Results 21 to 30 of about 21,045 (211)

Interaction Energetics and Druggability of the Protein-Protein Interaction between Kelch-like ECH-Associated Protein 1 (KEAP1) and Nuclear Factor Erythroid 2 Like 2 (Nrf2). [PDF]

open access: yesBiochemistry, 2020
Development of small molecule inhibitors of protein-protein interactions (PPIs) is hampered by our poor understanding of the druggability of PPI target sites. Here, we describe the combined application of alanine-scanning mutagenesis, fragment screening, and FTMap computational hot spot mapping to evaluate the energetics and druggability of the highly ...
Zhong M   +16 more
europepmc   +4 more sources

Marburg Virus VP24 Protein Relieves Suppression of the NF-κB Pathway Through Interaction With Kelch-like ECH-Associated Protein 1. [PDF]

open access: yesJ Infect Dis, 2015
Marburg virus (MARV) is an emerging zoonotic pathogen that causes hemorrhagic fever. MARV VP24 (mVP24) protein interacts with the host cell protein Kelch-like-ECH-associated protein 1 (Keap1). Keap1 interacts with and promotes the degradation of IκB kinase β (IKKβ), a component of the IκB kinase (IKK) complex that regulates nuclear factor-κB (NF-κB ...
Edwards MR, Basler CF.
europepmc   +4 more sources

Psoralen and Isopsoralen Activate Nuclear Factor Erythroid 2-Related Factor 2 Through Interaction With Kelch-Like ECH-Associated Protein 1. [PDF]

open access: yesFood Sci Nutr
ABSTRACTAs natural furocoumarins, psoralen and its isomer isopsoralen are widely distributed in various fruits including Ficus carica L., vegetables including celery, and medicinal herbs including Psoralea corylifolia L. Although psoralen and isopsoralen have been used as dietary supplements because of their bioactivities such as antibacterial and anti‐
Lv C   +8 more
europepmc   +3 more sources

Chronic Activation of Hepatic Nrf2 Has No Major Effect on Fatty Acid and Glucose Metabolism in Adult Mice [PDF]

open access: yes, 2016
The transcription factor NF-E2-related factor 2 (Nrf2) induces cytoprotective genes, but has also been linked to the regulation of hepatic energy metabolism. In order to assess the pharmacological potential of hepatic Nrf2 activation in metabolic disease,
Brachs, Maria   +10 more
core   +13 more sources

Association between Kelch-like ECH-associated protein-1 and GRACE risk score in non-ST elevation myocardial infarction.

open access: yesEuropean review for medical and pharmacological sciences, 2023
In this study, we measured the levels of Kelch-like ECH-associated protein 1 (KEAP1), which has the potential antioxidant capacity, among non-ST elevation myocardial infarction (NSTEMI) patients compared with healthy controls. We also investigated the possible association between KEAP1 levels and the GRACE score, which is a universal risk score ...
Vuruskan, E.   +8 more
openaire   +2 more sources

Kelch-like ECH-associated Protein 1/Nuclear Factor Erythroid 2-related Factor 2 Pathway and Its Interplay with Oncogenes in Lung Tumorigenesis. [PDF]

open access: yesJ Cancer Prev
Nuclear factor erythroid 2-related factor 2 (NRF2), a transcription factor regulating cellular redox homeostasis, exhibits a complex role in cancer biology. Genetic mutations in the Kelch-like ECH-associated protein 1 (KEAP1)/NRF2 system, which lead to NRF2 hyperactivation, are found in 20% to 30% of lung cancer cases.
Bae T, Kwak MK.
europepmc   +2 more sources

Structure-Based Identification of Kelch-like ECH-Associated Protein 1 as a Pharmacological Target of Electrophile-Containing Catechol-O-Methyltransferase Inhibitors. [PDF]

open access: yesACS Pharmacol Transl Sci
Entacapone and nitecapone are electrophile-containing catechol-O-methyltransferase (COMT) inhibitors that are used to treat Parkinson's disease in combination with L-DOPA. It is desirable to investigate whether they can covalently bind to cellular protein targets using their reactive electrophilic warheads.
Wang P   +11 more
europepmc   +3 more sources

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