Drug Design & Discovery
Title: Discovery of AX8312, an N-alkyl-Gly-boro-Pro Derivative that Accelerates Recovery from Neutropenia in the Mouse
Volume: 5 Issue: 5
Author(s): Emme C.K. Lin, Kevin R. Shreder, Melissa C. Zhang, Yi Hu, Lisa Morera, Min Wu, Melissa S. Wong, Lifu Ma, Doris Chun, Sergio Corral and John W. Kozarich
Affiliation:
Keywords: N-alkyl-Gly-boro-Pro, G-CSF, Neutropenia, Cytokine, AX8312
Abstract: A screen of N-alkyl-Gly-boro-Pro DPP inhibitors using an acute murine model revealed that N-adamantyl and N-cycloalkyl groups greater in size than cyclobutyl significantly induced G-CSF. Treatment of neutropenic mice with the most efficacious compound, AX8312 (N-(1-adamantyl)-Gly-boro-Pro), resulted in a faster and greater neutrophil recovery versus vehicle-treated mice.
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Lin C.K. Emme, Shreder R. Kevin, Zhang C. Melissa, Hu Yi, Morera Lisa, Wu Min, Wong S. Melissa, Ma Lifu, Chun Doris, Corral Sergio and Kozarich W. John, Discovery of AX8312, an N-alkyl-Gly-boro-Pro Derivative that Accelerates Recovery from Neutropenia in the Mouse, Letters in Drug Design & Discovery 2008; 5 (5) . https://dx.doi.org/10.2174/157018008784912081
DOI https://dx.doi.org/10.2174/157018008784912081 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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