{"id":"https://openalex.org/W4210713879","doi":"https://doi.org/10.1021/acs.jcim.1c01100","title":"Identification, Synthesis, and Biological Evaluations of Potent Inhibitors Targeting Type I Protein Arginine Methyltransferases","display_name":"Identification, Synthesis, and Biological Evaluations of Potent Inhibitors Targeting Type I Protein Arginine Methyltransferases","publication_year":2022,"publication_date":"2022-01-31","ids":{"openalex":"https://openalex.org/W4210713879","doi":"https://doi.org/10.1021/acs.jcim.1c01100","pmid":"https://pubmed.ncbi.nlm.nih.gov/35098713"},"language":"en","primary_location":{"id":"doi:10.1021/acs.jcim.1c01100","is_oa":false,"landing_page_url":"https://doi.org/10.1021/acs.jcim.1c01100","pdf_url":null,"source":{"id":"https://openalex.org/S167262187","display_name":"Journal of Chemical Information and Modeling","issn_l":"1549-9596","issn":["1549-9596","1549-960X"],"is_oa":false,"is_in_doaj":false,"is_core":true,"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Chemical Information and Modeling","raw_type":"journal-article"},"type":"article","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/A5100785853","display_name":"Xiao Li","orcid":"https://orcid.org/0000-0002-2255-4499"},"institutions":[{"id":"https://openalex.org/I4210112820","display_name":"Shanghai Institute of Materia Medica","ror":"https://ror.org/022syn853","country_code":"CN","type":"facility","lineage":["https://openalex.org/I19820366","https://openalex.org/I4210112820"]},{"id":"https://openalex.org/I19820366","display_name":"Chinese Academy of Sciences","ror":"https://ror.org/034t30j35","country_code":"CN","type":"funder","lineage":["https://openalex.org/I19820366"]},{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]},{"id":"https://openalex.org/I4210165038","display_name":"University of Chinese Academy of Sciences","ror":"https://ror.org/05qbk4x57","country_code":"CN","type":"education","lineage":["https://openalex.org/I19820366","https://openalex.org/I4210165038"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Xiao Li","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","The Center for Chemical Biology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China","University of Chinese Academy of Sciences, 19 Yuquan Road, Beijing 100049, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]},{"raw_affiliation_string":"The Center for Chemical Biology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China","institution_ids":["https://openalex.org/I4210112820","https://openalex.org/I19820366"]},{"raw_affiliation_string":"University of Chinese Academy of Sciences, 19 Yuquan Road, Beijing 100049, China","institution_ids":["https://openalex.org/I4210165038"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100661412","display_name":"Lun Zhang","orcid":"https://orcid.org/0000-0002-0928-7568"},"institutions":[{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Lun Zhang","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100735421","display_name":"Jing Xu","orcid":"https://orcid.org/0009-0002-5968-1704"},"institutions":[{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Jing Xu","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100731332","display_name":"Chenyu Liu","orcid":"https://orcid.org/0000-0001-5048-948X"},"institutions":[{"id":"https://openalex.org/I66867065","display_name":"East China Normal University","ror":"https://ror.org/02n96ep67","country_code":"CN","type":"education","lineage":["https://openalex.org/I66867065"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Chenyu Liu","raw_affiliation_strings":["Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, China"],"affiliations":[{"raw_affiliation_string":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, China","institution_ids":["https://openalex.org/I66867065"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100685472","display_name":"Xiaojian Zhang","orcid":"https://orcid.org/0000-0002-3980-8563"},"institutions":[{"id":"https://openalex.org/I66867065","display_name":"East China Normal University","ror":"https://ror.org/02n96ep67","country_code":"CN","type":"education","lineage":["https://openalex.org/I66867065"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Xiaojian