Discovery of AX8312, an N-alkyl-Gly-boro-Pro Derivative that Accelerates Recovery from Neutropenia in the Mouse

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; John   W.   Kozarich

Letters in Drug Design & Discovery

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

DOI: 10.2174/157018008784912081

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Discovery of AX8312, an N-alkyl-Gly-boro-Pro Derivative that Accelerates Recovery from Neutropenia in the Mouse

Page: [340 - 345] Pages: 6

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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

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