{"id":"https://openalex.org/W3135619807","doi":"https://doi.org/10.1016/j.bmcl.2021.127908","title":"A novel class of selective non-nucleoside inhibitors of human DNA methyltransferase 3A","display_name":"A novel class of selective non-nucleoside inhibitors of human DNA methyltransferase 3A","publication_year":2021,"publication_date":"2021-03-09","ids":{"openalex":"https://openalex.org/W3135619807","doi":"https://doi.org/10.1016/j.bmcl.2021.127908","mag":"3135619807","pmid":"https://pubmed.ncbi.nlm.nih.gov/33705897"},"language":"en","primary_location":{"id":"doi:10.1016/j.bmcl.2021.127908","doi":"https://doi.org/10.1016/j.bmcl.2021.127908","is_oa":false,"landing_page_url":"https://doi.org/10.1016/j.bmcl.2021.127908","pdf_url":null,"source":{"id":"https://openalex.org/S30970080","display_name":"Bioorganic & Medicinal Chemistry Letters","issn_l":"0960-894X","issn":["0960-894X","1464-3405"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-b","jufo-1","ki-jl-1","medline","norway-1","poland-70","russia-white-list-2","vabb-shw"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Bioorganic &amp; Medicinal Chemistry Letters","raw_type":"journal-article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["crossref","pubmed"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5080997479","display_name":"Sunzeyu Huang","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I154570441","display_name":"University of California, Santa Barbara","ror":"https://ror.org/02t274463","country_code":"US","type":"education","lineage":["https://openalex.org/I154570441"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Sunzeyu Huang","raw_affiliation_strings":["The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA","institution_ids":["https://openalex.org/I154570441"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5057342984","display_name":"Nathaniel J. Stillson","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I154570441","display_name":"University of California, Santa Barbara","ror":"https://ror.org/02t274463","country_code":"US","type":"education","lineage":["https://openalex.org/I154570441"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Nathaniel J. Stillson","raw_affiliation_strings":["The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA","institution_ids":["https://openalex.org/I154570441"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5040667506","display_name":"Jonathan E. Sandoval","orcid":"https://orcid.org/0000-0003-1986-0804","observed_orcids":["https://orcid.org/0000-0003-1986-0804"]},"institutions":[{"id":"https://openalex.org/I154570441","display_name":"University of California, Santa Barbara","ror":"https://ror.org/02t274463","country_code":"US","type":"education","lineage":["https://openalex.org/I154570441"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Jonathan E. Sandoval","raw_affiliation_strings":["The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA; Molecular, Cellular and Developmental Biology, University of California, Santa Barbara 93106-9510, USA","Molecular, Cellular and Developmental Biology, University of California, Santa Barbara 93106-9510, USA","The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA"],"raw_orcid":"https://orcid.org/0000-0003-1986-0804","affiliations":[{"raw_affiliation_string":"The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA; Molecular, Cellular and Developmental Biology, University of California, Santa Barbara 93106-9510, USA","institution_ids":["https://openalex.org/I154570441"]},{"raw_affiliation_string":"Molecular, Cellular and Developmental Biology, University of California, Santa Barbara 93106-9510, USA","institution_ids":["https://openalex.org/I154570441"]},{"raw_affiliation_string":"The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA","institution_ids":["https://openalex.org/I154570441"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5080253864","display_name":"Chitoh Yung","orcid":"https://orcid.org/0000-0001-8138-0647","observed_orcids":["https://orcid.org/0000-0001-8138-0647"]},"institutions":[{"id":"https://openalex.org/I154570441","display_name":"University of California, Santa Barbara","ror":"https://ror.org/02t274463","country_code":"US","type":"education","lineage":["https://openalex.org/I154570441"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Chitoh Yung","raw_affiliation_strings":["The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA","institution_ids":["https://openalex.org/I154570441"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5064531954","display_name":"Norbert O. Reich","orcid":"https://orcid.org/0000-0001-6032-2704","observed_orcids":["https://orcid.org/0000-0001-6032-2704"]},"institutions":[{"id":"https://openalex.org/I154570441","display_name":"University of California, Santa Barbara","ror":"https://ror.org/02t274463","country_code":"US","type":"education","lineage":["https://openalex.org/I154570441"]}],"countries":["US"],"is_corresponding":true,"raw_author_name":"Norbert O. Reich","raw_affiliation_strings":["The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA. Electronic address: reich@chem.ucsb.edu","The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA. Electronic address: reich@chem.ucsb.edu","institution_ids":["https://openalex.org/I154570441"]},{"raw_affiliation_string":"The Department of Chemistry and Biochemistry, University of California, Santa