Zhang","raw_affiliation_strings":["Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, China"],"affiliations":[{"raw_affiliation_string":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, China","institution_ids":["https://openalex.org/I66867065"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5017406218","display_name":"Amr Abbas Abdelmoneim","orcid":null},"institutions":[{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Amr Abbas Abdelmoneim","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100401743","display_name":"Qian Zhang","orcid":"https://orcid.org/0000-0003-4928-3366"},"institutions":[{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Qian Zhang","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5050389858","display_name":"Jiaqi Ke","orcid":null},"institutions":[{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Jiaqi Ke","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100657998","display_name":"Yingnan Zhang","orcid":"https://orcid.org/0000-0002-9368-8814"},"institutions":[{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Yingnan Zhang","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100435978","display_name":"Lei Wang","orcid":"https://orcid.org/0000-0002-6340-6222"},"institutions":[{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Lei Wang","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5101488857","display_name":"Fan Yang","orcid":"https://orcid.org/0000-0002-0411-7391"},"institutions":[{"id":"https://openalex.org/I66867065","display_name":"East China Normal University","ror":"https://ror.org/02n96ep67","country_code":"CN","type":"education","lineage":["https://openalex.org/I66867065"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Fan Yang","raw_affiliation_strings":["Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, China"],"affiliations":[{"raw_affiliation_string":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, China","institution_ids":["https://openalex.org/I66867065"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5024637740","display_name":"Cheng Luo","orcid":"https://orcid.org/0000-0003-3864-8382"},"institutions":[{"id":"https://openalex.org/I114539943","display_name":"Zhejiang Chinese Medical University","ror":"https://ror.org/04epb4p87","country_code":"CN","type":"education","lineage":["https://openalex.org/I114539943"]},{"id":"https://openalex.org/I4210165038","display_name":"University of Chinese Academy of Sciences","ror":"https://ror.org/05qbk4x57","country_code":"CN","type":"education","lineage":["https://openalex.org/I19820366","https://openalex.org/I4210165038"]},{"id":"https://openalex.org/I19820366","display_name":"Chinese Academy of Sciences","ror":"https://ror.org/034t30j35","country_code":"CN","type":"funder","lineage":["https://openalex.org/I19820366"]},{"id":"https://openalex.org/I4210112820","display_name":"Shanghai Institute of Materia Medica","ror":"https://ror.org/022syn853","country_code":"CN","type":"facility","lineage":["https://openalex.org/I19820366","https://openalex.org/I4210112820"]}],"countries":["CN"],"is_corresponding":false,"raw_author_name":"Cheng Luo","raw_affiliation_strings":["School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310000, China","School of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou, 310053, China","The Center for Chemical Biology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China"],"affiliations":[{"raw_affiliation_string":"School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310000, China","institution_ids":["https://openalex.org/I4210165038"]},{"raw_affiliation_string":"School of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou, 310053, China","institution_ids":["https://openalex.org/I114539943"]},{"raw_affiliation_string":"The Center for Chemical Biology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China","institution_ids":["https://openalex.org/I4210112820","https://openalex.org/I19820366"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5010959343","display_name":"Jia Jin","orcid":"https://orcid.org/0000-0003-3315-4797"},"institutions":[{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]}],"countries":["CN"],"is_corresponding":true,"raw_author_name":"Jia