IntAct European Bioinformatics Institute IntAct intact http://www.ebi.ac.uk/ http://www.ebi.ac.uk/intact/query/${ac} EBI-[0-9]+|IA:[0-9]+ INTerAction database (IntAct) provides an open source database and toolkit for the storage, presentation and analysis of molecular interactions. http://www.ebi.ac.uk/intact European Bioinformatics Institute; Wellcome Trust Genome Campus; Hinxton, Cambridge; CB10 1SD; United Kingdom http://www.ebi.ac.uk/intact/ http://www.ebi.ac.uk/ andersen-2010-1 Regression of Castrate-Recurrent Prostate Cancer by a Small-Molecule Inhibitor of the Amino-Terminus Domain of the Androgen Receptor. human-lncap Human caucasian prostate carcinoma lncap Human caucasian prostate adenocarcinoma ch-ip chromatin immunoprecipitation assay ch-ip primer specific pcr primer specific pcr Andersen RJ., Mawji NR., Wang J., Wang G., Haile S., Myung JK., Watt K., Tam T., Yang YC., Banuelos CA., Williams DE., McEwan IJ., Wang Y., Sadar MD. Cancer - Interactions investigated in the context of cancer msadar@bcgsc.ca Cancer Cell (1535-6108) 2010 Only protein-protein interactions imex curation andersen-2010-3 Regression of Castrate-Recurrent Prostate Cancer by a Small-Molecule Inhibitor of the Amino-Terminus Domain of the Androgen Receptor. in vitro In vitro pull down pull down tag visualisation tag visualisation Andersen RJ., Mawji NR., Wang J., Wang G., Haile S., Myung JK., Watt K., Tam T., Yang YC., Banuelos CA., Williams DE., McEwan IJ., Wang Y., Sadar MD. Cancer - Interactions investigated in the context of cancer msadar@bcgsc.ca Cancer Cell (1535-6108) 2010 Only protein-protein interactions imex curation andersen-2010-4 Regression of Castrate-Recurrent Prostate Cancer by a Small-Molecule Inhibitor of the Amino-Terminus Domain of the Androgen Receptor. in vitro In vitro fps fluorescence polarization spectroscopy Fluorescence anisotropy FPS FPS Fluorescence anisotropy fps tag fluorescence tag visualisation by fluorescence tag fluorescence Andersen RJ., Mawji NR., Wang J., Wang G., Haile S., Myung JK., Watt K., Tam T., Yang YC., Banuelos CA., Williams DE., McEwan IJ., Wang Y., Sadar MD. Cancer - Interactions investigated in the context of cancer Fluorescent polarization. AR-LBD(His-GST)(Rat Androgen-Receptor Ligand-Binding Domain)is added to a fluorescently-tagged androgen ligand (Fluormone�) in the presence of competitor test compounds in microwell plates. The presence of effective competitors prevents the formation of a Fluormone/ AR-LBD(His-GST) complex resulting in a decrease of the polarization value due to ligand displacement caused by a competitor. Details of androgen receptor construct taken from manufacturer's website. msadar@bcgsc.ca Cancer Cell (1535-6108) 2010 Only protein-protein interactions imex curation andersen-2010-2 Regression of Castrate-Recurrent Prostate Cancer by a Small-Molecule Inhibitor of the Amino-Terminus Domain of the Androgen Receptor. human-lncap Human caucasian prostate carcinoma lncap Human caucasian