{"id":"https://openalex.org/W2124754264","doi":"https://doi.org/10.1158/1535-7163.targ-11-c94","title":"Abstract C94: A novel binding assay to identify inhibitors that bind to inactive forms of Bruton's tyrosine kinase based on fluorescence resonance energy transfer.","display_name":"Abstract C94: A novel binding assay to identify inhibitors that bind to inactive forms of Bruton's tyrosine kinase based on fluorescence resonance energy transfer.","publication_year":2011,"publication_date":"2011-11-01","ids":{"openalex":"https://openalex.org/W2124754264","doi":"https://doi.org/10.1158/1535-7163.targ-11-c94","mag":"2124754264"},"language":"en","primary_location":{"id":"doi:10.1158/1535-7163.targ-11-c94","doi":"https://doi.org/10.1158/1535-7163.targ-11-c94","is_oa":false,"landing_page_url":"https://doi.org/10.1158/1535-7163.targ-11-c94","pdf_url":null,"source":{"id":"https://openalex.org/S48437117","display_name":"Molecular Cancer Therapeutics","issn_l":"1535-7163","issn":["1535-7163","1538-8514"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","dongbi-b","doyens","jufo-1","ki-jl-1","medline","norway-2","poland-140","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":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Molecular Cancer Therapeutics","raw_type":"journal-article"},"volume":null,"type":"conference-abstract","is_traditional":false,"indexed_in":["crossref"],"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/A5081638860","display_name":"Tokiko Asami","orcid":"https://orcid.org/0000-0001-6783-4091","observed_orcids":["https://orcid.org/0000-0001-6783-4091"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Tokiko Asami","raw_affiliation_strings":["1Carna Biosciences, Inc., Kobe, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1Carna Biosciences, Inc., Kobe, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5028877245","display_name":"Wataru Kawahata","orcid":"https://orcid.org/0000-0002-2305-7363","observed_orcids":["https://orcid.org/0000-0002-2305-7363"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Wataru Kawahata","raw_affiliation_strings":["1Carna Biosciences, Inc., Kobe, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1Carna Biosciences, Inc., Kobe, Japan","institution_ids":[]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5011509062","display_name":"Masaaki Sawa","orcid":"https://orcid.org/0000-0002-0077-2188","observed_orcids":["https://orcid.org/0000-0002-0077-2188"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Masaaki Sawa","raw_affiliation_strings":["1Carna Biosciences, Inc., Kobe, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1Carna Biosciences, Inc., Kobe, Japan","institution_ids":[]}]}],"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":1,"citation_normalized_percentile":null,"cited_by_percentile_year":null,"biblio":{"volume":"10","issue":"11_Supplement","first_page":"C94","last_page":"C94"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10169","display_name":"Protein Kinase Regulation and GTPase Signaling","score":0.34450000524520874,"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/T10169","display_name":"Protein Kinase Regulation and GTPase Signaling","score":0.34450000524520874,"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/T10211","display_name":"Computational Drug Discovery Methods","score":0.13379999995231628,"subfield":{"id":"https://openalex.org/subfields/3002","display_name":"Drug Discovery"},"field":{"id":"https://openalex.org/fields/30","display_name":"Pharmacology, Toxicology and Pharmaceutics"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T11157","display_name":"Chronic Lymphocytic Leukemia Research","score":0.03370000049471855,"subfield":{"id":"https://openalex.org/subfields/2720","display_name":"Hematology"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/bruton-tyrosine-kinase","display_name":"Bruton's tyrosine kinase","score":0.996999979019165},{"id":"https://openalex.org/keywords/bruton-tyrosine-kinase-inhibitors","display_name":"BTK inhibitors","score":0.7080000042915344},{"id":"https://openalex.org/keywords/tr-fret","display_name":"time-resolved fluorescence resonance energy transfer","score":0.8130000233650208},{"id":"https://openalex.org/keywords/competitive-binding-assay","display_name":"competitive binding assay","score":0.8199999928474426},{"id":"https://openalex.org/keywords/kinase-dephosphorylation","display_name":"kinase