Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction

Tom D. Heightman; James F. Callahan; Elisabetta Chiarparin; Joseph E. Coyle; Charlotte Griffiths-Jones; Ami S. Lakdawala; Rachel McMenamin; Paul N. Mortenson; David Norton; Torren M. Peakman; Sharna J. Rich; Caroline Richardson; William L. Rumsey; Yolanda Sanchez; Gordon Saxty; Henriëtte M. G. Willems; Lawrence Wolfe; Alison J.-A. Woolford; Zining Wu; Hongxing Yan; Jeffrey K. Kerns; Thomas G. Davies

doi:10.1021/acs.jmedchem.9b00279

Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.9b00279 ◽

2019 ◽

Vol 62 (9) ◽

pp. 4683-4702 ◽

Cited By ~ 21

Author(s):

Tom D. Heightman ◽

James F. Callahan ◽

Elisabetta Chiarparin ◽

Joseph E. Coyle ◽

Charlotte Griffiths-Jones ◽

...

Keyword(s):

Propionic Acid ◽

Protein Interaction ◽

Related Factor ◽

Nuclear Factor ◽

Protein Protein Interaction ◽

Structure Activity ◽

Nrf2 Protein

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Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.6b00228 ◽

2016 ◽

Vol 59 (8) ◽

pp. 3991-4006 ◽

Cited By ~ 109

Author(s):

Thomas G. Davies ◽

William E. Wixted ◽

Joseph E. Coyle ◽

Charlotte Griffiths-Jones ◽

Keisha Hearn ◽

...

Keyword(s):

Protein Interaction ◽

Related Factor ◽

Nuclear Factor ◽

High Cell ◽

Protein Protein Interaction ◽

Nrf2 Protein

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Discovery and Development of Kelch-like ECH-Associated Protein 1. Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction Inhibitors: Achievements, Challenges, and Future Directions

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.6b00586 ◽

2016 ◽

Vol 59 (24) ◽

pp. 10837-10858 ◽

Cited By ~ 53

Author(s):

Zheng-Yu Jiang ◽

Meng-Chen Lu ◽

Qi-Dong You

Keyword(s):

Protein Interaction ◽

Related Factor ◽

Nuclear Factor ◽

Future Directions ◽

Protein Protein Interaction ◽

Nrf2 Protein

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ZJ01, a Small Molecule Inhibitor of the Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Protein-Protein Interaction, Reduces Hyperoxic Acute Lung Injury in a Mouse Model

Medical Science Monitor ◽

10.12659/msm.920467 ◽

2020 ◽

Vol 26 ◽

Author(s):

Jun Wan ◽

Shaoyan Lin ◽

Xiuling Huang ◽

Qianqin Li ◽

Lingjun Zeng ◽

...

Keyword(s):

Acute Lung Injury ◽

Lung Injury ◽

Mouse Model ◽

Small Molecule ◽

Protein Interaction ◽

Related Factor ◽

Nuclear Factor ◽

Protein Protein Interaction ◽

Molecule Inhibitor ◽

Nrf2 Protein

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Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein−Protein Interaction

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.1c01351 ◽

2021 ◽

Author(s):

David Norton ◽

William G. Bonnette ◽

James F. Callahan ◽

Maria G. Carr ◽

Charlotte M. Griffiths-Jones ◽

...

Keyword(s):

Carboxylic Acid ◽

Protein Interaction ◽

Related Factor ◽

Nuclear Factor ◽

Guided Discovery ◽

Protein Protein Interaction ◽

Nrf2 Protein

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Faculty Opinions recommendation of Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.726256171.793523282 ◽

2016 ◽

Author(s):

Peter R Bernstein

Keyword(s):

Protein Interaction ◽

Related Factor ◽

Nuclear Factor ◽

High Cell ◽

Protein Protein Interaction ◽

Nrf2 Protein

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Emerging Substrate Proteins of Kelch-like ECH Associated Protein 1 (Keap1) and Potential Challenges for the Development of Small-Molecule Inhibitors of the Keap1-Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Protein–Protein Interaction

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.9b01865 ◽

2020 ◽

Vol 63 (15) ◽

pp. 7986-8002 ◽

Cited By ~ 5

Author(s):

Yong Zhang ◽

Zeyu Shi ◽

Yujun Zhou ◽

Qiong Xiao ◽

Hongyue Wang ◽

...

Keyword(s):

Small Molecule ◽

Protein Interaction ◽

Small Molecule Inhibitors ◽

Related Factor ◽

Nuclear Factor ◽

Protein Protein Interaction ◽

Substrate Proteins ◽

Nrf2 Protein

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Design, Synthesis, and Structure–Activity Relationships of Indoline-Based Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-Like 2 (Keap1-Nrf2) Protein–Protein Interaction Inhibitors

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.0c01116 ◽

2020 ◽

Vol 63 (19) ◽

pp. 11149-11168 ◽

Cited By ~ 1

Author(s):

Hai-Shan Zhou ◽

Lv-Bin Hu ◽

Han Zhang ◽

Wen-Xin Shan ◽

Yan Wang ◽

...

Keyword(s):

Protein Interaction ◽

Nuclear Factor ◽

Design Synthesis ◽

Structure Activity Relationships ◽

Protein Protein Interaction ◽

Structure Activity ◽

Nrf2 Protein

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Faculty Opinions recommendation of Discovery and Development of Kelch-like ECH-Associated Protein 1. Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction Inhibitors: Achievements, Challenges, and Future Directions.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.726815278.793538955 ◽

2017 ◽

Author(s):

Stuart Lipton

Keyword(s):

Protein Interaction ◽

Related Factor ◽

Nuclear Factor ◽

Future Directions ◽

Protein Protein Interaction ◽

Nrf2 Protein

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Discovery of a Potent Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1–Nrf2) Protein–Protein Interaction Inhibitor with Natural Proline Structure as a Cytoprotective Agent against Acetaminophen-Induced Hepatotoxicity

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.9b00818 ◽

2019 ◽

Vol 62 (14) ◽

pp. 6796-6813 ◽

Cited By ~ 12

Author(s):

Meng-Chen Lu ◽

Xian Zhang ◽

Feng Wu ◽

Shi-Jie Tan ◽

Jing Zhao ◽

...

Keyword(s):

Protein Interaction ◽

Related Factor ◽

Nuclear Factor ◽

Protein Protein Interaction ◽

Cytoprotective Agent ◽

Nrf2 Protein

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Structure–Activity and Structure–Property Relationship and Exploratory in Vivo Evaluation of the Nanomolar Keap1–Nrf2 Protein–Protein Interaction Inhibitor

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.5b00185 ◽

2015 ◽

Vol 58 (16) ◽

pp. 6410-6421 ◽

Cited By ~ 52

Author(s):

Zheng-Yu Jiang ◽

Li−Li Xu ◽

Meng-Chen Lu ◽

Zhi-Yun Chen ◽

Zhen-Wei Yuan ◽

...

Keyword(s):

Protein Interaction ◽

Structure Property ◽

In Vivo Evaluation ◽

Protein Protein Interaction ◽

Property Relationship ◽

Structure Activity ◽

Structure Property Relationship ◽

Nrf2 Protein

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