Wnt breakers in colon cancer.
Beta-catenin and Tcf4 are the downstream effectors of the Wnt signaling cascade. In colorectal cancer, mutations in Wnt cascade genes such as APC lead to the inappropriate formation of beta-catenin/Tcf4 complexes. Earlier work has predicted that disruption of the beta-catenin/Tcf4 protein-protein interaction could revert the proliferative phenotype of colorectal cancer cells. In this issue of Cancer Cell, Shivdasani and colleagues have explored high-throughput screening of compound libraries in a search for small molecule inhibitors of the Wnt cascade. Ultimately, such inhibitors could become a novel class of smart anticancer drugs.
Clevers
Hans
H
Hubrecht Laboratory, 3584 CT Utrecht, The Netherlands. clevers@niob.knaw.nl
D025601:Adenomatous Polyposis Coli Protein; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D003110:Colonic Neoplasms / Q000378:metabolism; D020650:Combinatorial Chemistry Techniques; D003598:Cytoskeletal Proteins / Q000187:drug effects / Q000378:metabolism*; D004268:DNA-Binding Proteins / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D009154:Mutation; D011485:Protein Binding / Q000187:drug effects / Q000502:physiology; D011518:Proto-Oncogene Proteins / Q000187:drug effects / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects / Q000502:physiology; D051820:TCF Transcription Factors; D015534:Trans-Activators / Q000187:drug effects / Q000378:metabolism*; D058118:Transcription Factor 7-Like 2 Protein; D014157:Transcription Factors / Q000187:drug effects / Q000378:metabolism*; D051153:Wnt Proteins; D029961:Zebrafish Proteins; D051176:beta Catenin
D025601:Adenomatous Polyposis Coli Protein; D000970:Antineoplastic Agents; C495270:CTNNB1 protein, human; D003598:Cytoskeletal Proteins; D004268:DNA-Binding Proteins; D011518:Proto-Oncogene Proteins; D051820:TCF Transcription Factors; C544894:TCF7L2 protein, human; D015534:Trans-Activators; D058118:Transcription Factor 7-Like 2 Protein; D014157:Transcription Factors; D051153:Wnt Proteins; D029961:Zebrafish Proteins; D051176:beta Catenin