Targeting the Nuclear Receptor-Binding SET Domain Family of Histone Lysine Methyltransferases for Cancer Therapy: Recent Progress and Perspectives

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dc.contributor.authorShrestha, Aarajanako
dc.contributor.authorKim, Nayeonko
dc.contributor.authorLee, Su-Jeongko
dc.contributor.authorJeon, Yong Hyunko
dc.contributor.authorSong, Ji-Joonko
dc.contributor.authorAn, Hongchanko
dc.contributor.authorCho, Sung Jinko
dc.contributor.authorKadayat, Tara Manko
dc.contributor.authorChin, Jungwookko
dc.date.accessioned2021-11-30T06:42:51Z-
dc.date.available2021-11-30T06:42:51Z-
dc.date.created2021-11-29-
dc.date.created2021-11-29-
dc.date.created2021-11-29-
dc.date.issued2021-10-
dc.identifier.citationJOURNAL OF MEDICINAL CHEMISTRY, v.64, no.20, pp.14913 - 14929-
dc.identifier.issn0022-2623-
dc.identifier.urihttp://hdl.handle.net/10203/289683-
dc.description.abstractNuclear receptor-binding SET domain (NSD) proteins are a class of histone lysine methyltransferases (HKMTases) that are amplified, mutated, translocated, or overexpressed in various types of cancers. Several campaigns to develop NSD inhibitors for cancer treatment have begun following recent advances in knowledge of NSD1, NSD2, and NSD3 structures and functions as well as the U.S. FDA approval of the first HKMTase inhibitor (tazemetostat, an EZH2 inhibitor) to treat follicular lymphoma and epithelioid sarcoma. This perspective highlights recent findings on the structures of catalytic su(var), enhancer-of-zeste, trithorax (SET) domains and other functional domains of NSD methyltransferases. In addition, recent progress and efforts to discover NSD-specific small molecule inhibitors against cancer-targeting catalytic SET domains, plant homeodomains, and proline-tryptophan-tryptophan-proline domains are summarized.-
dc.languageEnglish-
dc.publisherAMER CHEMICAL SOC-
dc.titleTargeting the Nuclear Receptor-Binding SET Domain Family of Histone Lysine Methyltransferases for Cancer Therapy: Recent Progress and Perspectives-
dc.typeArticle-
dc.identifier.wosid000713412900001-
dc.identifier.scopusid2-s2.0-85115611067-
dc.type.rimsART-
dc.citation.volume64-
dc.citation.issue20-
dc.citation.beginningpage14913-
dc.citation.endingpage14929-
dc.citation.publicationnameJOURNAL OF MEDICINAL CHEMISTRY-
dc.identifier.doi10.1021/acs.jmedchem.1c01116-
dc.embargo.liftdate9999-12-31-
dc.embargo.terms9999-12-31-
dc.contributor.localauthorSong, Ji-Joon-
dc.contributor.nonIdAuthorShrestha, Aarajana-
dc.contributor.nonIdAuthorKim, Nayeon-
dc.contributor.nonIdAuthorLee, Su-Jeong-
dc.contributor.nonIdAuthorJeon, Yong Hyun-
dc.contributor.nonIdAuthorAn, Hongchan-
dc.contributor.nonIdAuthorCho, Sung Jin-
dc.contributor.nonIdAuthorKadayat, Tara Man-
dc.contributor.nonIdAuthorChin, Jungwook-
dc.description.isOpenAccessN-
dc.type.journalArticleArticle-
dc.subject.keywordPlusSQUAMOUS-CELL CARCINOMA-
dc.subject.keywordPlusPROTEIN METHYLTRANSFERASES-
dc.subject.keywordPlusGENE-EXPRESSION-
dc.subject.keywordPlusPOOR-PROGNOSIS-
dc.subject.keywordPlusNSD FAMILY-
dc.subject.keywordPlusMMSET-
dc.subject.keywordPlusMETHYLATION-
dc.subject.keywordPlusWHSC1-
dc.subject.keywordPlusPROLIFERATION-
dc.subject.keywordPlusMETASTASIS-
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