A protein tertiary structure mimetic modulator of the Hippo signalling pathway

Adihou H, Gopalakrishnan R, Förster T, Guéret SM, Gasper R, Geschwindner S, Carrillo García C, Karatas H, Pobbati AV, Vazquez-Chantada M, Davey P, Wassvik CM, Pang JKS, Soh BS, Hong W, Chiarparin E, Schade D, Plowright AT, Valeur E, Lemurell M, Grossmann TN, Waldmann H. (2020) Nat Commun

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The therapeutic regulation of gene transcription is a long-standing goal in pharmaceutical research. Transcription factors, proteins with key roles in this process, mediate their function mainly by protein-protein interactions, which makes them challenging targets. In a unique collaboration of academia and pharmaceutical industry scientists from AstraZeneca, the Vrije Universiteit (VU) Amsterdam and the Max Planck Institute of Molecular Physiology in Dortmund (MPI) have now developed a protein tertiary structure mimetic capable of inhibiting the interaction of the transcription factor (TF) TEAD with its co-repressor VGL4 and thereby activating proliferation via the Hippo pathway.

Proteomimetic binds to the transcription factor TEAD and thereby activates transcription of TEAD target genes of the Hippo signaling pathway
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