A New Class of Molecular Glues: Double Allostery Restores KEAP1 Control of NRF2

Roy and colleagues describe VVD-065, a covalent allosteric molecular glue that binds KEAP1 at Cys151 to enhance KEAP1-CUL3 assembly, restore NRF2 ubiquitination and degradation, and selectively suppress NRF2-driven tumors by reactivating endogenous E3 ligase function. See related article by Roy et al., p. 953.

Authors

George M. Burslem (ORCID: https://orcid.org/0000-0002-2812-983X)
Jordi C J Hintzen

Institutions

University of Pennsylvania (US)

Publication Details

Journal: Cancer Discovery
Published: 2026-05-01
DOI: https://doi.org/10.1158/2159-8290.cd-26-0342
Primary Topic: Melanoma and MAPK Pathways
Type: article
Field-Weighted Citation Impact: 0.00

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article

A New Class of Molecular Glues: Double Allostery Restores KEAP1 Control of NRF2

George M. Burslem, Jordi C J Hintzen

May 1, 2026

Cancer Discovery

Melanoma and MAPK Pathways

article

A New Class of Molecular Glues: Double Allostery Restores KEAP1 Control of NRF2

George M. Burslem, Jordi C J Hintzen

May 1, 2026article en

Abstract

Cancer DiscoveryVol. 16(5)

University of Pennsylvania (US)

Openalex Percentile: Top 12%

Melanoma and MAPK Pathways

DOI Source OpenAlex

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A New Class of Molecular Glues: Double Allostery Restores KEAP1 Control of NRF2 — George M. Burslem, Jordi C J Hintzen · Cancer Discovery (2026) | TGRS Research Map | TGRS