{"id":"https://openalex.org/W2967540280","doi":null,"title":"Development of screening tools for the identification of small molecule inhibitors of HIF-1\u03b1/HIF-1\u03b2 protein-protein interaction","display_name":"Development of screening tools for the identification of small molecule inhibitors of HIF-1\u03b1/HIF-1\u03b2 protein-protein interaction","publication_year":2005,"publication_date":"2005-05-01","ids":{"openalex":"https://openalex.org/W2967540280","mag":"2967540280"},"language":"en","primary_location":{"id":"mag:2967540280","doi":null,"is_oa":false,"landing_page_url":"https://cancerres.aacrjournals.org/content/65/9_Supplement/403.1","pdf_url":null,"source":{"id":"https://openalex.org/S168522863","display_name":"Cancer Research","issn_l":"0008-5472","issn":["0008-5472","1538-7445"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","doyens","jufo-3","ki-jl-3","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320273","host_organization_name":"American Association for Cancer Research","host_organization_lineage":["https://openalex.org/P4310320273"],"host_organization_lineage_names":["American Association for Cancer Research"],"type":"journal"},"license":null,"license_id":null,"version":null,"is_accepted":false,"is_published":false,"raw_source_name":"Cancer Research","raw_type":null},"volume":null,"type":"article","is_traditional":true,"indexed_in":[],"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/A5100697866","display_name":"Eun\u2010Jung Park","orcid":"https://orcid.org/0000-0002-2778-1834","observed_orcids":["https://orcid.org/0000-0002-2778-1834","https://orcid.org/0000-0002-5761-0454"]},"institutions":[{"id":"https://openalex.org/I880747138","display_name":"Science Applications International Corporation (United States)","ror":"https://ror.org/00zv91802","country_code":"US","type":"company","lineage":["https://openalex.org/I880747138"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Eun\u2010Jung Park","raw_affiliation_strings":["SAIC\u2010Frederick Inc, Frederick, MD"],"raw_orcid":"https://orcid.org/0000-0002-2778-1834","affiliations":[{"raw_affiliation_string":"SAIC\u2010Frederick Inc, Frederick, MD","institution_ids":["https://openalex.org/I880747138"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110113202","display_name":"Dehe Kong","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I880747138","display_name":"Science Applications International Corporation (United States)","ror":"https://ror.org/00zv91802","country_code":"US","type":"company","lineage":["https://openalex.org/I880747138"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Dehe Kong","raw_affiliation_strings":["SAIC\u2010Frederick Inc, Frederick, MD"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"SAIC\u2010Frederick Inc, Frederick, MD","institution_ids":["https://openalex.org/I880747138"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5035537529","display_name":"Robert J. Fisher","orcid":"https://orcid.org/0000-0003-4598-2274","observed_orcids":["https://orcid.org/0000-0003-4598-2274"]},"institutions":[{"id":"https://openalex.org/I880747138","display_name":"Science Applications International Corporation (United States)","ror":"https://ror.org/00zv91802","country_code":"US","type":"company","lineage":["https://openalex.org/I880747138"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Robert J. Fisher","raw_affiliation_strings":["SAIC\u2010Frederick Inc, Frederick, MD"],"raw_orcid":"https://orcid.org/0000-0003-4598-2274","affiliations":[{"raw_affiliation_string":"SAIC\u2010Frederick Inc, Frederick, MD","institution_ids":["https://openalex.org/I880747138"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5084816440","display_name":"Robert H. Shoemaker","orcid":"https://orcid.org/0000-0003-3608-1714","observed_orcids":["https://orcid.org/0000-0003-3608-1714"]},"institutions":[{"id":"https://openalex.org/I880747138","display_name":"Science Applications