Home
Resources
Publications
A Small Molecule Inhibits Deregulated NRF2 Transcriptional Activity in Cancer

A Small Molecule Inhibits Deregulated NRF2 Transcriptional Activity in Cancer

Michael J Bollong, Hwayoung Yun, Lance Sherwood, Ashley K Woods, Luke L Lairson, Peter G Schultz

ACS Chem Biol. 2015 Oct 16;10(10):2193-8.

PMID: 26270491

Abstract:

NRF2 serves as the master regulator of oxidative stress resistance in mammalian cells. Although NRF2 activation decreases tumorigenic events in normal cells, accumulating evidence suggests that cancers have broadly selected for NRF2-activating mutations to promote anabolic growth and chemoresistance. Small molecules which inhibit NRF2 activity may therefore offer promise as an alternative anticancer treatment in NRF2 dependent cancers. We have used a high throughput screen to identify small molecules which decrease NRF2 transcriptional activity at antioxidant response element sites. One such molecule, termed AEM1, is capable of broadly decreasing the expression of NRF2 controlled genes, sensitizing A549 cells to various chemotherapeutic agents, and inhibiting the growth of A549 cells in vitro and in vivo. Profiling of multiple cell lines for their responsiveness to AEM1 revealed that AEM1's activities are restricted to cell lines harboring mutations which render NRF2 constitutively active.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1030123900	AEM1		1030123-90-0	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: