CF3DODA-Me induces apoptosis, degrades Sp1, and blocks the transformation phase of the blebbishield emergency program. Academic Article uri icon

abstract

  • Cancer stem cells are capable of undergoing cellular transformation after commencement of apoptosis through the blebbishield emergency program in a VEGF-VEGFR2-dependent manner. Development of therapeutics targeting the blebbishield emergency program would thus be important in cancer therapy. Specificity protein 1 (Sp1) orchestrates the transcription of both VEGF and VEGFR2; hence, Sp1 could act as a therapeutic target. Here, we demonstrate that CF3DODA-Me induced apoptosis, degraded Sp1, inhibited the expression of multiple drivers of the blebbishield emergency program such as VEGFR2, p70S6K, and N-Myc through activation of caspase-3, inhibited reactive oxygen species; and inhibited K-Ras activation to abolish transformation from blebbishields as well as transformation in soft agar. These findings confirm CF3DODA-Me as a potential therapeutic candidate that can induce apoptosis and block transformation from blebbishields.

published proceedings

  • Apoptosis

altmetric score

  • 1

author list (cited authors)

  • Taoka, R., Jinesh, G. G., Xue, W., Safe, S., & Kamat, A. M.

citation count

  • 16

complete list of authors

  • Taoka, Rikiya||Jinesh, Goodwin G||Xue, Wenrui||Safe, Stephen||Kamat, Ashish M

publication date

  • May 2017