dephosphorylation","score":0.6740000247955322},{"id":"https://openalex.org/keywords/kinase-autophosphorylation","display_name":"kinase autophosphorylation","score":0.7670000195503235},{"id":"https://openalex.org/keywords/kinase-inhibitor-selectivity","display_name":"kinase selectivity","score":0.5699999928474426},{"id":"https://openalex.org/keywords/high-throughput-screening","display_name":"high-throughput screening","score":0.7200000286102295},{"id":"https://openalex.org/keywords/b-cell-activation","display_name":"B cell activation","score":0.47200000286102295},{"id":"https://openalex.org/keywords/mast-cell-activation","display_name":"mast cell activation","score":0.9010000228881836},{"id":"https://openalex.org/keywords/b-cell-malignancies","display_name":"B-cell malignancies","score":0.5249999761581421},{"id":"https://openalex.org/keywords/asthma","display_name":"asthma","score":0.7149999737739563},{"id":"https://openalex.org/keywords/rheumatoid-arthritis","display_name":"rheumatoid arthritis","score":0.9990000128746033}],"concepts":[{"id":"https://openalex.org/C90059517","wikidata":"https://www.wikidata.org/wiki/Q423572","display_name":"Bruton's tyrosine kinase","level":4,"score":0.9868569374084473},{"id":"https://openalex.org/C42362537","wikidata":"https://www.wikidata.org/wiki/Q87099740","display_name":"Tyrosine kinase","level":3,"score":0.6577125787734985},{"id":"https://openalex.org/C184235292","wikidata":"https://www.wikidata.org/wiki/Q421851","display_name":"Kinase","level":2,"score":0.5864511728286743},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.5521303415298462},{"id":"https://openalex.org/C96305047","wikidata":"https://www.wikidata.org/wiki/Q367473","display_name":"F\u00f6rster resonance energy transfer","level":3,"score":0.527561366558075},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.45837947726249695},{"id":"https://openalex.org/C101544691","wikidata":"https://www.wikidata.org/wiki/Q420511","display_name":"Receptor tyrosine kinase","level":3,"score":0.41459792852401733},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.33273017406463623},{"id":"https://openalex.org/C62478195","wikidata":"https://www.wikidata.org/wiki/Q828130","display_name":"Signal transduction","level":2,"score":0.3227250277996063},{"id":"https://openalex.org/C91881484","wikidata":"https://www.wikidata.org/wiki/Q191807","display_name":"Fluorescence","level":2,"score":0.18438711762428284},{"id":"https://openalex.org/C121332964","wikidata":"https://www.wikidata.org/wiki/Q413","display_name":"Physics","level":0,"score":0.0},{"id":"https://openalex.org/C62520636","wikidata":"https://www.wikidata.org/wiki/Q944","display_name":"Quantum mechanics","level":1,"score":0.0}],"mesh":[],"locations_count":1,"locations":[{"id":"doi:10.1158/1535-7163.targ-11-c94","doi":"https://doi.org/10.1158/1535-7163.targ-11-c94","is_oa":false,"landing_page_url":"https://doi.org/10.1158/1535-7163.targ-11-c94","pdf_url":null,"source":{"id":"https://openalex.org/S48437117","display_name":"Molecular Cancer Therapeutics","issn_l":"1535-7163","issn":["1535-7163","1538-8514"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","dongbi-b","doyens","jufo-1","ki-jl-1","medline","norway-2","poland-140","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":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Molecular Cancer Therapeutics","raw_type":"journal-article"}],"best_oa_location":null,"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being","score":0.5683000087738037}],"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/W1976433367","https://openalex.org/W2075177981","https://openalex.org/W2078241524","https://openalex.org/W2571078282","https://openalex.org/W2954187991","https://openalex.org/W2327194176","https://openalex.org/W2171594021","https://openalex.org/W2986142356","https://openalex.org/W2019216438","https://openalex.org/W4281615863"],"abstract_inverted_index":{"Abstract":[0],"Bruton's":[1],"tyrosine":[2,14],"kinase":[3,100,140,146,178],"(Btk)":[4],"is":[5,17,42,79,189],"a":[6,74,83,161,223,234,262,349,363],"member":[7],"of":[8,12,19,50,112,125,149,167,170,197,219,230,251,308,372,381,401,410,426],"the":[9,20,24,36,47,88,110,116,123,143,184,194,227,249,252,270,286,327,342,355,369,376,382,407,427],"Tec":[10],"family":[11,147],"non-receptor":[13],"kinases.":[15],"Btk":[16,41,76,177,266,309,411],"one":[18],"crucial":[21],"kinases":[22],"for":[23,46],"B":[25,63],"cell":[26,33,59,64],"maturation":[27],"and":[28,67,269,288,320,329,395,433],"also":[29],"involved":[30],"in":[31,122