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/ Targeting androgen receptor and JunD interaction for prevention of prostate cancer progression. Targeting androgen receptor and JunD interaction for prevention of prostate cancer progression. Prostate (0270-4137) 2014 imex curation Mehraein-Ghomi F., Kegel S.J., Church D.R., Schmidt J.S., Reuter Q.R., Saphner E.L., Basu H.S., Wilding G. Cancer - Interactions investigated in the context of cancer Affinomics - Interactions curated for the Affinomics consortium. gxw@medicine.wisc.edu 05-Jan-2015: Contacted by IntAct-Help. Only protein-protein interactions human-lncap Human caucasian prostate carcinoma lncap Human caucasian prostate adenocarcinoma pla proximity ligation assay pELISA pELISA PLA antibody detection identification by antibody antibody detection Mehraein-Ghomi F., Kegel S.J., Church D.R., Schmidt J.S., Reuter Q.R., Saphner E.L., Basu H.S., Wilding G. Cancer - Interactions investigated in the context of cancer gxw@medicine.wisc.edu Accepted 2014-DEC-09 by ORCHARD Prostate (0270-4137) 2014 Only protein-protein interactions imex curation Targeting androgen receptor and JunD interaction for prevention of prostate cancer progression. Targeting androgen receptor and JunD interaction for prevention of prostate cancer progression. Prostate (0270-4137) 2014 imex curation Mehraein-Ghomi F., Kegel S.J., Church D.R., Schmidt J.S., Reuter Q.R., Saphner E.L., Basu H.S., Wilding G. Cancer - Interactions investigated in the context of cancer Affinomics - Interactions curated for the Affinomics consortium. gxw@medicine.wisc.edu 05-Jan-2015: Contacted by IntAct-Help. Only protein-protein interactions human-hep_3b Homo sapiens hepatocellular carcinoma (HCC) cells (p53-null). hep_3b human hepatocellular carcinoma (HCC) cells (p53-null). split luciferase complementation split luciferase complementation tag luciferase tag visualisation by luciferase assay tag luciferase Mehraein-Ghomi F., Kegel S.J., Church D.R., Schmidt J.S., Reuter Q.R., Saphner E.L., Basu H.S., Wilding G. Cancer - Interactions investigated in the context of cancer Gaussia luciferase reconstitution assay Gaussia luciferase is a naturally secreted protein by the copepod, Gaussia princeps. At 19kD, it is the smallest known luciferase and its catalytic properties make it one of the “brightest” known. (pmid:17099704) gxw@medicine.wisc.edu Accepted 2014-DEC-09 by ORCHARD Prostate (0270-4137) 2014 Only protein-protein interactions imex curation Targeting androgen receptor and JunD interaction for prevention of prostate cancer progression. Targeting androgen receptor and JunD interaction for prevention of prostate cancer progression. Prostate (0270-4137) 2014 imex curation Mehraein-Ghomi F., Kegel S.J., Church D.R., Schmidt J.S., Reuter Q.R., Saphner E.L., Basu H.S., Wilding G. Cancer - Interactions investigated in the context of cancer Affinomics - Interactions curated for the Affinomics consortium. gxw@medicine.wisc.edu 05-Jan-2015: Contacted by IntAct-Help. Only protein-protein interactions in vitro In vitro fps fluorescence polarization spectroscopy Fluorescence anisotropy FPS FPS Fluorescence anisotropy fps tag fluorescence tag visualisation by fluorescence tag fluorescence Mehraein-Ghomi F., Kegel S.J., Church D.R., Schmidt J.S., Reuter Q.R., Saphner E.L., Basu H.S., Wilding G. Cancer - Interactions investigated in the context of cancer This interaction was lifted from anderesn-2010-4 with alteration of roles. I have not made another interaction for compound GWARJD22 as there is no info (no google result, no structure in this paper) about it - and as it is being not used any further in this publication, seems a waste of time... 