Jin","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5100357234","display_name":"Fei Ye","orcid":"https://orcid.org/0000-0003-4119-3219"},"institutions":[{"id":"https://openalex.org/I114539943","display_name":"Zhejiang Chinese Medical University","ror":"https://ror.org/04epb4p87","country_code":"CN","type":"education","lineage":["https://openalex.org/I114539943"]},{"id":"https://openalex.org/I1328775524","display_name":"Zhejiang Sci-Tech University","ror":"https://ror.org/03893we55","country_code":"CN","type":"education","lineage":["https://openalex.org/I1328775524"]}],"countries":["CN"],"is_corresponding":true,"raw_author_name":"Fei Ye","raw_affiliation_strings":["College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","School of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou, 310053, China"],"affiliations":[{"raw_affiliation_string":"College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China","institution_ids":["https://openalex.org/I1328775524"]},{"raw_affiliation_string":"School of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou, 310053, China","institution_ids":["https://openalex.org/I114539943"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":14,"corresponding_author_ids":["https://openalex.org/A5010959343","https://openalex.org/A5100357234"],"corresponding_institution_ids":["https://openalex.org/I114539943","https://openalex.org/I1328775524"],"apc_list":null,"apc_paid":null,"fwci":0.7815,"has_fulltext":false,"cited_by_count":11,"citation_normalized_percentile":{"value":0.68087789,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":94,"max":99},"biblio":{"volume":"62","issue":"3","first_page":"692","last_page":"702"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T13157","display_name":"Cancer-related gene regulation","score":1.0,"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/T13157","display_name":"Cancer-related gene regulation","score":1.0,"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/T10269","display_name":"Epigenetics and DNA Methylation","score":0.9925000071525574,"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"}}],"keywords":[{"id":"https://openalex.org/keywords/protein-arginine-methyltransferase-5","display_name":"Protein arginine methyltransferase 5","score":0.7419803142547607},{"id":"https://openalex.org/keywords/methyltransferase","display_name":"Methyltransferase","score":0.7167009711265564},{"id":"https://openalex.org/keywords/arginine","display_name":"Arginine","score":0.6319073438644409},{"id":"https://openalex.org/keywords/biochemistry","display_name":"Biochemistry","score":0.5553989410400391},{"id":"https://openalex.org/keywords/western-blot","display_name":"Western blot","score":0.5545482039451599},{"id":"https://openalex.org/keywords/ic50","display_name":"IC50","score":0.5430036187171936},{"id":"https://openalex.org/keywords/potency","display_name":"Potency","score":0.43794649839401245},{"id":"https://openalex.org/keywords/chemistry","display_name":"Chemistry","score":0.41871944069862366},{"id":"https://openalex.org/keywords/enzyme","display_name":"Enzyme","score":0.4164445698261261},{"id":"https://openalex.org/keywords/biology","display_name":"Biology","score":0.4044603705406189},{"id":"https://openalex.org/keywords/pharmacology","display_name":"Pharmacology","score":0.35319286584854126},{"id":"https://openalex.org/keywords/methylation","display_name":"Methylation","score":0.30340760946273804},{"id":"https://openalex.org/keywords/amino-acid","display_name":"Amino acid","score":0.2531532049179077},{"id":"https://openalex.org/keywords/in-vitro","display_name":"In vitro","score":0.22102788090705872},{"id":"https://openalex.org/keywords/gene","display_name":"Gene","score":0.05515199899673462}],"concepts":[{"id":"https://openalex.org/C111819275","wikidata":"https://www.wikidata.org/wiki/Q18035368","display_name":"Protein arginine methyltransferase 