Keap1-Kelch-targeting protein-protein interaction inhibitors, but not reversibly-binding electrophiles, increase the thermostability of Keap1 in the cellular environment

Sharadha Dayalan Naidu; Dina Dikovskaya; Jasmine M Walker; Charlotte J.Y. Lim Jia Yee; Annamarie J. Cafferkey; Manaka Tatsuno; Jialin Feng; Terry W. Moore; Tatum Johnson; Tadashi Honda; Geoff Wells; Takafumi Suzuki; Masayuki Yamamoto; Albena T. Dinkova-Kostova

doi:10.1039/d6cb00045b

January 1, 2025RSC Chemical BiologyOpen Access

Keap1-Kelch-targeting protein-protein interaction inhibitors, but not reversibly-binding electrophiles, increase the thermostability of Keap1 in the cellular environment

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Key Points

To investigate how different inhibitors affect the thermostability of Keap1 in a cellular context.
Evaluated protein-protein interactions using inhibitors targeting Keap1-Kelch.
Assessed the impact of electrophiles on Keap1 stability.
Conducted stability assays under various cellular conditions.
Keap1 thermostability increased significantly with protein-protein interaction inhibitors.
Reversibly-binding electrophiles did not enhance Keap1 stability.
Enhanced stability correlates with improved cellular defense against stress.

Implication

Inhibitors improve Keap1 thermostability in cellular environments, suggesting potential therapeutic strategies.

Abstract

The Kelch-like ECH-associated protein 1 / Nuclear factor erythroid 2-p45-related factor 2 (Keap1/Nrf2) partnership orchestrates the cellular defence against oxidative, inflammatory and metabolic stress. Dysregulation of Nrf2 is involved in...

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Cite This Study

Naidu et al. (2025) studied this question.

synapsesocial.com/papers/69d894526c1944d70ce053d7 https://doi.org/10.1039/d6cb00045b

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Keap1-Kelch-targeting protein-protein interaction inhibitors, but not reversibly-binding electrophiles, increase the thermostability of Keap1 in the cellular environment

Key Points

Implication

Abstract

Discussion

Cite This Study

Keap1-Kelch-targeting protein-protein interaction inhibitors, but not reversibly-binding electrophiles, increase the thermostability of Keap1 in the cellular environment

Key Points

Implication

Abstract

Discussion

Cite This Study

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