Nature Communications (Oct 2020)
A protein tertiary structure mimetic modulator of the Hippo signalling pathway
- Hélène Adihou,
- Ranganath Gopalakrishnan,
- Tim Förster,
- Stéphanie M. Guéret,
- Raphael Gasper,
- Stefan Geschwindner,
- Carmen Carrillo García,
- Hacer Karatas,
- Ajaybabu V. Pobbati,
- Mercedes Vazquez‐Chantada,
- Paul Davey,
- Carola M. Wassvik,
- Jeremy Kah Sheng Pang,
- Boon Seng Soh,
- Wanjin Hong,
- Elisabetta Chiarparin,
- Dennis Schade,
- Alleyn T. Plowright,
- Eric Valeur,
- Malin Lemurell,
- Tom N. Grossmann,
- Herbert Waldmann
Affiliations
- Hélène Adihou
- Medicinal Chemistry, Research and Early Development Cardiovascular, Renal and Metabolism, BioPharmaceuticals R&D, AstraZeneca
- Ranganath Gopalakrishnan
- Medicinal Chemistry, Research and Early Development Cardiovascular, Renal and Metabolism, BioPharmaceuticals R&D, AstraZeneca
- Tim Förster
- AstraZeneca-MPI Satellite Unit
- Stéphanie M. Guéret
- Medicinal Chemistry, Research and Early Development Cardiovascular, Renal and Metabolism, BioPharmaceuticals R&D, AstraZeneca
- Raphael Gasper
- Max Planck Institute for Molecular Physiology
- Stefan Geschwindner
- Structure & Biophysics, Discovery Sciences, R&D, AstraZeneca
- Carmen Carrillo García
- Department of Pharmaceutical and Medicinal Chemistry, Christian-Albrechts-University of Kiel
- Hacer Karatas
- Max Planck Institute for Molecular Physiology
- Ajaybabu V. Pobbati
- Department of Multi-Modal Molecular (M3) Biology, A*STAR Institute of Molecular and Cell Biology
- Mercedes Vazquez‐Chantada
- Mechanistic Biology & Profiling, BioPharmaceuticals R&D, AstraZeneca
- Paul Davey
- Medicinal Chemistry, Oncology R&D, AstraZeneca
- Carola M. Wassvik
- Medicinal Chemistry, Research and Early Development Cardiovascular, Renal and Metabolism, BioPharmaceuticals R&D, AstraZeneca
- Jeremy Kah Sheng Pang
- Disease Modelling and Therapeutics Laboratory, A*STAR Institute of Molecular and Cell Biology
- Boon Seng Soh
- Disease Modelling and Therapeutics Laboratory, A*STAR Institute of Molecular and Cell Biology
- Wanjin Hong
- Department of Multi-Modal Molecular (M3) Biology, A*STAR Institute of Molecular and Cell Biology
- Elisabetta Chiarparin
- Medicinal Chemistry, Oncology R&D, AstraZeneca
- Dennis Schade
- Department of Pharmaceutical and Medicinal Chemistry, Christian-Albrechts-University of Kiel
- Alleyn T. Plowright
- Medicinal Chemistry, Research and Early Development Cardiovascular, Renal and Metabolism, BioPharmaceuticals R&D, AstraZeneca
- Eric Valeur
- Medicinal Chemistry, Research and Early Development Cardiovascular, Renal and Metabolism, BioPharmaceuticals R&D, AstraZeneca
- Malin Lemurell
- Medicinal Chemistry, Research and Early Development Cardiovascular, Renal and Metabolism, BioPharmaceuticals R&D, AstraZeneca
- Tom N. Grossmann
- Department of Chemistry and Pharmaceutical Sciences, VU University Amsterdam
- Herbert Waldmann
- Max Planck Institute for Molecular Physiology
- DOI
- https://doi.org/10.1038/s41467-020-19224-8
- Journal volume & issue
-
Vol. 11,
no. 1
pp. 1 – 10
Abstract
Targeting the interaction between transcription factor TEAD and its co-repressor VGL4 is an attractive strategy to chemically modulate Hippo signaling. Here, the authors develop a proteomimetic with stabilized tertiary structure that inhibits the TEAD:VGL4 interaction in vitro and in cells.