5","level":5,"score":0.7419803142547607},{"id":"https://openalex.org/C91965660","wikidata":"https://www.wikidata.org/wiki/Q415875","display_name":"Methyltransferase","level":4,"score":0.7167009711265564},{"id":"https://openalex.org/C2777468819","wikidata":"https://www.wikidata.org/wiki/Q173670","display_name":"Arginine","level":3,"score":0.6319073438644409},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.5553989410400391},{"id":"https://openalex.org/C2776415932","wikidata":"https://www.wikidata.org/wiki/Q48743","display_name":"Western blot","level":3,"score":0.5545482039451599},{"id":"https://openalex.org/C2777752497","wikidata":"https://www.wikidata.org/wiki/Q286779","display_name":"IC50","level":3,"score":0.5430036187171936},{"id":"https://openalex.org/C57992300","wikidata":"https://www.wikidata.org/wiki/Q2066956","display_name":"Potency","level":3,"score":0.43794649839401245},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.41871944069862366},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.4164445698261261},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.4044603705406189},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.35319286584854126},{"id":"https://openalex.org/C33288867","wikidata":"https://www.wikidata.org/wiki/Q518328","display_name":"Methylation","level":3,"score":0.30340760946273804},{"id":"https://openalex.org/C515207424","wikidata":"https://www.wikidata.org/wiki/Q8066","display_name":"Amino acid","level":2,"score":0.2531532049179077},{"id":"https://openalex.org/C202751555","wikidata":"https://www.wikidata.org/wiki/Q221681","display_name":"In vitro","level":2,"score":0.22102788090705872},{"id":"https://openalex.org/C104317684","wikidata":"https://www.wikidata.org/wiki/Q7187","display_name":"Gene","level":2,"score":0.05515199899673462}],"mesh":[{"descriptor_ui":"D001120","descriptor_name":"Arginine","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001120","descriptor_name":"Arginine","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001120","descriptor_name":"Arginine","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":true},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D011484","descriptor_name":"Protein-Arginine N-Methyltransferases","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D011484","descriptor_name":"Protein-Arginine N-Methyltransferases","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D011484","descriptor_name":"Protein-Arginine N-Methyltransferases","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D011485","descriptor_name":"Protein Binding","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":"D011485","descriptor_name":"Protein Binding","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1021/acs.jcim.1c01100","is_oa":false,"landing_page_url":"https://doi.org/10.1021/acs.jcim.1c01100","pdf_url":null,"source":{"id":"https://openalex.org/S167262187","display_name":"Journal of Chemical Information and Modeling","issn_l":"1549-9596","issn":["1549-9596","1549-960X"],"is_oa":false,"is_in_doaj":false,"is_core":true,"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Chemical Information and Modeling","raw_type":"journal-article"},{"id":"pmid:35098713","is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/35098713","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,"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":"Journal of chemical information and modeling","raw_type":null}],"best_oa_location":null,"sustainable_development_goals":[{"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3","score":0.7799999713897705}],"awards":[{"id":"https://openalex.org/G6909338033","display_name":null,"funder_award_id":"81803339","funder_id":"https://openalex.org/F4320321001","funder_display_name":"National Natural Science Foundation of China"}],"funders":[{"id":"https://openalex.org/F4320321001","display_name":"National Natural Science Foundation of