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Keap1 in adhesion complexes

Cell Motility, 2003
AbstractCell adhesion complexes are sensors that interact with the extracellular environment and allow for the transmission of signals found outside the cell across the plasma membrane to the cell interior. Keap1 is a newly identified component of cell adhesion complexes.
Michaella, Velichkova, Tama, Hasson
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Keap1ing an eye on Slc33A1

Nature Cancer, 2020
KEAP1 is a tumor suppressor encoded by a gene commonly mutated in lung cancer. A systematic search for Keap1-mutant cancer vulnerabilities now reveals that Slc33a1 is a context-specific essential gene that represents a promising new anti-cancer target.
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Development of Novel Inhibitors for Keap1-Nrf2 and Keap1-P62 Protein-Protein Interaction

Free Radical Biology and Medicine, 2016
Nrf2-Keap1 system is a biological defense mechanism in response to various stressors. An inhibitor for Keap1-Nrf2 interaction to activate Nrf2 is expected as a novel target for drug discovery in oxidative stress-related disorders. However, Nrf2 is accumulated in many types of cancer and its expression is induced during the course of drug resistance ...
Daisuke Yasuda   +14 more
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A double whammy for KEAP1

Cell Chemical Biology
In this issue of Cell Chemical Biology, Lu et al.1 report the discovery of a bivalent KEAP1 inhibitor (biKEAP1), which more rapidly activates NRF2 compared to previously reported monovalent KEAP1 inhibitors. biKEAP1suppresses acute inflammation in animal models.
Jan, Gerhartz, Radosław P, Nowak
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Keap1/Nrf2 system regulates neuronal survival as revealed through study of keap1 gene-knockout mice

Biochemical and Biophysical Research Communications, 2009
Keap1 is proposed to be a sensor protein of electrophilic compounds and a transducer of the signal from electrophilic compounds for transcriptional activation. Thus, the use of keap1 gene-knockout (KO) mice is a straightforward approach in order to clarify the molecular background for the use of electrophilies as neuroprotective compounds.
Takumi, Satoh   +5 more
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Role of human Keap1 S53 and S293 residues in modulating the binding of Keap1 to Nrf2

Biochimie, 2019
Keap1 is deemed as a suppressor of Nrf2 in cytoplasm by sequestrating Nrf2 to proteolysis as an adapter of the Cul3-Rbx1 E3 ubiquitin ligase complex. In the study, it was proposed that post-translational modification might affect the interaction between Nrf2 and Keap1, and the profiles of the phosphorylation of amino acid residues of Keap1 and its ...
Shuangshuang Wei   +7 more
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Patenting perspective on Keap1 inhibitors (2019–2024)

Expert Opinion on Therapeutic Patents
Kelch-like ECH-associated protein 1 (Keap1), an E3 ligase negatively regulating the nuclear factor erythroid 2-related factor 2 (Nrf2), has emerged as an auspicious drug target for treating ailments associated with oxidative stress and inflammation. Discovery of Keap1 inhibitors have attracted significant interest.This review covers patents on Keap1 ...
Yongfu, Luo   +7 more
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KEAP1/NRF2 SIGNALING IN AGED BONE

Bone health is a critical element in mammalian quality of life. The Keap1/Nrf2 signaling pathway has recently been observed to be instrumental in a multitude of regulatory processes pertaining to cytoprotective gene expression, with growing evidence of its role in bone metabolism.
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