prostate adenocarcinoma anti bait coip anti bait coimmunoprecipitation anti bait coip western blot western blot Immuno blot Immuno blot Andersen RJ., Mawji NR., Wang J., Wang G., Haile S., Myung JK., Watt K., Tam T., Yang YC., Banuelos CA., Williams DE., McEwan IJ., Wang Y., Sadar MD. Cancer - Interactions investigated in the context of cancer msadar@bcgsc.ca Cancer Cell (1535-6108) 2010 Only protein-protein interactions imex curation klk3_human_gene Human kallikrein-related peptidase 3 (KLK3) (PSA) gene gene human Homo sapiens Human andr_human Androgen receptor Dihydrotestosterone receptor Nuclear receptor subfamily 3 group C member 4 AR DHTR NR3C4 protein protein human Homo sapiens Human MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQSRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAAGPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAPYGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRLETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKLTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ cbp_human CREB-binding protein CREBBP CBP Histone lysine acetyltransferase CREBBP Protein-lysine acetyltransferase CREBBP protein protein human Homo sapiens Human MAENLLDGPPNPKRAKLSSPGFSANDSTDFGSLFDLENDLPDELIPNGGELGLLNSGNLVPDAASKHKQLSELLRGGSGSSINPGIGNVSASSPVQQGLGGQAQGQPNSANMASLSAMGKSPLSQGDSSAPSLPKQAASTSGPTPAASQALNPQAQKQVGLATSSPATSQTGPGICMNANFNQTHPGLLNSNSGHSLINQASQGQAQVMNGSLGAAGRGRGAGMPYPTPAMQGASSSVLAETLTQVSPQMTGHAGLNTAQAGGMAKMGITGNTSPFGQPFSQAGGQPMGATGVNPQLASKQSMVNSLPTFPTDIKNTSVTNVPNMSQMQTSVGIVPTQAIATGPTADPEKRKLIQQQLVLLLHAHKCQRREQANGEVRACSLPHCRTMKNVLNHMTHCQAGKACQVAHCASSRQIISHWKNCTRHDCPVCLPLKNASDKRNQQTILGSPASGIQNTIGSVGTGQQNATSLSNPNPIDPSSMQRAYAALGLPYMNQPQTQLQPQVPGQQPAQPQTHQQMRTLNPLGNNPMNIPAGGITTDQQPPNLISESALPTSLGATNPLMNDGSNSGNIGTLSTIPTAAPPSSTGVRKGWHEHVTQDLRSHLVHKLVQAIFPTPDPAALKDRRMENLVAYAKKVEGDMYESANSRDEYYHLLAEKIYKIQKELEEKRRSRLHKQGILGNQPALPAPGAQPPVIPQAQPVRPPNGPLSLPVNRMQVSQGMNSFNPMSLGNVQLPQAPMGPRAASPMNHSVQMNSMGSVPGMAISPSRMPQPPNMMGAHTNNMMAQAPAQSQFLPQNQFPSSSGAMSVGMGQPPAQTGVSQGQVPGAALPNPLNMLGPQASQLPCPPVTQSPLHPTPPPASTAAGMPSLQHTTPPGMTPPQPAAPTQPSTPVSSSGQTPTPTPGSVPSATQTQSTPTVQAAAQAQVTPQPQTPVQPPSVATPQSSQQQPTPVHAQPPGTPLSQAAASIDNRVPTPSSVASAETNSQQPGPDVPVLEMKTETQAEDTEPDPGESKGEPRSEMMEEDLQGASQVKEETDIAEQKSEPMEVDEKKPEVKVEVKEEEESSSNGTASQSTSPSQPRKKIFKPEELRQALMPTLEALYRQDPESLPFRQPVDPQLLGIPDYFDIVKNPMDLSTIKRKLDTGQYQEPWQYVDDVWLMFNNAWLYNRKTSRVYKFCSKLAEVFEQEIDPVMQSLGYCCGRKYEFSPQTLCCYGKQLCTIPRDAAYYSYQNRYHFCEKCFTEIQGENVTLGDDPSQPQTTISKDQFEKKKNDTLDPEPFVDCKECGRKMHQICVLHYDIIWPSGFVCDNCLKKTGRPRKENKFSAKRLQTTRLGNHLEDRVNKFLRRQNHPEAGEVFVRVVASSDKTVEVKPGMKSRFVDSGEMSESFPYRTKALFAFEEIDGVDVCFFGMHVQEYGSDCPPPNTRRVYISYLDSIHFFRPRCLRTAVYHEILIGYLEYVKKLGYVTGHIWACPPSEGDDYIFHCHPPDQKIPKPKRLQEWYKKMLDKAFAERIIHDYKDIFKQATEDRLTSAKELPYFEGDFWPNVLEESIKELEQEEEERKKEESTAASETTEGSQGDSKNAKKKNNKKTNKNKSSISRANKKKPSMPNVSNDLSQKLYATMEKHKEVFFVIHLHAGPVINTLPPIVDPDPLLSCDLMDGRDAFLTLARDKHWEFSSLRRSKWSTLCMLVELHTQGQDRFVYTCNECKHHVETRWHCTVCEDYDLCINCYNTKSHAHKMVKWGLGLDDEGSSQGEPQSKSPQESRRLSIQRCIQSLVHACQCRNANCSLPSCQKMKRVVQHTKGCKRKTNGGCPVCKQLIALCCYHAKHCQENKCPVPFCLNIKHKLRQQQIQHRLQQAQLMRRRMATMNTRNVPQQSLPSPTSAPPGTPTQQPSTPQTPQPPAQPQPSPVSMSPAGFPSVARTQPPTTVSTGKPTSQVPAPPPPAQPPPAAVEAARQIEREAQQQQHLYRVNINNSMPPGRTGMGTPGSQMAPVSLNVPRPNQVSGPVMPSMPPGQWQQAPLPQQQPMPGLPRPVISMQAQAAVAGPRMPSVQPPRSISPSALQDLLRTLKSPSSPQQQQQVLNILKSNPQLMAAFIKQRTAKYVANQPGMQPQPGLQSQPGMQPQPGMHQQPSLQNLNAMQAGVPRPGVPPQQQAMGGLNPQGQALNIMNPGHNPNMASMNPQYREMLRRQLLQQQQQQQQQQQQQQQQQQGSAGMAGGMAGHGQFQQPQGPGGYPPAMQQQQRMQQHLPLQGSSMGQMAAQMGQLGQMGQPGLGADSTPNIQQALQQRILQQQQMKQQIGSPGQPNPMSPQQHMLSGQPQASHLPGQQIATSLSNQVRSPAPVQSPRPQSQPPHSSPSPRIQPQPSPHHVSPQTGSPHPGLAVTMASSIDQGHLGNPEQSAMLPQLNTPSRSALSSELSLVGDTTGDTLEKFVEGL tmps2_human_gene Human TMPS2/TMPRSS2 gene gene gene human Homo sapiens Human t2fa_human General transcription factor IIF subunit 1 Transcription initiation factor IIF subunit alpha GTF2F1 RAP74 Transcription initiation factor RAP74 General transcription factor IIF 74 kDa subunit protein protein human Homo sapiens Human MAALGPSSQNVTEYVVRVPKNTTKKYNIMAFNAADKVNFATWNQARLERDLSNKKIYQEEEMPESGAGSEFNRKLREEARRKKYGIVLKEFRPEDQPWLLRVNGKSGRKFKGIKKGGVTENTSYYIFTQCPDGAFEAFPVHNWYNFTPLARHRTLTAEEAEEEWERRNKVLNHFSIMQQRRLKDQDQDEDEEEKEKRGRRKASELRIHDLEDDLEMSSDASDASGEEGGRVPKAKKKAPLAKGGRKKKKKKGSDDEAFEDSDDGDFEGQEVDYMSDGSSSSQEEPESKAKAPQQEEGPKGVDEQSDSSEESEEEKPPEEDKEEEEEKKAPTPQEKKRRKDSSEESDSSEESDIDSEASSALFMAKKKTPPKRERKPSGGSSRGNSRPGTPSAEGGSTSSTLRAAASKLEQGKRVSEMPAAKRLRLDTGPQSLSGKSTPQPPSGKTTPNSGDVQVTEDAVRRYLTRKPMTTKDLLKKFQTKKTGLSSEQTVNVLAQILKRLNPERKMINDKMHFSLKE fluormone_al_green Fluormone� AL Green, an androgen ligand, a fluorescent androgen analog. small molecule small molecule chemical synthesis Chemical synthesis (Chemical synthesis) a fluorescently-tagged androgen ligand (Fluormone� AL Green)- supplied by Invitrogen. It binds AR-LBD with a similar affinity as DHT. andr_rat Androgen receptor Ar Nr3c4 Dihydrotestosterone receptor Nuclear receptor subfamily 3 group C member 4 protein protein rat Rattus norvegicus (Rat) Rat MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREAIQNPGPRHPEAASIAPPGACLQQRQETSPRRRRRQQHPEDGSPQAHIRGTTGYLALEEEQQPSQQQSASEGHPESGCLPEPGAATAPGKGLPQQPPAPPDQDDSAAPSTLSLLGPTFPGLSSCSADIKDILSEAGTMQLLQQQQQQQQQQQQQQQQQQQQQQEVISEGSSSVRAREATGAPSSSKDSYLGGNSTISDSAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYASLLGGPPAVRPTPCAPLAECKGLSLDEGPGKGTEETAEYSSFKGGYAKGLEGESLGCSGSSEAGSSGTLEIPSSLSLYKSGAVDEAAAYQNRDYYNFPLALSGPPHPPPPTHPHARIKLENPSDYGSAWAAAAAQCRYGDLASLHGGSVAGPSTGSPPATASSSWHTLFTAEEGQLYGPGGGGGSSSPSDAGPVAPYGYTRPPQGLASQEGDFSASEVWYPGGVVNRVPYPSPSCVKSEMGPWMENYSGPYGDMRLDSTRDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGENSSAGSPTEDPSQKMTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ bicalutamide Bicalutamide, an androgen antagonist small molecule small molecule chemical synthesis Chemical synthesis (Chemical synthesis) r1881 R1881, Metribolone, a synthetic androgen small molecule small molecule chemical synthesis Chemical synthesis (Chemical synthesis) Also known as