Page last updated: 2024-08-07 20:42:20
Protein cereblon
A protein cereblon that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q96SW2]
Synonyms
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 | 4 (28.57) | 24.3611 |
| 2020's | 10 (71.43) | 2.80 |
Compounds (29)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| thalidomide | Homo sapiens (human) | EC50 | 0.0360 | 1 | 1 |
| pomalidomide | Homo sapiens (human) | EC50 | 0.0183 | 3 | 3 |
| lenalidomide | Homo sapiens (human) | EC50 | 0.0770 | 2 | 2 |
| dasatinib | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| ponatinib | Homo sapiens (human) | EC50 | 0.0106 | 1 | 1 |
Drugs with Other Measurements
SJPYT-195: A Designed Nuclear Receptor Degrader That Functions as a Molecular Glue Degrader of GSPT1.ACS medicinal chemistry letters, , Aug-11, Volume: 13, Issue:8, 2022
Physicochemistry of Cereblon Modulating Drugs Determines Pharmacokinetics and Disposition.ACS medicinal chemistry letters, , Nov-11, Volume: 12, Issue:11, 2021
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.ACS medicinal chemistry letters, , Jan-14, Volume: 12, Issue:1, 2021
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
A FRET-Based Assay for the Identification and Characterization of Cereblon Ligands.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.Leukemia, , Volume: 26, Issue:11, 2012
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.ACS medicinal chemistry letters, , Jan-14, Volume: 12, Issue:1, 2021
A FRET-Based Assay for the Identification and Characterization of Cereblon Ligands.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
SJPYT-195: A Designed Nuclear Receptor Degrader That Functions as a Molecular Glue Degrader of GSPT1.ACS medicinal chemistry letters, , Aug-11, Volume: 13, Issue:8, 2022
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.ACS medicinal chemistry letters, , Jan-14, Volume: 12, Issue:1, 2021
Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Physicochemistry of Cereblon Modulating Drugs Determines Pharmacokinetics and Disposition.ACS medicinal chemistry letters, , Nov-11, Volume: 12, Issue:11, 2021
A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 2018
Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.Leukemia, , Volume: 26, Issue:11, 2012
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.ACS medicinal chemistry letters, , Jan-14, Volume: 12, Issue:1, 2021
Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Physicochemistry of Cereblon Modulating Drugs Determines Pharmacokinetics and Disposition.ACS medicinal chemistry letters, , Nov-11, Volume: 12, Issue:11, 2021
Ligand Design for Cereblon Based Immunomodulatory Therapy.ACS medicinal chemistry letters, , Jun-11, Volume: 11, Issue:6, 2020
A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos.Journal of medicinal chemistry, , 01-25, Volume: 61, Issue:2, 2018
Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.Leukemia, , Volume: 26, Issue:11, 2012
Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects.Journal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| transmembrane transporter binding | molecular function | Binding to a transmembrane transporter, a protein or protein complex that enables the transfer of a substance, usually a specific substance or a group of related substances, from one side of a membrane to the other. [GOC:BHF, GOC:jl, PMID:33199372] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| 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] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| Cul4A-RING E3 ubiquitin ligase complex | cellular component | A ubiquitin ligase complex in which a cullin from the Cul4A subfamily and a RING domain protein form the catalytic core; substrate specificity is conferred by an adaptor protein. [PMID:15571813, PMID:15688063] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|
| protein ubiquitination | biological process | The process in which one or more ubiquitin groups are added to a protein. [GOC:ai] |
| positive regulation of Wnt signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of Wnt signal transduction. [GOC:dph, GOC:go_curators, GOC:tb] |
| negative regulation of protein-containing complex assembly | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of protein complex assembly. [GOC:mah] |
| positive regulation of protein-containing complex assembly | biological process | Any process that activates or increases the frequency, rate or extent of protein complex assembly. [GOC:mah] |
| negative regulation of monoatomic ion transmembrane transport | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the directed movement of ions from one side of a membrane to the other. [GOC:mah] |
| locomotory exploration behavior | biological process | The specific movement from place to place of an organism in response to a novel environment. [GOC:sart, PMID:17151232] |
| proteasome-mediated 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 ubiquitin, and mediated by the proteasome. [GOC:go_curators] |