Barbara 93106-9510, USA","institution_ids":["https://openalex.org/I154570441"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":["https://openalex.org/A5064531954"],"corresponding_institution_ids":["https://openalex.org/I154570441"],"apc_list":{"value":3000,"currency":"USD","value_usd":3000},"apc_paid":null,"fwci":1.1212,"has_fulltext":false,"cited_by_count":24,"citation_normalized_percentile":{"value":0.75568187,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":87,"max":98},"biblio":{"volume":"40","issue":null,"first_page":"127908","last_page":"127908"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10269","display_name":"Epigenetics and DNA Methylation","score":0.9229000210762024,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T10269","display_name":"Epigenetics and DNA Methylation","score":0.9229000210762024,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T12827","display_name":"Biochemical and Molecular Research","score":0.019099999219179153,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.011900000274181366,"subfield":{"id":"https://openalex.org/subfields/1605","display_name":"Organic Chemistry"},"field":{"id":"https://openalex.org/fields/16","display_name":"Chemistry"},"domain":{"id":"https://openalex.org/domains/3","display_name":"Physical Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/dnmt3a","display_name":"DNMT3A","score":0.8889999985694885},{"id":"https://openalex.org/keywords/pyrazolones","display_name":"pyrazolone derivatives","score":0.8349999785423279},{"id":"https://openalex.org/keywords/pyridazines","display_name":"pyridazines","score":0.9909999966621399},{"id":"https://openalex.org/keywords/allosteric-inhibition","display_name":"allosteric inhibition","score":0.9620000123977661},{"id":"https://openalex.org/keywords/uncompetitive-inhibition","display_name":"uncompetitive inhibition","score":0.8230000138282776},{"id":"https://openalex.org/keywords/mixed-inhibition","display_name":"mixed-type inhibition","score":0.8159999847412109},{"id":"https://openalex.org/keywords/s-adenosylmethionine","display_name":"S-adenosylmethionine","score":0.8180000185966492},{"id":"https://openalex.org/keywords/de-novo-methylation","display_name":"de novo methylation","score":0.9620000123977661},{"id":"https://openalex.org/keywords/dna-methylation-maintenance","display_name":"DNA methylation maintenance","score":0.8100000023841858},{"id":"https://openalex.org/keywords/anticancer-drug-discovery","display_name":"anticancer drug discovery","score":0.5699999928474426}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.8336528539657593},{"id":"https://openalex.org/C91965660","wikidata":"https://www.wikidata.org/wiki/Q415875","display_name":"Methyltransferase","level":4,"score":0.6157338619232178},{"id":"https://openalex.org/C2779979206","wikidata":"https://www.wikidata.org/wiki/Q1154602","display_name":"DNA methyltransferase","level":5,"score":0.5880976319313049},{"id":"https://openalex.org/C175211621","wikidata":"https://www.wikidata.org/wiki/Q14907998","display_name":"DNMT1","level":5,"score":0.5654735565185547},{"id":"https://openalex.org/C2780235182","wikidata":"https://www.wikidata.org/wiki/Q1181878","display_name":"Decitabine","level":5,"score":0.5414801239967346},{"id":"https://openalex.org/C166342909","wikidata":"https://www.wikidata.org/wiki/Q845326","display_name":"Allosteric regulation","level":3,"score":0.5395009517669678},{"id":"https://openalex.org/C552990157","wikidata":"https://www.wikidata.org/wiki/Q7430","display_name":"DNA","level":2,"score":0.5335977673530579},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.4924122095108032},{"id":"https://openalex.org/C190727270","wikidata":"https://www.wikidata.org/wiki/Q874745","display_name":"DNA methylation","level":4,"score":0.48786306381225586},{"id":"https://openalex.org/C161624437","wikidata":"https://www.wikidata.org/wiki/Q1988322","display_name":"Small molecule","level":2,"score":0.4685301184654236},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.4606698751449585},{"id":"https://openalex.org/C41183919","wikidata":"https://www.wikidata.org/wiki/Q423026","display_name":"Active site","level":3,"score":0.44154930114746094},{"id":"https://openalex.org/C2756471","wikidata":"https://www.wikidata.org/wiki/Q206286","display_name":"DNA polymerase","level":3,"score":0.43635204434394836},{"id":"https://openalex.org/C33288867","wikidata":"https://www.wikidata.org/wiki/Q518328","display_name":"Methylation","level":3,"score":0.32660984992980957},{"id":"https://openalex.org/C150194340","wikidata":"https://www.wikidata.org/wiki/Q26972","display_name":"Gene expression","level":3,"score":0.13120073080062866},{"id":"https://openalex.org/C104317684","wikidata":"https://www.wikidata.org/wiki/Q7187","display_name":"Gene","level":2,"score":0.1301417350769043}],"mesh":[{"descriptor_ui":"D000077209","descriptor_name":"Decitabine","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D000090205","descriptor_name":"DNA Methyltransferase 3A","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001374","descriptor_name":"Azacitidine","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D004247","descriptor_name":"DNA","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D004248","descriptor_name":"DNA (Cytosine-5-)-Methyltransferases","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":true},{"descriptor_ui":"D004353","descriptor_name":"Drug