China","ror":"https://ror.org/01h0zpd94"}],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":48,"referenced_works":["https://openalex.org/W1970569586","https://openalex.org/W1985588649","https://openalex.org/W1990014790","https://openalex.org/W2001856542","https://openalex.org/W2008876829","https://openalex.org/W2010899127","https://openalex.org/W2012957359","https://openalex.org/W2015475080","https://openalex.org/W2022433519","https://openalex.org/W2025277638","https://openalex.org/W2027423337","https://openalex.org/W2032271983","https://openalex.org/W2039556247","https://openalex.org/W2043509228","https://openalex.org/W2053961392","https://openalex.org/W2074682587","https://openalex.org/W2081829478","https://openalex.org/W2087719423","https://openalex.org/W2091896816","https://openalex.org/W2096184225","https://openalex.org/W2103432725","https://openalex.org/W2111692348","https://openalex.org/W2127792718","https://openalex.org/W2165938086","https://openalex.org/W2183828138","https://openalex.org/W2282994692","https://openalex.org/W2331846333","https://openalex.org/W2473904577","https://openalex.org/W2510334948","https://openalex.org/W2541038380","https://openalex.org/W2553756300","https://openalex.org/W2570732803","https://openalex.org/W2763919936","https://openalex.org/W2773350707","https://openalex.org/W2795742294","https://openalex.org/W2892349206","https://openalex.org/W2907450938","https://openalex.org/W2949815414","https://openalex.org/W2975888204","https://openalex.org/W2982635561","https://openalex.org/W3005800239","https://openalex.org/W3026109815","https://openalex.org/W3032567445","https://openalex.org/W3048653545","https://openalex.org/W3125448631","https://openalex.org/W3139197589","https://openalex.org/W3150783208","https://openalex.org/W4242235585"],"related_works":["https://openalex.org/W4392375946","https://openalex.org/W2988905850","https://openalex.org/W2995805737","https://openalex.org/W2980573094","https://openalex.org/W2032623135","https://openalex.org/W3179398810","https://openalex.org/W2323240402","https://openalex.org/W2034379669","https://openalex.org/W2751282779","https://openalex.org/W4232246399"],"abstract_inverted_index":{"CARM1":[0,34,65,114,159,188],"(coactivator-associated":[1],"arginine":[2,12],"methyltransferase":[3],"1),":[4],"which":[5],"belongs":[6],"to":[7,44,57,71,98],"type":[8,94,100,120],"I":[9,95,101,121],"PRMTs":[10],"(protein":[11],"methyltransferases),":[13],"is":[14],"a":[15,77,130,171],"potential":[16],"therapeutic":[17],"target":[18,158],"for":[19,174],"treatment":[20],"of":[21,132,142,186],"multiple":[22],"cancers.":[23],"In":[24,145],"this":[25],"study,":[26],"we":[27,166],"first":[28],"identified":[29,167],"several":[30],"hit":[31],"compounds":[32,59],"against":[33,92,113,118],"by":[35],"structure-based":[36],"virtual":[37],"screening":[38],"(IC<sub>50</sub>":[39,66],"=":[40,67],"35.51":[41],"\u00b1":[42,46,69,73],"6.68":[43],"68.70":[45],"8.12":[47],"\u03bcM)":[48],"and":[49,115,150,179,193],"then":[50],"carried":[51],"out":[52],"chemical":[53],"structural":[54],"optimizations,":[55],"leading":[56],"six":[58],"with":[60,79,190],"significantly":[61],"improved":[62],"activities":[63,128,192],"targeting":[64],"18":[68],"2":[70],"107":[72],"6":[74],"nM).":[75],"As":[76],"compound":[78],"an":[80],"ethylenediamino":[81],"motif,":[82],"the":[83,99,164,183],"most":[84],"potent":[85,90,172],"inhibitor,":[86],"ZL-28-6,":[87],"also":[88],"exhibited":[89],"inhibition":[91],"other":[93,119],"PRMTs.":[96,122],"Compared":[97],"PRMT":[102],"inhibitor":[103,165],"from":[104],"our":[105],"previous":[106],"work":[107],"(DCPR049_12),":[108],"ZL-28-6":[109,124,156],"showed":[110,125],"increased":[111],"potency":[112],"decreased":[116],"activity":[117],"Moreover,":[123],"better":[126],"antiproliferation":[127],"toward":[129],"series":[131],"solid":[133],"tumor":[134],"cells":[135],"than":[136],"DCPR049_12,":[137],"indicating":[138],"its":[139],"broad":[140],"spectrum":[141],"anticancer":[143],"activity.":[144],"addition,":[146],"cellular":[147],"thermal":[148],"shift":[149],"Western":[151],"blot":[152],"assays":[153],"validated":[154],"that":[155],"could":[157,168],"in":[160],"cells.":[161],"Taken":[162],"together,":[163],"serve":[169],"as":[170],"probe":[173],"studying":[175],"CARM1's":[176],"biological":[177],"functions":[178],"shed":[180],"light":[181],"on":[182],"future":[184],"design":[185],"novel":[187],"inhibitors":[189],"stronger":[191],"selectivities.":[194]},"counts_by_year":[{"year":2026,"cited_by_count":2},{"year":2025,"cited_by_count":2},{"year":2024,"cited_by_count":5},{"year":2023,"cited_by_count":2}],"updated_date":"2026-03-15T09:29:46.208133","created_date":"2025-10-10T00:00:00"}