Back

Speaker Details

Biography

Abstract

Our investigations establish linear correlations between the ionization potential of exogenous phenol (P) and fl avone (F) derivatives and their biological eff ects on induction of a powerful cancer-protective enzyme NAD(P)H:quinone reductase (NQO1) via the Nrf2-Keap1 pathway. Th ey also show that the NQO1 activation involves (i) oxidation of the P and F inducers to oxidant species which are their quinone derivatives (Q) and (ii) oxidation by these quinones Q of two highly reactive thiol groups of a protein Keap1 activating transcription factor Nrf2. Th e linear correlations observed for benefi cial cancerprotective pathways triggered by electrophiles Q in vitro explain the linear correlations which we observe in vivo (rodents) for the inhibition of chemically-induced carcinogenesis by P and F derivatives. Our in silico evaluation of biological activity of P and F derivatives should orient the rational design of new congeners with greater potency for cancer chemoprotection and might reduce the expensive use of in vivo and in vitro bioassays.

Speaker Presentations

Photos

    No Photos Avilable

PDFs

No PDF File Avilable

PPTs

No PPT File Avilable