Drug name: Irinotecan + YHO-13351


Related CSCTT Targets

ABCG2 [ref.1, 2]Q9UNQ0

irinotecan, CPT11

Cas.no PubChem ID
97682-44-5 60838
Known Target
DNA topoisomerase 1P11387
DNA topoisomerase I, mitochondrialQ969P6
Structure
...
Introduction
Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. It is a derivative of camptothecin that inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex, and causes double-strand DNA breakage and cell death. It is a derivative of camptothecin.

YHO-13351

Cas.no PubChem ID
912288-64-3
Known Target
ATP-binding cassette sub-family G member 2Q9UNQ0
Structure
...
Introduction
An in vivo bioavailable and highly water soluble ( >100 mg/ml) diethylaminoacetate prodrug of YHO-13177 that reverses ABCG2-mediated irinotecan resistance in P388/BCRP and HCT116/BCRP xenograft mouse models, and suppresses tumor growth and significantly enhances the survival (100 or 200 mg/kg, i.p.).

Reference

  • [1] ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan. Shishido, Y., et al. (2013).Anticancer Res.33(4):1379-86.
    23564776. [ 23564776 ]
  • [2] Novel acrylonitrile derivatives, YHO-13177 and YHO-13351, reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo. Yamazaki, R., et al. (2011).Mol Cancer Ther.10(7):1252-63.
    21566063. [ 21566063 ]

Back to top