{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Nalli M"],"funding":["Associazione Italiana per la Ricerca sul Cancro","Ministero della Salute","Università Cattolica del Sacro Cuore","China Academy of Traditional Chinese Medicine","Sapienza Università di Roma","Fondazione Umberto Veronesi","Institut Pasteur Italy"],"pagination":["1087-1103"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC10353061"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["6(7)"],"pubmed_abstract":["Despite intensive efforts, no inhibitors of the Wnt/β-catenin signaling pathway have been approved so far for the clinical treatment of cancer. We synthesized novel <i>N</i>-(heterocyclylphenyl)benzenesulfonamides as β-catenin inhibitors. Compounds <b>5</b>-<b>10</b> showed strong inhibition of the luciferase activity. Compounds <b>5</b> and <b>6</b> inhibited the MDA-MB-231, HCC1806, and HCC1937 TNBC cells. Compound <b>9</b> induced in vitro cell death in SW480 and HCT116 cells and in vivo tumorigenicity of a human colorectal cancer line HCT116. In a co-immunoprecipitation study in HCT116 cells transfected with Myc-tagged T-cell factor 4 (Tcf-4), compound <b>9</b> abrogated the association between β-catenin and Tcf-4. The crystallographic analysis of the β-catenin Armadillo repeats domain"],"journal":["ACS pharmacology & translational science"],"pubmed_title":["Novel &lt;i&gt;N&lt;/i&gt;-(Heterocyclylphenyl)benzensulfonamide Sharing an Unreported Binding Site with T-Cell Factor 4 at the β-Catenin Armadillo Repeats Domain as an Anticancer Agent."],"pmcid":["PMC10353061"],"funding_grant_id":["RM120172A7EAD07C","IG 2020  24703","IG 2021 25833","RG120172AD61BE52","MFGA 21899","RM11916B5598E3C4","RG12117A61923A6F","A1-U21-205-01010202","RG11816428A9B4D5","RM12117A85D9076B"],"pubmed_authors":["Wen Y","Sebastiani J","Masci D","La Regina G","Sette C","Capelli D","D'Angelo S","Stornaiuolo M","Liu T","D'Ambrosio M","Liu X","Di Pastena F","Biagioni S","Puxeddu M","Ripa S","Naro C","Urbani A","Coluccia A","Parisi A","Dondio G","Sorato A","Canettieri G","Nalli M","Pastore A","Bigogno C","Silvestri R","Montanari R","Di Magno L","Orlando V"],"additional_accession":[]},"is_claimable":false,"name":"Novel &lt;i&gt;N&lt;/i&gt;-(Heterocyclylphenyl)benzensulfonamide Sharing an Unreported Binding Site with T-Cell Factor 4 at the β-Catenin Armadillo Repeats Domain as an Anticancer Agent.","description":"Despite intensive efforts, no inhibitors of the Wnt/β-catenin signaling pathway have been approved so far for the clinical treatment of cancer. We synthesized novel <i>N</i>-(heterocyclylphenyl)benzenesulfonamides as β-catenin inhibitors. Compounds <b>5</b>-<b>10</b> showed strong inhibition of the luciferase activity. Compounds <b>5</b> and <b>6</b> inhibited the MDA-MB-231, HCC1806, and HCC1937 TNBC cells. Compound <b>9</b> induced in vitro cell death in SW480 and HCT116 cells and in vivo tumorigenicity of a human colorectal cancer line HCT116. In a co-immunoprecipitation study in HCT116 cells transfected with Myc-tagged T-cell factor 4 (Tcf-4), compound <b>9</b> abrogated the association between β-catenin and Tcf-4. The crystallographic analysis of the β-catenin Armadillo repeats domain","dates":{"release":"2023-01-01T00:00:00Z","publication":"2023 Jul","modification":"2026-06-02T04:36:49.065Z","creation":"2024-10-16T07:23:54.639Z"},"accession":"S-EPMC10353061","cross_references":{"pubmed":["37470018"],"doi":["10.1021/acsptsci.3c00092"]}}