methyltrienolone. (17-methyloestra-4,9,11-trien-3-one,17b-ol). klk3-andr 958036 n/a 958040 unspecified role unspecified role prey prey n/a 958041 unspecified role unspecified role bait bait association association false false false R1881, a synthetic androgen. EPI-001:a small molecule derived from marine sponge extracts, that inhibits transactivation of the AR amino-terminal domain. R1881 treatment significantly increased AR and CBP binding to AREs in promoter and enhancer of PSA and TMPRSS2-ARE, which was significantly inhibited by EPI-001. Figure 2C. klk3-cbp 958036 n/a 958040 unspecified role unspecified role prey prey n/a 958042 unspecified role unspecified role bait bait association association false false false R1881, a synthetic androgen. EPI-001:a small molecule derived from marine sponge extracts, that inhibits transactivation of the AR amino-terminal domain. R1881 treatment significantly increased AR and CBP binding to AREs in promoter and enhancer of PSA and TMPRSS2-ARE, which was significantly inhibited by EPI-001. Figure 2C. tmps2-cbp 958036 n/a 958042 unspecified role unspecified role bait bait n/a 958043 unspecified role unspecified role prey prey association association false false false R1881, a synthetic androgen. EPI-001:a small molecule derived from marine sponge extracts, that inhibits transactivation of the AR amino-terminal domain. R1881 treatment significantly increased AR and CBP binding to AREs in promoter and enhancer of PSA and TMPRSS2-ARE, which was significantly inhibited by EPI-001. Figure 2D. tmps2-andr 958036 n/a 958043 unspecified role unspecified role prey prey n/a 958041 unspecified role unspecified role bait bait association association false false false R1881, a synthetic androgen. EPI-001:a small molecule derived from marine sponge extracts, that inhibits transactivation of the AR amino-terminal domain. R1881 treatment significantly increased AR and CBP binding to AREs in promoter and enhancer of PSA and TMPRSS2-ARE, which was significantly inhibited by EPI-001. Figure 2D. ar-cbp-1 958037 n/a 958041 unspecified role unspecified role bait bait af1_domain sufficient to bind sufficient binding region sufficient to bind range range range range false n/a 958042 unspecified role unspecified role prey prey n terminal domain sufficient to bind sufficient binding region sufficient to bind undetermined undetermined sequence position undetermined undetermined undetermined sequence position undetermined false physical association physical association false false false EPI-001:a small molecule derived from marine sponge extracts, that inhibits transactivation of the AR amino-terminal domain. EPI-001 inhibited interaction between AF-1 (AR NTD) and CBP-CTD recombinant proteins as well as AF-1 interaction with the large subunit of general transcription factor TFIIF (RAP74). Figure 3F. ar-t2fa 958037 n/a 958044 unspecified role unspecified role prey prey c terminal domain sufficient to bind sufficient binding region sufficient