,183,415],"mast":[32,58],"activation":[34],"through":[35],"high-affinity":[37],"IgE":[38],"receptor.":[39],"Therefore":[40],"an":[43,216],"attractive":[44],"target":[45],"potential":[48],"treatment":[49],"multiple":[51],"therapeutic":[52],"areas":[53],"that":[54,175,212,247],"involve":[55],"B-cell":[56],"and/or":[57],"activation,":[60],"such":[61],"as":[62,87,209],"malignances,":[65],"asthma,":[66],"rheumatoid":[68],"arthritis.":[69],"In":[70],"order":[71],"to":[72,81,104,138,164,191,193,215,256,284,305,340,362,387],"develop":[73,222],"selective":[75,85],"inhibitor,":[77],"it":[78],"important":[80],"identify":[82,105,165],"highly":[84],"compound":[86],"drug":[89],"discovery":[90],"starting":[91],"point.":[92],"Generally,":[93],"activity-based":[94,117],"high-throughput":[95],"screening":[96,224],"(HTS)":[97],"using":[98],"active":[99,156],"has":[101],"been":[102,181],"used":[103],"hit":[106],"compounds":[107,174,337],"by":[108,332],"measuring":[109,333],"inhibition":[111],"substrate":[113,334],"phosphorylation.":[114,335],"However,":[115],"HTS":[118],"campaign":[119],"frequently":[120],"results":[121],"enrichment":[124],"classical":[126],"ATP":[127,276],"competitive":[128,235,364],"inhibitors,":[129],"which":[130],"would":[131],"often":[132],"require":[133],"considerable":[134],"medicinal":[135],"chemistry":[136],"efforts":[137],"increase":[139],"selectivity,":[141],"because":[142],"human":[144],"protein":[145,267,272],"consists":[148],"over":[150],"500":[151],"enzymes":[152],"with":[153,205,275,279,317,375,392],"very":[154],"similar":[155],"sites.":[157],"Here":[158],"we":[159,200,232,367],"describe":[160],"novel":[162,403],"approach":[163],"inhibitors":[166],"inactive":[168,195,217,228,408],"form":[169,196,218,229,409],"Btk.":[171,220,258],"Method:":[172],"Several":[173,336],"inhibit":[176],"activity":[179,299],"have":[180],"described":[182],"literature.":[185],"One":[186],"compound,":[187],"CGI1746":[188,203,254,315,357],"reported":[190],"bind":[192,214],"Btk,":[198,231],"so":[199],"synthesized":[201,312,384],"FITC-labeled":[202,253,314,356],"derivatives":[204,316,358],"various":[206,313],"linker":[207],"groups":[208],"fluorescent":[210],"probes":[211,374,383],"preferentially":[213],"To":[221,352],"system":[225],"targeting":[226,406],"designed":[233],"binding":[236,250,365,404],"assay":[237,378,405],"based":[238],"on":[239],"time-resolved":[240],"fluorescence":[241],"resonance":[242],"energy":[243],"transfer":[244],"(TR-FRET)":[245],"platform":[246],"measures":[248],"probe":[255],"biotinylated":[257,265],"Result:":[259],"We":[260,311],"produced":[261],"single":[263],"endogenous":[264],"(BTN-Btk),":[268],"BTN-Btk":[271,290,294,331],"was":[273],"treated":[274],"(autophosphorylation)":[277],"or":[278],"Lambda":[280],"Protein":[281],"Phosophatase":[282],"(dephosphorylation)":[283],"obtain":[285],"activated":[287,328],"unactivated":[289,330],"respectively.":[291],"Interestingly,":[292],"dephosphorylated":[293],"still":[295],"showed":[296],"weak":[297],"catalytic":[298],"indicating":[300],"phosphatase-treatment":[301],"might":[302],"not":[303],"able":[304],"remove":[306],"phosphates":[307],"completely.":[310],"different":[318],"linkers,":[319],"determined":[321,368],"their":[322],"IC50":[323],"value":[324,371],"against":[325],"both":[326],"were":[338,385],"found":[339,386],"maintain":[341],"original":[343],"inhibitory":[344],"potency":[345],"even":[346],"after":[347],"introducing":[348],"FITC":[350],"fluorophore.":[351],"test":[353],"if":[354],"can":[359],"be":[360,388,413],"applied":[361],"assay,":[366],"Kd":[370],"each":[373],"TR-FRET":[377],"platform.":[379],"Most":[380],"excellent":[389],"FRET":[390],"acceptors":[391],"high":[393],"affinity":[394],"low":[396],"background":[397],"signals.":[398],"Detailed":[399],"data":[400],"this":[402,416],"will":[412],"presented":[414],"poster.":[417],"Citation":[418],"Format:":[419],"{Authors}.":[420],"{Abstract":[421],"title}":[422],"[abstract].":[423],"In:":[424],"Proceedings":[425],"AACR-NCI-EORTC":[428],"International":[429],"Conference:":[430],"Molecular":[431],"Targets":[432],"Cancer":[434,446],"Therapeutics;":[435],"2011":[436],"Nov":[437],"12-16;":[438],"San":[439],"Francisco,":[440],"CA.":[441],"Philadelphia":[442],"(PA):":[443],"AACR;":[444],"Mol":[445],"Ther":[447],"2011;10(11":[448],"Suppl):Abstract":[449],"nr":[450],"C94.":[451]},"counts_by_year":[{"year":2015,"cited_by_count":1}],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2016-06-24T00:00:00"}
