{"id":"https://openalex.org/W4362494909","doi":"https://doi.org/10.1158/1535-7163.c.6537717","title":"Data from Potent Dual BET Bromodomain-Kinase Inhibitors as Value-Added Multitargeted Chemical Probes and Cancer Therapeutics","display_name":"Data from Potent Dual BET Bromodomain-Kinase Inhibitors as Value-Added Multitargeted Chemical Probes and Cancer Therapeutics","publication_year":2023,"publication_date":"2023-04-03","ids":{"openalex":"https://openalex.org/W4362494909","doi":"https://doi.org/10.1158/1535-7163.c.6537717"},"language":"en","primary_location":{"id":"doi:10.1158/1535-7163.c.6537717","doi":"https://doi.org/10.1158/1535-7163.c.6537717","is_oa":true,"landing_page_url":"http://dx.doi.org/10.1158/1535-7163.c.6537717","pdf_url":null,"source":null,"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"acceptedVersion","is_accepted":true,"is_published":false,"raw_source_name":"American Association for Cancer Research","raw_type":"posted-content"},"volume":null,"type":"other","indexed_in":["crossref"],"open_access":{"is_oa":true,"oa_status":"gold","oa_url":"http://dx.doi.org/10.1158/1535-7163.c.6537717","any_repository_has_fulltext":null},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5072503883","display_name":"S.W. Ember","orcid":"https://orcid.org/0009-0004-6051-4625","observed_orcids":["https://orcid.org/0009-0004-6051-4625"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Stuart W. Ember","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5015343580","display_name":"Que T. Lambert","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Que T. Lambert","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5032252707","display_name":"Norbert Berndt","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Norbert Berndt","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5087134189","display_name":"Steven Gunawan","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Steven Gunawan","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5008138011","display_name":"Muhammad Ayaz","orcid":"https://orcid.org/0000-0002-4299-2445","observed_orcids":["https://orcid.org/0000-0002-4299-2445","https://orcid.org/0009-0002-2021-3735"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Muhammad Ayaz","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5017977483","display_name":"Marilena Tauro","orcid":"https://orcid.org/0000-0003-2361-7364","observed_orcids":["https://orcid.org/0000-0003-2361-7364"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Marilena Tauro","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5041357428","display_name":"Jin\u2010Yi Zhu","orcid":"https://orcid.org/0000-0001-5436-4262","observed_orcids":["https://orcid.org/0000-0001-5436-4262"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Jin-Yi Zhu","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5068660492","display_name":"Paula J. C. Cranfill","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Paula J. Cranfill","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5088889740","display_name":"Patricia Greninger","orcid":"https://orcid.org/0000-0001-9110-7695","observed_orcids":["https://orcid.org/0000-0001-9110-7695"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Patricia Greninger","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5005942374","display_name":"Conor C. Lynch","orcid":"https://orcid.org/0000-0002-4506-6244","observed_orcids":["https://orcid.org/0000-0002-4506-6244"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Conor C. Lynch","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5060699951","display_name":"Cyril H. Benes","orcid":"https://orcid.org/0000-0002-8751-9707","observed_orcids":["https://orcid.org/0000-0002-8751-9707"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Cyril H. Benes","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5057921101","display_name":"Harshani R. Lawrence","orcid":"https://orcid.org/0000-0002-9263-7775","observed_orcids":["https://orcid.org/0000-0002-9263-7775"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Harshani R. Lawrence","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5060816904","display_name":"Gary W. Reuther","orcid":"https://orcid.org/0000-0002-2317-931X","observed_orcids":["https://orcid.org/0000-0002-2317-931X"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Gary W. Reuther","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5027503793","display_name":"Nicholas J. Lawrence","orcid":"https://orcid.org/0000-0003-1129-2558","observed_orcids":["https://orcid.org/0000-0003-1129-2558"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Nicholas