Evaluation, Preclinical","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011485","descriptor_name":"Protein Binding","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011724","descriptor_name":"Pyridazines","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D019175","descriptor_name":"DNA Methylation","qualifier_ui":"Q000187","qualifier_name":"drug effects","is_major_topic":false},{"descriptor_ui":"D020134","descriptor_name":"Catalytic Domain","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D047069","descriptor_name":"Pyrazolones","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D054852","descriptor_name":"Small Molecule Libraries","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D054852","descriptor_name":"Small Molecule Libraries","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true}],"locations_count":3,"locations":[{"id":"doi:10.1016/j.bmcl.2021.127908","doi":"https://doi.org/10.1016/j.bmcl.2021.127908","is_oa":false,"landing_page_url":"https://doi.org/10.1016/j.bmcl.2021.127908","pdf_url":null,"source":{"id":"https://openalex.org/S30970080","display_name":"Bioorganic & Medicinal Chemistry Letters","issn_l":"0960-894X","issn":["0960-894X","1464-3405"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-b","jufo-1","ki-jl-1","medline","norway-1","poland-70","russia-white-list-2","vabb-shw"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Bioorganic &amp; Medicinal Chemistry Letters","raw_type":"journal-article"},{"id":"pmid:33705897","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/33705897","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Bioorganic & medicinal chemistry letters","raw_type":"Journal Article"},{"id":"pmh:oai:escholarship.org:ark:/13030/qt6p9393kq","doi":null,"is_oa":false,"landing_page_url":"https://escholarship.org/uc/item/6p9393kq","pdf_url":null,"source":{"id":"https://openalex.org/S4306400115","display_name":"eScholarship (California Digital Library)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I2801248553","host_organization_name":"California Digital Library","host_organization_lineage":["https://openalex.org/I2801248553"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"","raw_type":"etd"}],"best_oa_location":null,"sustainable_development_goals":[{"display_name":"Good health and well-being","score":0.428600013256073,"id":"https://metadata.un.org/sdg/3"}],"study_designs":[],"awards":[{"id":"https://openalex.org/G4426335512","display_name":"Mechanistic investigation of processive and distributive DNA modification","funder_award_id":"1808775","funder_id":"https://openalex.org/F4320306076","funder_display_name":"National Science Foundation"}],"funders":[{"id":"https://openalex.org/F4320306076","display_name":"National Science Foundation","ror":"https://ror.org/021nxhr62"}],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":51,"referenced_works":["https://openalex.org/W23768266","https://openalex.org/W1525055187","https://openalex.org/W1529120072","https://openalex.org/W1577875429","https://openalex.org/W1585338920","https://openalex.org/W1982356313","https://openalex.org/W2002788005","https://openalex.org/W2006040339","https://openalex.org/W2006500779","https://openalex.org/W2008563981","https://openalex.org/W2017394727","https://openalex.org/W2025193307","https://openalex.org/W2041686632","https://openalex.org/W2046241907","https://openalex.org/W2048389974","https://openalex.org/W2053217245","https://openalex.org/W2055728251","https://openalex.org/W2060446375","https://openalex.org/W2062671889","https://openalex.org/W2067501960","https://openalex.org/W2072523970","https://openalex.org/W2074929227","https://openalex.org/W2080324830","https://openalex.org/W2081152501","https://openalex.org/W2083787690","https://openalex.org/W2094815969","https://openalex.org/W2100645337","https://openalex.org/W2108664872","https://openalex.org/W2114599216","https://openalex.org/W2122116522","https://openalex.org/W2154249927","https://openalex.org/W2283716387","https://openalex.org/W2308056733","https://openalex.org/W2325267338","https://openalex.org/W2515644879","https://openalex.org/W2560908657","https://openalex.org/W2737953029","https://openalex.org/W2766704091","https://openalex.org/W2786755330","https://openalex.org/W2802220743","https://openalex.org/W2915374540","https://openalex.org/W2930632179","https://openalex.org/W2939052792","https://openalex.org/W2944244575","https://openalex.org/W2972076780","https://openalex.org/W2980874287","https://openalex.org/W2981459585","https://openalex.org/W2991108194","https://openalex.org/W2994934962","https://openalex.org/W3013096229","https://openalex.org/W4319291164"],"related_works":["https://openalex.org/W4394568520","https://openalex.org/W4291595134","https://openalex.org/W2757735000","https://openalex.org/W2554232244","https://openalex.org/W2767185040","https://openalex.org/W2301017911","https://openalex.org/W775539882","https://openalex.org/W4399584564","https://openalex.org/W2083787690","https://openalex.org/W2326246873"],"abstract_inverted_index":null,"counts_by_year":[{"year":2026,"cited_by_count":3},{"year":2025,"cited_by_count":5},{"year":2024,"cited_by_count":7},{"year":2023,"cited_by_count":3},{"year":2022,"cited_by_count":5},{"year":2021,"cited_by_count":1}],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2021-03-15T00:00:00"}
