{"id":"https://openalex.org/W4361947526","doi":"https://doi.org/10.1158/1535-7163.c.6530952","title":"Data from Identification and characterization of small-molecule inhibitors of hepsin","display_name":"Data from Identification and characterization of small-molecule inhibitors of hepsin","publication_year":2023,"publication_date":"2023-03-31","ids":{"openalex":"https://openalex.org/W4361947526","doi":"https://doi.org/10.1158/1535-7163.c.6530952"},"language":"en","primary_location":{"id":"doi:10.1158/1535-7163.c.6530952","doi":"https://doi.org/10.1158/1535-7163.c.6530952","is_oa":true,"landing_page_url":"https://doi.org/10.1158/1535-7163.c.6530952","pdf_url":null,"source":null,"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"American Association for Cancer Research","raw_type":"posted-content"},"volume":null,"type":"other","is_traditional":false,"indexed_in":["crossref"],"open_access":{"is_oa":true,"oa_status":"gold","oa_url":"https://doi.org/10.1158/1535-7163.c.6530952","any_repository_has_fulltext":null},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5086308028","display_name":"John R. Chevillet","orcid":"https://orcid.org/0000-0002-2546-7067","observed_orcids":["https://orcid.org/0000-0002-2546-7067"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"John R. Chevillet","raw_affiliation_strings":["Human Biology and","Program in Molecular and Cellular Biology, Departments of 4 Medicine,"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Human Biology and","institution_ids":[]},{"raw_affiliation_string":"Program in Molecular and Cellular Biology, Departments of 4 Medicine,","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5041240320","display_name":"Gemma J. Park","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210089486","display_name":"Fred Hutch Cancer Center","ror":"https://ror.org/007ps6h72","country_code":"US","type":"nonprofit","lineage":["https://openalex.org/I4210089486"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Gemma J. Park","raw_affiliation_strings":["Clinical Research, Fred Hutchinson Cancer Research Center;"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Clinical Research, Fred Hutchinson Cancer Research Center;","institution_ids":["https://openalex.org/I4210089486"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5062105620","display_name":"Antonio Bedalov","orcid":"https://orcid.org/0000-0002-7373-8255","observed_orcids":["https://orcid.org/0000-0002-7373-8255"]},"institutions":[{"id":"https://openalex.org/I4210089486","display_name":"Fred Hutch Cancer Center","ror":"https://ror.org/007ps6h72","country_code":"US","type":"nonprofit","lineage":["https://openalex.org/I4210089486"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Antonio Bedalov","raw_affiliation_strings":["Clinical Research, Fred Hutchinson Cancer Research Center;"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Clinical Research, Fred Hutchinson Cancer Research Center;","institution_ids":["https://openalex.org/I4210089486"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5056736840","display_name":"Julian A. Simon","orcid":"https://orcid.org/0000-0001-9235-7565","observed_orcids":["https://orcid.org/0000-0001-9235-7565"]},"institutions":[{"id":"https://openalex.org/I4210089486","display_name":"Fred Hutch Cancer Center","ror":"https://ror.org/007ps6h72","country_code":"US","type":"nonprofit","lineage":["https://openalex.org/I4210089486"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Julian A. Simon","raw_affiliation_strings":["Chemistry, and","Clinical Research, Fred Hutchinson Cancer Research Center;"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Chemistry, and","institution_ids":[]},{"raw_affiliation_string":"Clinical Research, Fred Hutchinson Cancer Research Center;","institution_ids":["https://openalex.org/I4210089486"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5080093390","display_name":"Valeri I. Vasioukhin","orcid":"https://orcid.org/0000-0002-6730-0281","observed_orcids":["https://orcid.org/0000-0002-6730-0281"]},"institutions":[{"id":"https://openalex.org/I201448701","display_name":"University of Washington","ror":"https://ror.org/00cvxb145","country_code":"US","type":"education","lineage":["https://openalex.org/I201448701"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Valeri I. Vasioukhin","raw_affiliation_strings":["Human Biology and","Institute for Stem Cells and Regenerative Medicine, University of Washington, Seattle, Washington","Pathology, and"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Human Biology