International Corporation (United States)","ror":"https://ror.org/00zv91802","country_code":"US","type":"company","lineage":["https://openalex.org/I880747138"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Robert H. Shoemaker","raw_affiliation_strings":["SAIC\u2010Frederick Inc, Frederick, MD"],"raw_orcid":"https://orcid.org/0000-0003-3608-1714","affiliations":[{"raw_affiliation_string":"SAIC\u2010Frederick Inc, Frederick, MD","institution_ids":["https://openalex.org/I880747138"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5000029047","display_name":"Giovanni Melillo","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I880747138","display_name":"Science Applications International Corporation (United States)","ror":"https://ror.org/00zv91802","country_code":"US","type":"company","lineage":["https://openalex.org/I880747138"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Giovanni Melillo","raw_affiliation_strings":["SAIC\u2010Frederick Inc, Frederick, MD"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"SAIC\u2010Frederick Inc, Frederick, MD","institution_ids":["https://openalex.org/I880747138"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":[],"corresponding_institution_ids":["https://openalex.org/I880747138"],"apc_list":null,"apc_paid":null,"fwci":0.0,"has_fulltext":false,"cited_by_count":0,"citation_normalized_percentile":{"value":0.36471899,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":null,"biblio":{"volume":"65","issue":null,"first_page":"403","last_page":"403"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10631","display_name":"Cancer, Hypoxia, and Metabolism","score":0.9868000149726868,"subfield":{"id":"https://openalex.org/subfields/1306","display_name":"Cancer Research"},"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/T10631","display_name":"Cancer, Hypoxia, and Metabolism","score":0.9868000149726868,"subfield":{"id":"https://openalex.org/subfields/1306","display_name":"Cancer Research"},"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/T13426","display_name":"Kruppel-like factors research","score":0.0007999999797903001,"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":0.00039999998989515007,"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/hif-1alpha","display_name":"HIF-1\u03b1","score":0.7310000061988831},{"id":"https://openalex.org/keywords/aryl-hydrocarbon-receptor-nuclear-translocator","display_name":"ARNT","score":0.9959999918937683},{"id":"https://openalex.org/keywords/protein-protein-interaction-inhibitors","display_name":"protein-protein interaction inhibitors","score":0.8859999775886536},{"id":"https://openalex.org/keywords/small-molecule-inhibitors","display_name":"small molecule inhibitors","score":0.7620000243186951},{"id":"https://openalex.org/keywords/hypoxia-inducible-factor","display_name":"hypoxia-inducible factor","score":0.8029999732971191},{"id":"https://openalex.org/keywords/drug-screening","display_name":"drug screening","score":0.4129999876022339},{"id":"https://openalex.org/keywords/transcription-factor-inhibitors","display_name":"transcription factor inhibitors","score":0.7329999804496765},{"id":"https://openalex.org/keywords/cancer-therapeutics","display_name":"cancer therapeutics","score":0.6349999904632568}],"concepts":[{"id":"https://openalex.org/C45815257","wikidata":"https://www.wikidata.org/wiki/Q109984923","display_name":"Aryl hydrocarbon receptor nuclear translocator","level":5,"score":0.7785781621932983},{"id":"https://openalex.org/C86339819","wikidata":"https://www.wikidata.org/wiki/Q407384","display_name":"Transcription factor","level":3,"score":0.6916041374206543},{"id":"https://openalex.org/C6174537","wikidata":"https://www.wikidata.org/wiki/Q377955","display_name":"Basic helix-loop-helix","level":5,"score":0.657092273235321},{"id":"https://openalex.org/C2778875234","wikidata":"https://www.wikidata.org/wiki/Q36626","display_name":"PAS