• Corpus ID: 44777298

Preclinical Development Novel Acrylonitrile Derivatives , YHO-13177 and YHO-13351 , Reverse BCRP / ABCG 2-Mediated Drug Resistance In Vitro and In Vivo

  title={Preclinical Development Novel Acrylonitrile Derivatives , YHO-13177 and YHO-13351 , Reverse BCRP / ABCG 2-Mediated Drug Resistance In Vitro and In Vivo},
  author={Ryuta Yamazaki and Yukiko Nishiyama and Tomio Furuta and Hiroshi Hatano and Yoshiaki Igarashi and Naoyuki Asakawa and Hiroshi Kodaira and Hiroyuki Takahashi and Ritsuo Aiyama and Takeshi Matsuzaki and Naomi Yagi and Yoshikazu Sugimoto},
Breast cancer resistance protein (BCRP/ABCG2) confers resistance to anticancer drugs such as 7-ethyl-10hydroxycamptothecin (SN-38, an active metabolite of irinotecan), mitoxantrone, and topotecan. In this study, we examined the reversing effects of YHO-13177, a novel acrylonitrile derivative, and its water-soluble diethylaminoacetate prodrug YHO-13351 on the BCRP-mediated drug resistance. YHO-13177 potentiated the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human… 
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  • S. Kawabata, M. Oka, S. Kohno
  • Biology, Medicine
    Clinical cancer research : an official journal of the American Association for Cancer Research
  • 2003
The levels of BCRP mRNA expression in the cell lines were significantly correlated with the B CRP function and the sensitivity to SN-38 and topotecan, and some NSCLC tissues expressed sufficient levels of the BCRp mRNA to confer drug resistance in vitro.