Entry | Database: PDB / ID: 8vv8 |
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Title | Crystal Structure of EHMT2 bound to EZM8266 |
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Components | Histone-lysine N-methyltransferase EHMT2 |
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Keywords | GENE REGULATION / inhibitor / EHMT2 / G9a / EZM8266 |
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Function / homology | Function and homology information
phenotypic switching / histone H3K56 methyltransferase activity / neuron fate specification / [histone H3]-lysine9 N-methyltransferase / peptidyl-lysine dimethylation / histone H3K9 methyltransferase activity / histone H3K9me2 methyltransferase activity / histone H3K27 methyltransferase activity / synaptonemal complex assembly / negative regulation of autophagosome assembly ...phenotypic switching / histone H3K56 methyltransferase activity / neuron fate specification / [histone H3]-lysine9 N-methyltransferase / peptidyl-lysine dimethylation / histone H3K9 methyltransferase activity / histone H3K9me2 methyltransferase activity / histone H3K27 methyltransferase activity / synaptonemal complex assembly / negative regulation of autophagosome assembly / oocyte development / C2H2 zinc finger domain binding / protein-lysine N-methyltransferase activity / fertilization / cellular response to cocaine / organ growth / DNA methylation-dependent constitutive heterochromatin formation / negative regulation of gene expression via chromosomal CpG island methylation / Transcriptional Regulation by E2F6 / spermatid development / regulation of DNA replication / RNA Polymerase I Transcription Initiation / Transcriptional Regulation by VENTX / behavioral response to cocaine / Regulation of endogenous retroelements by the Human Silencing Hub (HUSH) complex / Transferases; Transferring one-carbon groups; Methyltransferases / epigenetic regulation of gene expression / cellular response to starvation / ERCC6 (CSB) and EHMT2 (G9a) positively regulate rRNA expression / transcription corepressor binding / RNA polymerase II transcription regulatory region sequence-specific DNA binding / Regulation of TP53 Activity through Methylation / promoter-specific chromatin binding / PKMTs methylate histone lysines / p53 binding / Senescence-Associated Secretory Phenotype (SASP) / nuclear speck / chromatin / negative regulation of transcription by RNA polymerase II / zinc ion binding / nucleoplasm / nucleusSimilarity search - Function Histone-lysine N-methyltransferase EHMT2 / Histone-lysine N-methyltransferase EHMT1/EHMT2 / : / Histone-lysine N-methyltransferase EHMT1/EHMT2, Cys-rich region / Pre-SET motif / Pre-SET domain / Pre-SET domain profile. / N-terminal to some SET domains / SET (Su(var)3-9, Enhancer-of-zeste, Trithorax) domain / SET domain ...Histone-lysine N-methyltransferase EHMT2 / Histone-lysine N-methyltransferase EHMT1/EHMT2 / : / Histone-lysine N-methyltransferase EHMT1/EHMT2, Cys-rich region / Pre-SET motif / Pre-SET domain / Pre-SET domain profile. / N-terminal to some SET domains / SET (Su(var)3-9, Enhancer-of-zeste, Trithorax) domain / SET domain / SET domain superfamily / SET domain profile. / SET domain / Ankyrin repeat / Ankyrin repeats (3 copies) / Ankyrin repeat profile. / Ankyrin repeat region circular profile. / ankyrin repeats / Ankyrin repeat / Ankyrin repeat-containing domain superfamilySimilarity search - Domain/homology |
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Biological species | Homo sapiens (human) |
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Method | X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution: 2 Å |
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Authors | Cocozaki, A. / Farrow, N.A. |
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Funding support | 1items Organization | Grant number | Country |
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Not funded | | |
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Citation | Journal: Mol.Cancer Ther. / Year: 2024 Title: Combining EHMT and PARP Inhibition: A Strategy to Diminish Therapy-Resistant Ovarian Cancer Tumor Growth while Stimulating Immune Activation. Authors: Nguyen, L.L. / Watson, Z.L. / Ortega, R. / Woodruff, E.R. / Jordan, K.R. / Iwanaga, R. / Yamamoto, T.M. / Bailey, C.A. / To, F. / Jeong, A.D. / Guntupalli, S.R. / Behbakht, K. / Gibaja, V. / ...Authors: Nguyen, L.L. / Watson, Z.L. / Ortega, R. / Woodruff, E.R. / Jordan, K.R. / Iwanaga, R. / Yamamoto, T.M. / Bailey, C.A. / To, F. / Jeong, A.D. / Guntupalli, S.R. / Behbakht, K. / Gibaja, V. / Arnoult, N. / Cocozaki, A. / Chuong, E.B. / Bitler, B.G. |
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History | Deposition | Jan 30, 2024 | Deposition site: RCSB / Processing site: RCSB |
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Revision 1.0 | Dec 11, 2024 | Provider: repository / Type: Initial release |
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Revision 1.1 | Jun 25, 2025 | Group: Database references / Category: citation / citation_author Item: _citation.country / _citation.journal_abbrev ..._citation.country / _citation.journal_abbrev / _citation.journal_id_CSD / _citation.journal_id_ISSN / _citation.page_first / _citation.page_last / _citation.pdbx_database_id_DOI / _citation.pdbx_database_id_PubMed / _citation.title / _citation.year |
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Revision 1.2 | Jul 23, 2025 | Group: Database references / Category: citation Item: _citation.journal_volume / _citation.page_first ..._citation.journal_volume / _citation.page_first / _citation.page_last / _citation.pdbx_database_id_PubMed |
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