Results 31 to 40 of about 45,202 (305)

Keap1–Nrf2 signalling in pancreatic cancer [PDF]

The International Journal of Biochemistry & Cell Biology, 2015
Transcription factor NF-E2 p45-related factor 2 (Nrf2, also called Nfe2l2), a master regulator of redox homeostasis, and its dominant negative regulator, Kelch-like ECH-associated protein 1 (Keap1), together tightly control the expression of numerous detoxifying and antioxidant genes.
Alastair J, Hayes, Christos, Skouras, Beate, Haugk, Richard M, Charnley   +3 more
openaire   +2 more sources

Structural Characterization of KEAP1 R415K to Guide the Design of KEAP1‐Nrf2 Peptide Inhibitors

The FASEB Journal, 2021
Oxidative stress can cause extensive damage to DNA, proteins, and lipids. Thus, long‐term oxidative stress has been linked to many diseases including cancer and Alzheimer's disease. The highly‐charged binding interface between regulatory protein Kelch‐like ECH‐associated protein 1 (KEAP1) and transcription factor nuclear erythroid factor 2‐like 2 (Nrf2)
Gwendolyn Pyeatt, Samantha Muellers, Adrian Whitty, Karen Allen   +3 more
openaire   +1 more source

Mutant p53–Nrf2 axis regulates the proteasome machinery in cancer

Molecular & Cellular Oncology, 2017
The proteasome machinery is a common target of gain-of-function p53 missense mutants. Upregulation of the proteasome fosters chemoresistance to proteasome inhibitors.
Kamil Lisek, Dawid Walerych, Giannino Del Sal   +2 more
doaj   +1 more source

Modification of Keap1 Cysteine Residues by Sulforaphane [PDF]

Chemical Research in Toxicology, 2011
Activation of the transcription factor NF-E2-related factor-2 (Nrf2) through modification of Kelch-like ECH-associated protein 1 (Keap1) cysteines, leading to up-regulation of the antioxidant response element (ARE), is an important mechanism of cellular defense against reactive oxygen species and xenobiotic electrophiles.
Chenqi, Hu, Aimee L, Eggler, Andrew D, Mesecar, Richard B, van Breemen   +3 more
openaire   +2 more sources

Advances in developing noncovalent small molecules targeting Keap1 [PDF]

, 2023
Kelch-like ECH-associated protein 1 (Keap1) is a drug target for diseases involving oxidative stress and inflammation. There are three covalent Keap1-binding drugs on the market, but noncovalent compounds that inhibit the interaction between Keap1 and ...
Qin, Yuting, Barraja, Paola, Cadot, Marie Elodie Hélène, Marilia Barreca, Yuting Qin, Marie Elodie Hélène Cadot, Paola Barraja, Hélène Cadot, Marie Elodie, Bach, Anders, Anders Bach, Barreca, Marilia   +10 more
core   +1 more source

The KEAP1-NRF2 System and Esophageal Cancer

Cancers, 2022
NRF2 (nuclear factor erythroid 2-related factor 2) is a transcription factor that regulates the expression of many cytoprotective genes. NRF2 activation is mainly regulated by KEAP1 (kelch-like ECH-associated protein 1) through ubiquitination and proteasome degradation.
Wataru Hirose, Hiroyuki Oshikiri, Keiko Taguchi, Masayuki Yamamoto   +3 more
openaire   +2 more sources

PGAM5 expression levels in heart failure and protection ROS-induced oxidative stress and ferroptosis by Keap1/Nrf2

Clinical and Experimental Hypertension, 2023
Objectives As a common and frequently occurring disease, heart failure has been paid more and more attention, but the mechanism of its occurrence and development is still unclear.
Shuangfei Li, Ping Wen, Dayong Zhang, Decai Li, Qidong Gao, Hong Liu, Yunfeng Di   +6 more
doaj   +1 more source

Chemical tuning enhances both potency toward Nrf2 and in vitro therapeutic index of triterpenoids [PDF]

, 2014
The transcription factor Nrf2 protects against a number of experimental pathologies, and is a promising therapeutic target. The clinical investigation of a potent Nrf2-inducing agent, the triterpenoid (TP) bardoxolone methyl (BARD), was recently halted ...
Lister, Adam, Shelton, Luke M., Kratschmar, Denise V., Copple, Ian M., Park, B. Kevin, Goldring, Christopher E., Honda, Tadashi, Odermatt, Alex, Walsh, Joanne, Dinkova-Kostova, Albena T.; id_orcid, Dinkova-Kostova, Albena T., Kratschmar DV, Walsh J, Park BK, Dinkova-Kostova AT, Odermatt A, Goldring CE, Copple IM, Lister A, Shelton LM, Honda T   +20 more
core   +1 more source

Targeting Nrf2 signaling in dry eye [PDF]

International Journal of Ophthalmology
Dry eye, the most common ocular surface disease, can cause ocular surface tissue damage and discomfort symptoms and seriously affect people's quality of life. The etiology of dry eye is diverse, and its pathogenesis is complex.
Yu-Nuo Zhang, Wei-Jie Ouyang, Jiao-Yue Hu, Zu-Guo Liu   +3 more
doaj   +1 more source

Nrf2 impacts cellular bioenergetics by controlling substrate availability for mitochondrial respiration [PDF]

, 2013
Transcription factor Nrf2 and its repressor Keap1 regulate a network of cytoprotective genes involving more than 1% of the genome, their best known targets being drug-metabolizing and antioxidant genes.
Iain Hargreaves, Land, John M., Kira M. Holmström, Andrey Y. Abramov, Chalasani, A, Annapurna Chalasani, Holmstrom, KM, Masayuki Yamamoto, Baird, Liam, Baird, L, John M. Land, Yamamoto, Masayuki, Lee Stanyer, Land, JM, Dinkova-Kostova, AT, Holmström, Kira M., Liam Baird, Albena T. Dinkova-Kostova, Ying Zhang, Abramov, Andrey Y., Zhang, Y, Hargreaves, Iain, Chalasani, Annapurna, Abramov, AY, Stanyer, L, Hargreaves, IP, Yamamoto, M, Zhang, Ying, Stanyer, Lee, Dinkova-Kostova, Albena T.; id_orcid   +29 more
core   +1 more source