Page last updated: 2024-08-07 22:39:58
Methylosome protein 50
A methylosome protein WDR77 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9BQA1]
Synonyms
MEP-50;
Androgen receptor cofactor p44;
WD repeat-containing protein 77;
p44/Mep50
Research
Bioassay Publications (8)
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 | 5 (62.50) | 24.3611 |
2020's | 3 (37.50) | 2.80 |
Compounds (5)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 28, Issue:23-24, 2018
Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 28, Issue:9, 2018
Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction.Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders.Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 28, Issue:9, 2018
Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 28, Issue:23-24, 2018
Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.ACS medicinal chemistry letters, , Feb-11, Volume: 7, Issue:2, 2016
Enables
This protein enables 4 target(s):
Target | Category | Definition |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
methyl-CpG binding | molecular function | Binding to a methylated cytosine/guanine dinucleotide. [GOC:jl, PMID:11746232] |
nuclear receptor coactivator activity | molecular function | A transcription coactivator activity that activates or increases the transcription of specific gene sets via binding to a DNA-bound nuclear receptor, either on its own or as part of a complex. Coactivators often act by altering chromatin structure and modifications. For example, one class of transcription coregulators modifies chromatin structure through covalent modification of histones. A second class remodels the conformation of chromatin in an ATP-dependent fashion. A third class modulates interactions of DNA-bound DNA-binding transcription factors with other transcription coregulators. A fourth class of coactivator activity is the bridging of a DNA-binding transcription factor to the general (basal) transcription machinery. The Mediator complex, which bridges sequence-specific DNA binding transcription factors and RNA polymerase, is also a transcription coactivator. [GOC:dph, GOC:tb] |
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] |
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] |
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] |
Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [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] |
Part Of
This protein is part of 2 target(s):
Target | Category | Definition |
methylosome | cellular component | A large (20 S) protein complex that possesses protein arginine methyltransferase activity and modifies specific arginines to dimethylarginines in the arginine- and glycine-rich domains of several spliceosomal Sm proteins, thereby targeting these proteins to the survival of motor neurons (SMN) complex for assembly into small nuclear ribonucleoprotein (snRNP) core particles. Proteins found in the methylosome include the methyltransferase JBP1 (PRMT5), pICln (CLNS1A), MEP50 (WDR77), and unmethylated forms of SM proteins that have RG domains. [PMID:11713266, PMID:11756452] |
Cul4B-RING E3 ubiquitin ligase complex | cellular component | A ubiquitin ligase complex in which a cullin from the Cul4B subfamily and a RING domain protein form the catalytic core; substrate specificity is conferred by unknown subunits. [PMID:15571813, PMID:15688063] |
Involved In
This protein is involved in 11 target(s):
Target | Category | Definition |
protein polyubiquitination | biological process | Addition of multiple ubiquitin groups to a protein, forming a ubiquitin chain. [ISBN:0815316194] |
spliceosomal snRNP assembly | biological process | The aggregation, arrangement and bonding together of one or more snRNA and multiple protein components to form a ribonucleoprotein complex that is involved in formation of the spliceosome. [GOC:krc, GOC:mah, ISBN:0879695897] |
regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
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] |
positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
positive regulation of mRNA splicing, via spliceosome | biological process | Any process that activates or increases the rate or extent of mRNA splicing via a spliceosomal mechanism. [GOC:jid] |
secretory columnal luminar epithelial cell differentiation involved in prostate glandular acinus development | biological process | The process in which a relatively unspecialized epithelial cell acquires specialized features of a secretory columnal luminar epithelial cell of the prostate. [GOC:dph, PMID:18977204] |
epithelial cell proliferation involved in prostate gland development | biological process | The multiplication or reproduction of epithelial cells, resulting in the expansion of a cell population that contributes to the progression of the prostate gland over time. [GOC:dph] |
negative regulation of epithelial cell proliferation involved in prostate gland development | biological process | Any process that decreases the rate, frequency or extent of epithelial cell proliferation that contributes to the progression of the prostate gland over time. [GOC:dph] |
oocyte axis specification | biological process | The establishment, maintenance and elaboration of an axis in the oocyte. An example of this is found in Drosophila melanogaster. [GOC:mtg_sensu, ISBN:0879694238] |