Proteins > Kelch-like ECH-associated protein 1
Page last updated: 2024-08-07 18:41:46
Kelch-like ECH-associated protein 1
A kelch-like ECH-associated protein 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q14145]
Synonyms
Cytosolic inhibitor of Nrf2;
INrf2;
Kelch-like protein 19
Research
Bioassay Publications (14)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 8 (57.14) | 24.3611 |
| 2020's | 6 (42.86) | 2.80 |
Compounds (14)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 3-phenylpropionic acid | Homo sapiens (human) | Kd | 3,200.0000 | 1 | 1 |
| sulforaphane | Homo sapiens (human) | EC50 | 0.8700 | 1 | 1 |
| sulforaphane | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| 1-naphthylamine | Homo sapiens (human) | Kd | 1,200.0000 | 1 | 1 |
| 3-morpholinopropylamine | Homo sapiens (human) | Kd | 300.0000 | 1 | 1 |
| 2,4'-bisphenol f | Homo sapiens (human) | Kd | 1,000.0000 | 1 | 1 |
| hei 712 | Homo sapiens (human) | Kd | 1,800.0000 | 1 | 1 |
| 2-(5-Chlorobenzo[b]thiophen-3-yl)acetic acid | Homo sapiens (human) | Kd | 840.0000 | 1 | 1 |
| dimethyl fumarate | Homo sapiens (human) | EC50 | 5.1100 | 1 | 1 |
| umi-77 | Homo sapiens (human) | Kd | 14.7000 | 1 | 1 |
| (1S,2R)-2-[[(1S)-1-[(1,3-dioxo-2-isoindolyl)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-oxomethyl]-1-cyclohexanecarboxylic acid | Homo sapiens (human) | EC50 | 14.5750 | 4 | 4 |
| (1S,2R)-2-[[(1S)-1-[(1,3-dioxo-2-isoindolyl)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]-oxomethyl]-1-cyclohexanecarboxylic acid | Homo sapiens (human) | Kd | 1.7667 | 3 | 3 |
| nk 252 | Homo sapiens (human) | EC50 | 800.0000 | 1 | 1 |
| nk 252 | Homo sapiens (human) | Kd | 452.0000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nk 252 | Homo sapiens (human) | EC2 | 1.3600 | 1 | 1 |
Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
A novel chalcone derivative as Nrf2 activator attenuates learning and memory impairment in a scopolamine-induced mouse model.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo.Bioorganic & medicinal chemistry, , 02-15, Volume: 27, Issue:4, 2019
Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
Small molecules inhibiting Keap1-Nrf2 protein-protein interactions: a novel approach to activate Nrf2 function.MedChemComm, , Feb-01, Volume: 8, Issue:2, 2017
Design, Synthesis, and Evaluation of Triazole Derivatives That Induce Nrf2 Dependent Gene Products and Inhibit the Keap1-Nrf2 Protein-Protein Interaction.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Structure-Activity and Structure-Property Relationship and Exploratory in Vivo Evaluation of the Nanomolar Keap1-Nrf2 Protein-Protein Interaction Inhibitor.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| RNA polymerase II-specific DNA-binding transcription factor binding | molecular function | Binding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw] |
| disordered domain specific binding | molecular function | Binding to a disordered domain of a protein. [GOC:gg, PMID:11746698] |
| ubiquitin-like ligase-substrate adaptor activity | molecular function | The binding activity of a molecule that brings together a ubiquitin-like ligase (including ubiquitin ligase and UFM1 ligase) and its substrate. Usually mediated by F-box BTB/POZ domain proteins. [PMID:24658274] |
| transcription factor binding | molecular function | Binding to a transcription factor, a protein required to initiate or regulate transcription. [ISBN:0198506732] |
Located In
This protein is located in 8 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| actin filament | cellular component | A filamentous structure formed of a two-stranded helical polymer of the protein actin and associated proteins. Actin filaments are a major component of the contractile apparatus of skeletal muscle and the microfilaments of the cytoskeleton of eukaryotic cells. The filaments, comprising polymerized globular actin molecules, appear as flexible structures with a diameter of 5-9 nm. They are organized into a variety of linear bundles, two-dimensional networks, and three dimensional gels. In the cytoskeleton they are most highly concentrated in the cortex of the cell just beneath the plasma membrane. [GOC:mah, ISBN:0198506732, PMID:10666339] |
| inclusion body | cellular component | A discrete intracellular part formed of aggregated molecules such as proteins or other biopolymers. [GOC:mah, PMID:11121744] |
| midbody | cellular component | A thin cytoplasmic bridge formed between daughter cells at the end of cytokinesis. The midbody forms where the contractile ring constricts, and may persist for some time before finally breaking to complete cytokinesis. [ISBN:0815316194] |
| centriolar satellite | cellular component | A small (70-100 nm) cytoplasmic granule that contains a number of centrosomal proteins; centriolar satellites traffic toward microtubule minus ends and are enriched near the centrosome. [GOC:BHF, PMID:10579718, PMID:12403812] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| Cul3-RING ubiquitin ligase complex | cellular component | A ubiquitin ligase complex in which a cullin from the Cul3 subfamily and a RING domain protein form the catalytic core; substrate specificity is conferred by a BTB-domain-containing protein. [PMID:15571813, PMID:15688063] |
Involved In
This protein is involved in 10 target(s):
| Target | Category | Definition |
|---|
| in utero embryonic development | biological process | The process whose specific outcome is the progression of the embryo in the uterus over time, from formation of the zygote in the oviduct, to birth. An example of this process is found in Mus musculus. [GOC:go_curators, GOC:mtg_sensu] |
| ubiquitin-dependent protein catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of a protein or peptide by hydrolysis of its peptide bonds, initiated by the covalent attachment of a ubiquitin group, or multiple ubiquitin groups, to the protein. [GOC:go_curators] |
| regulation of autophagy | biological process | Any process that modulates the frequency, rate or extent of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| protein ubiquitination | biological process | The process in which one or more ubiquitin groups are added to a protein. [GOC:ai] |
| positive regulation of proteasomal ubiquitin-dependent protein catabolic process | biological process | Any process that activates or increases the frequency, rate or extent of the breakdown of a protein or peptide by hydrolysis of its peptide bonds, initiated by the covalent attachment of ubiquitin, and mediated by the proteasome. [GOC:mah] |
| cellular response to oxidative stress | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of oxidative stress, a state often resulting from exposure to high levels of reactive oxygen species, e.g. superoxide anions, hydrogen peroxide (H2O2), and hydroxyl radicals. [GOC:mah] |
| negative regulation of DNA-binding transcription factor activity | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the activity of a transcription factor, any factor involved in the initiation or regulation of transcription. [GOC:jl] |
| regulation of epidermal cell differentiation | biological process | Any process that modulates the frequency, rate or extent of epidermal cell differentiation. [GOC:go_curators] |
| cellular response to interleukin-4 | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an interleukin-4 stimulus. [GOC:mah] |
| negative regulation of response to oxidative stress | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of response to oxidative stress. [GO_REF:0000058, GOC:kmv, GOC:TermGenie, PMID:16899554] |