domain","level":4,"score":0.5356440544128418},{"id":"https://openalex.org/C11804247","wikidata":"https://www.wikidata.org/wiki/Q896177","display_name":"Protein\u2013protein interaction","level":2,"score":0.5330281257629395},{"id":"https://openalex.org/C2909350873","wikidata":"https://www.wikidata.org/wiki/Q104598479","display_name":"Hypoxia-Inducible Factor 1","level":4,"score":0.5098103880882263},{"id":"https://openalex.org/C31194975","wikidata":"https://www.wikidata.org/wiki/Q20970095","display_name":"HIF1A","level":3,"score":0.4927878677845001},{"id":"https://openalex.org/C104292427","wikidata":"https://www.wikidata.org/wiki/Q899781","display_name":"Protein subunit","level":3,"score":0.4879457354545593},{"id":"https://openalex.org/C161624437","wikidata":"https://www.wikidata.org/wiki/Q1988322","display_name":"Small molecule","level":2,"score":0.47709164023399353},{"id":"https://openalex.org/C179926584","wikidata":"https://www.wikidata.org/wiki/Q207714","display_name":"Transcription (linguistics)","level":2,"score":0.47360873222351074},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.4618277847766876},{"id":"https://openalex.org/C95444343","wikidata":"https://www.wikidata.org/wiki/Q7141","display_name":"Cell biology","level":1,"score":0.44164854288101196},{"id":"https://openalex.org/C83730767","wikidata":"https://www.wikidata.org/wiki/Q24778884","display_name":"G alpha subunit","level":4,"score":0.41425007581710815},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.4139323830604553},{"id":"https://openalex.org/C104317684","wikidata":"https://www.wikidata.org/wiki/Q7187","display_name":"Gene","level":2,"score":0.36293062567710876},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.3205971121788025},{"id":"https://openalex.org/C153911025","wikidata":"https://www.wikidata.org/wiki/Q7202","display_name":"Molecular biology","level":1,"score":0.3201560974121094},{"id":"https://openalex.org/C94966510","wikidata":"https://www.wikidata.org/wiki/Q2252764","display_name":"DNA-binding protein","level":4,"score":0.29128336906433105},{"id":"https://openalex.org/C33594762","wikidata":"https://www.wikidata.org/wiki/Q155750","display_name":"Aryl hydrocarbon receptor","level":4,"score":0.08563673496246338},{"id":"https://openalex.org/C138885662","wikidata":"https://www.wikidata.org/wiki/Q5891","display_name":"Philosophy","level":0,"score":0.0},{"id":"https://openalex.org/C41895202","wikidata":"https://www.wikidata.org/wiki/Q8162","display_name":"Linguistics","level":1,"score":0.0}],"mesh":[],"locations_count":1,"locations":[{"id":"mag:2967540280","doi":null,"is_oa":false,"landing_page_url":"https://cancerres.aacrjournals.org/content/65/9_Supplement/403.1","pdf_url":null,"source":{"id":"https://openalex.org/S168522863","display_name":"Cancer Research","issn_l":"0008-5472","issn":["0008-5472","1538-7445"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","doyens","jufo-3","ki-jl-3","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320273","host_organization_name":"American Association for Cancer Research","host_organization_lineage":["https://openalex.org/P4310320273"],"host_organization_lineage_names":["American Association for Cancer Research"],"type":"journal"},"license":null,"license_id":null,"version":null,"is_accepted":false,"is_published":false,"raw_source_name":"Cancer Research","raw_type":null}],"best_oa_location":null,"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","score":0.8371999859809875,"display_name":"Good health and