| http://purl.uniprot.org/citations/30581134 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/30581134 | http://www.w3.org/2000/01/rdf-schema#comment | "The Hippo pathway coordinates extracellular signals onto the control of tissue homeostasis and organ size. Hippo signaling primarily regulates the ability of Yap1 to bind and co-activate TEA domain (TEAD) transcription factors. Yap1 tightly binds to TEAD4 via a large flat interface, making the development of small-molecule orthosteric inhibitors highly challenging. Here, we report small-molecule TEAD⋅Yap inhibitors that rapidly and selectively form a covalent bond with a conserved cysteine located within the unique deep hydrophobic palmitate-binding pocket of TEADs. Inhibition of TEAD4 binding to Yap1 by these compounds was irreversible and occurred on a longer time scale. In mammalian cells, the compounds formed a covalent complex with TEAD4, inhibited its binding to Yap1, blocked its transcriptional activity, and suppressed expression of connective tissue growth factor. The compounds inhibited cell viability of patient-derived glioblastoma spheroids, making them suitable as chemical probes to explore Hippo signaling in cancer."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.chembiol.2018.11.010"xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Xu D."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Zhou D."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Si Y."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Meroueh S.O."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Corson T.W."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Wells C.D."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Gonzalez-Gutierrez G."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Pollok K.E."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Shannon H.E."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Bailey B.J."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Bum-Erdene K."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/author | "Ghozayel M.K."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/date | "2019"xsd:gYear |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/name | "Cell Chem Biol"xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/pages | "378-389.e13"xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/title | "Small-Molecule Covalent Modification of Conserved Cysteine Leads to Allosteric Inhibition of the TEAD⋅Yap Protein-Protein Interaction."xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://purl.uniprot.org/core/volume | "26"xsd:string |
| http://purl.uniprot.org/citations/30581134 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/30581134 |
| http://purl.uniprot.org/citations/30581134 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/30581134 |
| http://purl.uniprot.org/uniprot/#_Q15562-mappedCitation-30581134 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/30581134 |
| http://purl.uniprot.org/uniprot/Q15562 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/30581134 |