to bind c-term range C-terminal range c-term range c-term range C-terminal range c-term range false n/a 958041 unspecified role unspecified role bait bait af1_domain sufficient to bind sufficient binding region sufficient to bind range range range range false physical association physical association false false false EPI-001:a small molecule derived from marine sponge extracts, that inhibits transactivation of the AR amino-terminal domain. EPI-001 inhibited interaction between AF-1 (AR NTD) and CBP-CTD recombinant proteins as well as AF-1 interaction with the large subunit of general transcription factor TFIIF (RAP74). Figure 3F. andr-fluormone_bic 958038 n/a 958045 competitor competitor competitor prey prey n/a 958046 unspecified role unspecified role bait bait lbd domain sufficient to bind sufficient binding region sufficient to bind range range range range false region gst tag glutathione s tranferase tag glutathione S-tranferase tag glutathione S-tranferase tag gst tag undetermined undetermined sequence position undetermined undetermined undetermined sequence position undetermined false region his tag his tag Hexa-His-tag 6-His-tag Histidine-tag Hexa-His-tag Histidine-tag 6-His-tag undetermined undetermined sequence position undetermined undetermined undetermined sequence position undetermined false n/a 958047 unspecified role unspecified role prey prey physical association physical association false false false Fig 3B. Both R1881 and bicalutamide bound to the AR-LBD as expected. EPI-001 in the concentration range of 0.1 nM to 100 uM did not prevent ligand-binding. andr-fluormone_r1881 958038 n/a 958048 unspecified role unspecified role prey prey n/a 958045 competitor competitor competitor prey prey n/a 958046 unspecified role unspecified role bait bait lbd domain sufficient to bind sufficient binding region sufficient to bind range range range range false region gst tag glutathione s tranferase tag glutathione S-tranferase tag glutathione S-tranferase tag gst tag undetermined undetermined sequence position undetermined undetermined undetermined sequence position undetermined false region his tag his tag Hexa-His-tag 6-His-tag Histidine-tag Hexa-His-tag Histidine-tag 6-His-tag undetermined undetermined sequence position undetermined undetermined undetermined sequence position undetermined false physical association physical association false false false Fig 3B. Both R1881 and bicalutamide bound to the AR-LBD as expected. EPI-001 in the concentration range of 0.1 nM to 100 uM did not prevent ligand-binding. ar-cbp 958039 n/a 958042 unspecified role unspecified role bait bait n/a 958041 unspecified role unspecified role prey prey physical association physical association false false false R1881, a synthetic androgen. EPI-001:a small molecule derived from marine sponge extracts, that inhibits transactivation of the AR amino-terminal domain. EPI-001 prevents physical interaction between endogenous AR and CBP. Figure 3E. IL-6