well-being"}],"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/W2080364889","https://openalex.org/W2050442786","https://openalex.org/W2102939299","https://openalex.org/W2020344223","https://openalex.org/W2121314018","https://openalex.org/W2401794280","https://openalex.org/W4236852887","https://openalex.org/W2913963915","https://openalex.org/W3024229949","https://openalex.org/W1995501049"],"abstract_inverted_index":{"1708":[0],"Transcription":[2],"factors":[3,16],"are":[4,52,325],"attractive":[5],"targets":[6],"for":[7,38,149,345],"development":[8,39],"of":[9,14,40,49,57,74,77,138,152,156,165,169,184,219,246,250,255,268,275,321,333,341,348],"novel":[10],"therapeutics.":[11,41],"Selective":[12],"inhibitors":[13,155,351],"transcription":[15,48],"might":[17],"be":[18,353],"obtained":[19],"by":[20,203,216,266,295],"inhibiting":[21],"protein-protein":[22,30],"interaction,":[23],"a":[24,35,69,263,269,312],"crucial":[25,55],"step":[26],"in":[27,54,111,117,257,262,311],"dimerization.":[28],"However,":[29,113],"interaction":[31],"is":[32,68,99,105],"generally":[33],"considered":[34],"difficult":[36],"target":[37,344],"Hypoxia-inducible":[42],"factor":[43],"1":[44],"(HIF-1)":[45],"activates":[46],"the":[47,78,93,129,136,150,166,175,192,230,240,247,272,297,304,318,338,346],"genes":[50],"that":[51],"involved":[53],"aspects":[56],"cancer":[58],"biology,":[59],"including":[60],"angiogenesis,":[61],"cell":[62,236],"survival,":[63],"and":[64,86,109,127,171,186,195,215,252,323],"glucose":[65],"metabolism.":[66],"HIF-1":[67],"heterodimeric":[70],"protein":[71,206,270],"complex":[72],"composed":[73],"two":[75],"members":[76],"basic":[79],"helix-loop-helix":[80],"Per-ARNT-Sim":[81],"(bHLH-PAS)":[82],"domain":[83,168,340],"family,":[84],"HIF-1\u03b1":[85,98,114,170,185,251],"HIF-1\u03b2":[87,96,126,172,187],"(or":[88],"ARNT).":[89],"In":[90,142,225],"contrast":[91],"to":[92,119,145,174,234,283,327],"constitutively":[94],"expressed":[95,162,189],"subunit,":[97],"an":[100,143],"oxygen":[101],"labile":[102],"protein,":[103],"which":[104],"degraded":[106],"through":[107],"hydroxylation":[108],"ubiquitination":[110],"normoxia.":[112],"becomes":[115],"stabilized":[116],"response":[118,131],"hypoxia":[120,130],"or":[121,177],"iron":[122],"chelators,":[123],"dimerizes":[124],"with":[125],"binds":[128],"element":[132],"(HRE),":[133],"thereby":[134],"activating":[135],"expression":[137],"numerous":[139],"hypoxia-response":[140],"genes.":[141],"attempt":[144],"develop":[146],"screening":[147,296,335],"tools":[148,278],"identification":[151,347],"small":[153,349],"molecule":[154,350],"HIF-1\u03b1/\u03b2":[157,322,342],"heterodimer":[158],"formation,":[159],"we":[160,227],"have":[161,228],"several":[163,285],"fragments":[164,183],"N-terminal":[167,182,273],"fused":[173],"His":[176],"Flag":[178],"tags,":[179],"respectively.":[180],"Several":[181,307],"were":[188,281,293,309],"containing":[190,271,303,317],"either":[191],"bHLH,":[193],"PAS-A":[194,319,339],"PAS-B":[196],"domains.":[197,306],"An":[198],"ELISA":[199],"has":[200],"been":[201],"developed":[202],"immobilizing":[204],"HIF-1\u03b2-Flag":[205],"on":[207],"anti-flag":[208],"M2":[209],"monoclonal":[210],"antibodies":[211],"coated":[212],"96-well":[213],"plates":[214],"detecting":[217],"binding":[218,245],"HIF-1\u03b1-His":[220],"tag":[221],"using":[222,301,315,337],"anti-His-HRP":[223],"conjugate.":[224],"addition,":[226],"used":[229],"mammalian":[231],"two-hybrid":[232],"system":[233],"generate":[235],"lines":[237],"(293-PAS-A)":[238],"expressing":[239],"luciferase":[241,256],"reporter":[242],"gene":[243],"upon":[244],"pasA":[248],"domains":[249,320],"HIF-1\u03b2.":[253],"Expression":[254],"293-PAS-A":[258],"cells":[259],"was":[260],"inhibited":[261],"competitive":[264],"fashion":[265],"co-transfection":[267],"region":[274],"HIF-1\u03b1.":[276],"The":[277],"described":[279],"above":[280],"utilized":[282],"screen":[284,314],"libraries":[286],"available":[287],"at":[288],"NCI.":[289],"No":[290],"active":[291,330],"compounds":[292,308],"identified":[294,310],"NCI":[298],"diversity":[299],"set":[300],"proteins":[302,316],"bHLH":[305],"primary":[313],"studies":[324],"ongoing":[326,334],"validate":[328],"these":[329],"leads.":[331],"Results":[332],"activities":[336],"as":[343],"will":[352],"presented.":[354]},"counts_by_year":[],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2019-08-22T00:00:00"}
