Prodrug strategy for PSMA-targeted delivery of TGX-221 to prostate cancer cells

Y Zhao, S Duan, X Zeng, C Liu, NM Davies…

Index: Zhao, Yunqi; Duan, Shaofeng; Zeng, Xing; Liu, Chunjing; Davies, Neal M.; Li, Benyi; Forrest, M. Laird Molecular Pharmaceutics, 2012 , vol. 9, # 6 p. 1705 - 1716

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Citation Number: 28

Abstract

TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit. Recent studies showed that TGX-221 has antiproliferative activity against PTEN-deficient tumor cell lines including prostate cancers. The objective of this study was to develop an encapsulation system for parenterally delivering TGX-221 to the target tissue through a prostate-specific membrane aptamer (PSMAa10) with little or no side effects. In ...