J. Lawrence","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"last","author":{"id":"https://openalex.org/A5024223427","display_name":"E. Sch\u00f6nbrunn","orcid":"https://orcid.org/0000-0002-3589-3510","observed_orcids":["https://orcid.org/0000-0002-3589-3510"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Ernst Sch\u00f6nbrunn","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]}],"institutions":[],"countries_distinct_count":0,"institutions_distinct_count":0,"corresponding_author_ids":[],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":null,"has_fulltext":false,"cited_by_count":0,"citation_normalized_percentile":null,"cited_by_percentile_year":null,"biblio":{"volume":null,"issue":null,"first_page":null,"last_page":null},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T12534","display_name":"Protein Degradation and Inhibitors","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/T12534","display_name":"Protein Degradation and Inhibitors","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/T11533","display_name":"Melanoma and MAPK Pathways","score":0.0,"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/T10274","display_name":"Synthesis and biological activity","score":0.0,"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/bet-inhibitors","display_name":"BET inhibitors","score":0.8410000205039978},{"id":"https://openalex.org/keywords/kinase-inhibitors","display_name":"kinase inhibitors","score":0.6980000138282776},{"id":"https://openalex.org/keywords/brd4","display_name":"BRD4","score":0.8999999761581421},{"id":"https://openalex.org/keywords/jak2","display_name":"JAK2","score":0.7360000014305115},{"id":"https://openalex.org/keywords/flt3","display_name":"FLT3","score":0.9909999966621399},{"id":"https://openalex.org/keywords/ret","display_name":"RET","score":0.9959999918937683},{"id":"https://openalex.org/keywords/ros1","display_name":"ROS1","score":0.9990000128746033},{"id":"https://openalex.org/keywords/myeloproliferative-neoplasms","display_name":"myeloproliferative neoplasms","score":0.8460000157356262},{"id":"https://openalex.org/keywords/hematopoietic-progenitor-cells","display_name":"hematopoietic progenitor cells","score":0.9729999899864197},{"id":"https://openalex.org/keywords/drug-synergy","display_name":"drug synergy","score":0.8349999785423279},{"id":"https://openalex.org/keywords/jq1","display_name":"JQ1","score":0.5419999957084656},{"id":"https://openalex.org/keywords/hematologic-malignancies","display_name":"hematologic malignancies","score":0.5},{"id":"https://openalex.org/keywords/bone-cancer","display_name":"bone cancer","score":0.6859999895095825}],"concepts":[{"id":"https://openalex.org/C74401373","wikidata":"https://www.wikidata.org/wiki/Q1829843","display_name":"Bromodomain","level":4,"score":0.8525202870368958},{"id":"https://openalex.org/C2780862049","wikidata":"https://www.wikidata.org/wiki/Q25326844","display_name":"BET inhibitor","level":5,"score":0.6981660723686218},{"id":"https://openalex.org/C184235292","wikidata":"https://www.wikidata.org/wiki/Q421851","display_name":"Kinase","level":2,"score":0.6310528516769409},{"id":"https://openalex.org/C2779634854","wikidata":"https://www.wikidata.org/wiki/Q18037206","display_name":"BRD4","level":5,"score":0.5627663135528564},{"id":"https://openalex.org/C502942594","wikidata":"https://www.wikidata.org/wiki/Q3421914","display_name":"Cancer research","level":1,"score":0.5548068284988403},{"id":"https://openalex.org/C121608353","wikidata":"https://www.wikidata.org/wiki/Q12078","display_name":"Cancer","level":2,"score":0.5367409586906433},{"id":"https://openalex.org/C96232424","wikidata":"https://www.wikidata.org/wiki/Q4118072","display_name":"Cancer cell","level":3,"score":0.5212210416793823},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.4998915195465088},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.4450932741165161},{"id":"https://openalex.org/C2777752497","wikidata":"https://www.wikidata.org/wiki/Q286779","display_name":"IC50","level":3,"score":0.43334347009658813},{"id":"https://openalex.org/C62112901","wikidata":"https://www.wikidata.org/wiki/Q189159","display_name":"Cell growth","level":2,"score":0.4284239411354065},{"id":"https://openalex.org/C81885089","wikidata":"https://www.wikidata.org/wiki/Q189082","display_name":"Cell culture","level":2,"score":0.4152350425720215},{"id":"https://openalex.org/C42362537","wikidata":"https://www.wikidata.org/wiki/Q87099740","display_name":"Tyrosine