and","institution_ids":[]},{"raw_affiliation_string":"Institute for Stem Cells and Regenerative Medicine, University of Washington, Seattle, Washington","institution_ids":["https://openalex.org/I201448701"]},{"raw_affiliation_string":"Pathology, and","institution_ids":[]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":2,"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/T10620","display_name":"Protease and Inhibitor Mechanisms","score":0.9994999766349792,"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/T10620","display_name":"Protease and Inhibitor Mechanisms","score":0.9994999766349792,"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/T10543","display_name":"Prostate Cancer Treatment and Research","score":0.00019999999494757503,"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/T12505","display_name":"Peptidase Inhibition and Analysis","score":9.999999747378752e-05,"subfield":{"id":"https://openalex.org/subfields/1303","display_name":"Biochemistry"},"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/hepsin","display_name":"hepsin","score":1.0},{"id":"https://openalex.org/keywords/small-molecule-inhibitors","display_name":"small molecule inhibitors","score":0.953000009059906},{"id":"https://openalex.org/keywords/prostate-cancer","display_name":"prostate cancer","score":0.8489999771118164},{"id":"https://openalex.org/keywords/metastasis","display_name":"metastasis","score":0.703000009059906},{"id":"https://openalex.org/keywords/serine-protease","display_name":"serine protease","score":0.5979999899864197},{"id":"https://openalex.org/keywords/high-throughput-screening","display_name":"high-throughput screening","score":0.7429999709129333},{"id":"https://openalex.org/keywords/drug-repurposing","display_name":"drug repurposing","score":0.8529999852180481},{"id":"https://openalex.org/keywords/therapeutic-target","display_name":"therapeutic target","score":0.4740000069141388}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.5874649882316589},{"id":"https://openalex.org/C2777807008","wikidata":"https://www.wikidata.org/wiki/Q87324999","display_name":"Serine protease","level":4,"score":0.5708547234535217},{"id":"https://openalex.org/C161624437","wikidata":"https://www.wikidata.org/wiki/Q1988322","display_name":"Small molecule","level":2,"score":0.5537089109420776},{"id":"https://openalex.org/C502942594","wikidata":"https://www.wikidata.org/wiki/Q3421914","display_name":"Cancer research","level":1,"score":0.54462730884552},{"id":"https://openalex.org/C2776414213","wikidata":"https://www.wikidata.org/wiki/Q183290","display_name":"Serine","level":3,"score":0.5322895646095276},{"id":"https://openalex.org/C2780192828","wikidata":"https://www.wikidata.org/wiki/Q181257","display_name":"Prostate cancer","level":3,"score":0.5209725499153137},{"id":"https://openalex.org/C2779013556","wikidata":"https://www.wikidata.org/wiki/Q181876","display_name":"Metastasis","level":3,"score":0.5034162402153015},{"id":"https://openalex.org/C121608353","wikidata":"https://www.wikidata.org/wiki/Q12078","display_name":"Cancer","level":2,"score":0.4771527647972107},{"id":"https://openalex.org/C2779256057","wikidata":"https://www.wikidata.org/wiki/Q16909647","display_name":"Tumor progression","level":3,"score":0.44526806473731995},{"id":"https://openalex.org/C24530287","wikidata":"https://www.wikidata.org/wiki/Q424204","display_name":"Transmembrane protein","level":3,"score":0.4246554672718048},{"id":"https://openalex.org/C96232424","wikidata":"https://www.wikidata.org/wiki/Q4118072","display_name":"Cancer cell","level":3,"score":0.41257452964782715},{"id":"https://openalex.org/C2776714187","wikidata":"https://www.wikidata.org/wiki/Q212410","display_name":"Protease","level":3,"score":0.3811385929584503},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.3376256823539734},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.28527140617370605},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.2506859302520752},{"id":"https://openalex.org/C104317684","wikidata":"https://www.wikidata.org/wiki/Q7187","display_name":"Gene","level":2,"score":0.11847329139709473},{"id":"https://openalex.org/C54355233","wikidata":"https://www.wikidata.org/wiki/Q7162","display_name":"Genetics","level":1,"score":0.09220883250236511},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.07963022589683533}],"mesh":[],"locations_count":1,"locations":[{"id":"doi:10.1158/1535-7163.c.6530952","doi":"https://doi.org/10.1158/1535-7163.c.6530952","is_oa":true,"landing_page_url":"https://doi.org/10.1158/1535-7163.c.6530952","pdf_url":null,"source":null,"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"submittedVersion","is_accepted":false,"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.6530952","doi":"https://doi.org/10.1158/1535-7163.c.6530952","is_oa":true,"landing_page_url":"https://doi.org/10.1158/1535-7163.c.6530952","pdf_url":null,"source":null,"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"American