Stabilization of the Karenitecin® lactone by alpha-1 acid glycoprotein

@article{Yao2015StabilizationOT,
  title={Stabilization of the Karenitecin{\textregistered} lactone by alpha-1 acid glycoprotein},
  author={S. Yao and Pavankumar N. Petluru and Aulma R. Parker and Daoyuan Ding and Xinghai Chen and Qiuli Huang and Harry Kochat and Frederick H. Hausheer},
  journal={Cancer Chemotherapy and Pharmacology},
  year={2015},
  volume={75},
  pages={719-728}
}
PurposeCamptothecins contain a lactone ring that is necessary for antitumor activity, and hydrolysis of the lactone ring yields an inactive carboxylate species. Human serum albumin (HSA) and alpha-1 acid glycoprotein (AGP) are clinically significant plasma proteins thought to have important roles in camptothecin lactone stability. Herein, we examined the effect(s) of HSA and AGP on the lactone stability of Karenitecin, a novel, highly lipophilic camptothecin analog, currently at the phase 3… Expand
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