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. Origins and details of constructs used obtained from Invitrogen website. gxw@medicine.wisc.edu Accepted 2014-DEC-09 by ORCHARD Prostate (0270-4137) 2014 Only protein-protein interactions imex curation andr_human Androgen receptor Dihydrotestosterone receptor Nuclear receptor subfamily 3 group C member 4 AR DHTR NR3C4 protein protein human Homo sapiens Human MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQSRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAAGPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAPYGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRLETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKLTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ DIP protein P10275 original sequence version: 220 DIP protein P10275-1 original sequence version: 213 DIP protein P10275 original sequence version: 216 DIP protein P10275 original sequence version: 143 DIP protein P10275 original sequence version: 174 DIP protein P10275 original sequence version: 169 DIP protein P10275 original sequence version: 188 DIP protein P10275-1 original sequence version: 188 DIP protein P10275 original sequence version: 196 DIP protein P10275 original sequence version: 217 DIP protein P10275-1 original sequence version: 217 DIP protein P10275-1 original sequence version: 207 A73432C55D39AE06 andr_rat Androgen receptor Ar Nr3c4 Dihydrotestosterone receptor Nuclear receptor subfamily 3 group C member 4 protein protein rat Rattus norvegicus (Rat) Rat MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREAIQNPGPRHPEAASIAPPGACLQQRQETSPRRRRRQQHPEDGSPQAHIRGTTGYLALEEEQQPSQQQSASEGHPESGCLPEPGAATAPGKGLPQQPPAPPDQDDSAAPSTLSLLGPTFPGLSSCSADIKDILSEAGTMQLLQQQQQQQQQQQQQQQQQQQQQQEVISEGSSSVRAREATGAPSSSKDSYLGGNSTISDSAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYASLLGGPPAVRPTPCAPLAECKGLSLDEGPGKGTEETAEYSSFKGGYAKGLEGESLGCSGSSEAGSSGTLEIPSSLSLYKSGAVDEAAAYQNRDYYNFPLALSGPPHPPPPTHPHARIKLENPSDYGSAWAAAAAQCRYGDLASLHGGSVAGPSTGSPPATASSSWHTLFTAEEGQLYGPGGGGGSSSPSDAGPVAPYGYTRPPQGLASQEGDFSASEVWYPGGVVNRVPYPSPSCVKSEMGPWMENYSGPYGDMRLDSTRDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGENSSAGSPTEDPSQKMTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ 43F4064759FDCBED bicalutamide Bicalutamide, an androgen antagonist small molecule small molecule chemical synthesis Chemical synthesis (Chemical synthesis) 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. a fluorescently-tagged androgen ligand (Fluormone� AL Green)- supplied by Invitrogen. It binds AR-LBD with a similar affinity as DHT. jund_human Transcription factor jun-D JUND protein protein human Homo sapiens Human METPFYGDEALSGLGGGASGSGGSFASPGRLFPGAPPTAAAGSMMKKDALTLSLSEQVAAALKPAAAPPPTPLRADGAPSAAPPDGLLASPDLGLLKLASPELERLIIQSNGLVTTTPTSSQFLYPKVAASEEQEFAEGFVKALEDLHKQNQLGAGAAAAAAAAAAGGPSGTATGSAPPGELAPAAAAPEAPVYANLSSYAGGAGGAGGAATVAFAAEPVPFPPPPPPGALGPPRLAALKDEPQTVPDVPSFGESPPLSPIDMDTQERIKAERKRLRNRIAASKCRKRKLERISRLEEKVKTLKSQNTELASTASLLREQVAQLKQKVLSHVNSGCQLLPQHQVPAY DIP protein P17535 original sequence version: 147 DIP protein P17535 original sequence version: 119 FE85A1AA2B5B9597 ar-jund 2 4 unspecified role unspecified role neutral component neutral component n_terminus_gluc1 (n-terminal part of of gaussia luciferase) luciferase tag luciferase tag n-term range n-terminal range n-term range n-term range n-terminal range n-term range 8 unspecified role unspecified role neutral component neutral component c_terminus_gluc2 (c-terminal part of gaussia luciferase) luciferase tag luciferase tag c-term range C-terminal range c-term range c-term range C-terminal range c-term range physical association physical association Fig 1 ar-bicalutamide 3 6 competitor competitor competitor prey prey 5 unspecified role unspecified role bait bait 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 lbd domain sufficient to bind sufficient binding region sufficient to bind range range range range 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 7 unspecified role unspecified role prey prey physical association physical association Fig 2 Bicalutamide, an anti-androgen, is a "positive" control. The compound GWARJD22 also gave a decrease in polarisation values. ar-bicalutamide-1 3 5 unspecified role unspecified role bait bait 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 lbd domain sufficient to bind sufficient binding region sufficient to bind range range range range 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 7 unspecified role unspecified role prey prey physical association physical association Fig 2 Bicalutamide, an anti-androgen, is a positive control. ar-jund-1 1 4 unspecified role unspecified role neutral component neutral component 8 unspecified role unspecified role neutral component neutral component proximity proximity close-contact colocalization neighbourhood interaction Fig. 4 synthetic androgen R1881 lead compound GWARJD10 (structure shown in fig 3)