kinase","level":3,"score":0.4108871817588806},{"id":"https://openalex.org/C202751555","wikidata":"https://www.wikidata.org/wiki/Q221681","display_name":"In vitro","level":2,"score":0.32349613308906555},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.3026237189769745},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.2849361300468445},{"id":"https://openalex.org/C62478195","wikidata":"https://www.wikidata.org/wiki/Q828130","display_name":"Signal transduction","level":2,"score":0.21555626392364502},{"id":"https://openalex.org/C119157956","wikidata":"https://www.wikidata.org/wiki/Q796604","display_name":"Acetylation","level":3,"score":0.18141987919807434},{"id":"https://openalex.org/C104317684","wikidata":"https://www.wikidata.org/wiki/Q7187","display_name":"Gene","level":2,"score":0.10769876837730408},{"id":"https://openalex.org/C54355233","wikidata":"https://www.wikidata.org/wiki/Q7162","display_name":"Genetics","level":1,"score":0.0697588324546814}],"mesh":[],"locations_count":1,"locations":[{"id":"doi:10.1158/1535-7163.c.6537717","doi":"https://doi.org/10.1158/1535-7163.c.6537717","is_oa":true,"landing_page_url":"http://dx.doi.org/10.1158/1535-7163.c.6537717","pdf_url":null,"source":null,"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"acceptedVersion","is_accepted":true,"is_published":false,"raw_source_name":"American Association for Cancer Research","raw_type":"posted-content"}],"best_oa_location":{"id":"doi:10.1158/1535-7163.c.6537717","doi":"https://doi.org/10.1158/1535-7163.c.6537717","is_oa":true,"landing_page_url":"http://dx.doi.org/10.1158/1535-7163.c.6537717","pdf_url":null,"source":null,"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"acceptedVersion","is_accepted":true,"is_published":false,"raw_source_name":"American Association for Cancer Research","raw_type":"posted-content"},"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being","score":0.8371999859809875}],"sustainable_development_goals_aurora":[{"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being","score":0.7599999904632568}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":0,"referenced_works":[],"related_works":["https://openalex.org/W2599917498","https://openalex.org/W2750537303","https://openalex.org/W2955921074","https://openalex.org/W2561160634","https://openalex.org/W2805159365","https://openalex.org/W1982033297","https://openalex.org/W4402308763","https://openalex.org/W2072981794","https://openalex.org/W4411442991","https://openalex.org/W4361953496"],"abstract_inverted_index":{"Abstract":[0],"Synergistic":[1],"action":[2],"of":[3,18,24,45,74,122,144],"kinase":[4,125],"and":[5,31,37,41,53,66,99,102,116,124,151],"BET":[6,109],"bromodomain":[7],"inhibitors":[8],"in":[9,60,135],"cell":[10,64,87,136],"killing":[11],"has":[12],"been":[13],"reported":[14],"for":[15,131],"a":[16,42,128],"variety":[17],"cancers.":[19],"Using":[20],"the":[21,25,72,107,132],"chemical":[22,149],"scaffold":[23],"JAK2":[26],"inhibitor":[27,110],"TG101348,":[28],"we":[29],"developed":[30],"characterized":[32],"single":[33,108],"agents":[34,146],"which":[35],"potently":[36],"simultaneously":[38],"inhibit":[39],"BRD4":[40,123],"specific":[43],"set":[44],"oncogenic":[46],"tyrosine":[47],"kinases":[48],"including":[49],"JAK2,":[50],"FLT3,":[51],"RET,":[52],"ROS1.":[54],"Lead":[55],"compounds":[56],"showed":[57],"on-target":[58],"inhibition":[59,126],"several":[61],"blood":[62,100],"cancer":[63,86,152],"lines":[65,88],"were":[67],"highly":[68],"efficacious":[69],"at":[70],"inhibiting":[71],"growth":[73,91],"hematopoietic":[75],"progenitor":[76],"cells":[77],"from":[78],"patients":[79],"with":[80,94],"myeloproliferative":[81],"neoplasm.":[82],"Screening":[83],"across":[84],"931":[85],"revealed":[89],"differential":[90],"inhibitory":[92],"potential":[93,143],"highest":[95],"activity":[96,105],"against":[97],"bone":[98],"cancers":[101],"greatly":[103],"enhanced":[104],"over":[106],"JQ1.":[111],"Gene":[112],"drug":[113,117],"sensitivity":[114],"analyses":[115],"combination":[118],"studies":[119],"indicate":[120,141],"synergism":[121],"as":[127,147],"plausible":[129],"reason":[130],"superior":[133],"potency":[134],"killing.":[137],"Combined,":[138],"our":[139],"findings":[140],"promising":[142],"these":[145],"novel":[148],"probes":[150],"therapeutics.":[153],"Mol":[154],"Cancer":[155],"Ther;":[156],"16(6);":[157],"1054\u201367.":[158],"\u00a92017":[159],"AACR.":[160]},"counts_by_year":[],"updated_date":"2026-10-14T16:39:01.820549","created_date":"2023-04-05T00:00:00"}