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Table 1 The selected activators and inhibitors of Nrf2 and their mechanisms of action

From: An update of Nrf2 activators and inhibitors in cancer prevention/promotion

 

Compound

Type

Mechanism of action

Reference

Nrf2 activators

SFN

Isothiocyanate

Electrophilic modification of Keap1-Cys-151

[87]

OPZ

Organosulfur compound

Electrophilic modification of Keap1-Cys-151

[107]

EGCG

Catechin

Oxidizing the cysteine thiols of Keap1

[110]

DMF

Fumaric acid ester

Electrophilic modification of Keap1-Cys-151

[127]

DATS

Isothiocyanate

Modification of Keap1-Cys-288

[141]

CUR

Stilbene

Electrophilic modification of Keap1-Cys-151

[159]

CDDO

Synthetic triterpenoids

Electrophilic modification of Keap1-Cys-151

[19]

API

Plant flavone

Epigenetic modifications of Nrf2

[179]

RES

(E)-Stilbene derivate

Electrophilic modification of Keap1-Cys-151

[188]

Nrf2 inhibitors

BRU

Triterpene lactone compound

Stimulation of Nrf2 poly-ubiquitination

[194]

LUT

Plant flavone

Nrf2 mRNA degradation, Reduction of Nrf2 binding to AREs

[198]

TRG

Coffee-derived alkaloid

Prevention of nuclear translocation of NRF2

[201]

AA

Natural vitamin

Electrophilic modification of Keap1-Cys-151

[204]

RA

Metabolite of vitamin A

Prevention of nuclear translocation of NRF2

[210]

CHR

Plant flavone

Prevention of nuclear translocation of NRF2

[219]

  1. AA Ascorbic acid; API Apigenin; BRU Brusatol; CDDO 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid; CHR Chrysin; CUR Curcumin; DATS Diallyl trisulfide; DMF Dimethylfumarate; EGCG Epigallocatechin-3-gallate; LUT Luteolin; OPZ Oltipraz; RA Retinoic Acid; RES Resveratrol; SFN Sulforaphane; TRG Trigonelline