Association for Cancer Research","raw_type":"posted-content"},"sustainable_development_goals":[{"display_name":"Good health and well-being","score":0.9476000070571899,"id":"https://metadata.un.org/sdg/3"}],"study_designs":[],"awards":[{"id":"https://openalex.org/G374615898","display_name":"Invasion and Metastasis in Prostate Cancer","funder_award_id":"R01CA102365","funder_id":"https://openalex.org/F4320337351","funder_display_name":"National Cancer Institute"}],"funders":[{"id":"https://openalex.org/F4320308793","display_name":"Fred Hutchinson Cancer Research Center","ror":"https://ror.org/007ps6h72"},{"id":"https://openalex.org/F4320310094","display_name":"University of Washington","ror":"https://ror.org/00cvxb145"},{"id":"https://openalex.org/F4320337351","display_name":"National Cancer Institute","ror":"https://ror.org/040gcmg81"}],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":30,"referenced_works":["https://openalex.org/W1508240107","https://openalex.org/W1568669558","https://openalex.org/W1605638342","https://openalex.org/W1969275365","https://openalex.org/W1991001144","https://openalex.org/W1997319983","https://openalex.org/W1999836692","https://openalex.org/W2000719088","https://openalex.org/W2011819665","https://openalex.org/W2020459876","https://openalex.org/W2036902495","https://openalex.org/W2041011601","https://openalex.org/W2044984001","https://openalex.org/W2052641699","https://openalex.org/W2057211902","https://openalex.org/W2060481368","https://openalex.org/W2067602854","https://openalex.org/W2075906979","https://openalex.org/W2086342587","https://openalex.org/W2124040992","https://openalex.org/W2139018594","https://openalex.org/W2143249068","https://openalex.org/W2146754019","https://openalex.org/W2148581834","https://openalex.org/W2155300042","https://openalex.org/W2158294624","https://openalex.org/W2328379097","https://openalex.org/W2395085382","https://openalex.org/W2395872536","https://openalex.org/W4237363429"],"related_works":["https://openalex.org/W2169541841","https://openalex.org/W2317670781","https://openalex.org/W2183077554","https://openalex.org/W2593569319","https://openalex.org/W2800931251","https://openalex.org/W2133436538","https://openalex.org/W4392725448","https://openalex.org/W2976171612","https://openalex.org/W3030803456","https://openalex.org/W3109470043"],"abstract_inverted_index":{"Abstract":[0],"Hepsin":[1],"is":[2],"a":[3,31,105,115],"type":[4],"II":[5],"transmembrane":[6],"serine":[7,101],"protease":[8,102],"overexpressed":[9],"in":[10,104],"the":[11,38],"majority":[12],"of":[13,40,44,56,80,117,135],"human":[14,51,94],"prostate":[15,23,139],"cancers.":[16],"We":[17,48],"recently":[18],"demonstrated":[19],"that":[20],"hepsin":[21,45,52,72,136],"promotes":[22],"cancer":[24,140],"progression":[25,141],"and":[26,28,59,63,77,132,142],"metastasis":[27],"thus":[29],"represents":[30],"potential":[32],"therapeutic":[33],"target.":[34],"Here":[35],"we":[36],"report":[37],"identification":[39],"novel":[41],"small-molecule":[42],"inhibitors":[43,134],"catalytic":[46],"activity.":[47],"utilized":[49],"purified":[50],"for":[53,93],"high-throughput":[54],"screening":[55],"established":[57,92],"drug":[58],"chemical":[60],"diversity":[61],"libraries":[62],"identified":[64],"sixteen":[65],"inhibitory":[66],"compounds":[67,87,97,121],"with":[68,109],"IC50":[69],"values":[70],"against":[71],"ranging":[73],"from":[74],"0.23-2.31":[75],"\u03bcM":[76],"relative":[78],"selectivity":[79],"up":[81],"to":[82,114,127,137],"86-fold":[83],"or":[84,111],"greater.":[85],"Two":[86],"are":[88],"orally":[89],"administered":[90],"drugs":[91],"use.":[95],"Four":[96],"attenuated":[98],"hepsin-dependent":[99],"pericellular":[100],"activity":[103],"dose":[106],"dependent":[107],"manner":[108],"limited":[110],"no":[112],"cytotoxicity":[113],"range":[116],"cell":[118],"types.":[119],"These":[120],"may":[122],"be":[123],"used":[124],"as":[125],"leads":[126],"develop":[128],"even":[129],"more":[130],"potent":[131],"specific":[133],"prevent":[138],"metastasis.":[143],"[Mol":[144],"Cancer":[145],"Ther":[146],"2008;7(10):3343\u201351]":[147]},"counts_by_year":[],"updated_date":"2026-11-09T13:22:03.289127","created_date":"2023-04-05T00:00:00"}
