A protein tertiary structure mimetic modulator of the Hippo signalling pathway

Autor: 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

Publikováno v: Nature Communications, Vol 11, Iss 1, Pp 1-10 (2020)

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 TEA

Externí odkaz: https://doaj.org/article/34105208594045348e3822ea97b488f7

AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity

Autor: Jacqueline H. L. Fok, Antonio Ramos-Montoya, Mercedes Vazquez-Chantada, Paul W. G. Wijnhoven, Valeria Follia, Neil James, Paul M. Farrington, Ankur Karmokar, Sophie E. Willis, Jonathan Cairns, Jenni Nikkilä, David Beattie, Gillian M. Lamont, M. Raymond V. Finlay, Joanne Wilson, Aaron Smith, Lenka Oplustil O’Connor, Stephanie Ling, Stephen E. Fawell, Mark J. O’Connor, Simon J. Hollingsworth, Emma Dean, Frederick W. Goldberg, Barry R. Davies, Elaine B. Cadogan

Publikováno v: Nature Communications, Vol 10, Iss 1, Pp 1-15 (2019)

DNA-dependent protein kinase (DNA-PK) plays a major role in the DNA damage response upon double-strand break formation. Here, the authors show that the DNA-PK inhibitor AZD7648, enhances the activity of radiotherapy, chemotherapy and the PARP inhibit

Externí odkaz: https://doaj.org/article/7547983126794fc0a17cf1c4d462a298

Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8H-purin-8-one Inhibitors of DNA-PK

Autor: Frederick W. Goldberg, Attilla K. T. Ting, David Beattie, Gillian M. Lamont, Charlene Fallan, M. Raymond V. Finlay, Beth Williamson, Marianne Schimpl, Alexander R. Harmer, Oladipupo B. Adeyemi, Pär Nordell, Anna S. Cronin, Mercedes Vazquez-Chantada, Derek Barratt, Antonio Ramos-Montoya, Elaine B. Cadogan, Barry R. Davies

Publikováno v: ACS Medicinal Chemistry Letters. 13:1295-1301

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cf9dfca39604357a47354a464d4b09f5
https://doi.org/10.1021/acsmedchemlett.2c00172

A protein tertiary structure mimetic modulator of the Hippo signalling pathway

Autor: Stefan Geschwindner, Mercedes Vazquez-Chantada, Hacer Karatas, Carmen Carrillo García, Elisabetta Chiarparin, Dennis Schade, Malin Lemurell, Tom N. Grossmann, Paul R. J. Davey, Alleyn T. Plowright, Jeremy Kah Sheng Pang, Hélène Adihou, Boon Seng Soh, Stéphanie M. Guéret, Wanjin Hong, Carola M. Wassvik, Ranganath Gopalakrishnan, Eric Valeur, Tim Förster, Herbert Waldmann, Raphael Gasper, Ajaybabu V. Pobbati

Publikováno v: Nature Communications, Vol 11, Iss 1, Pp 1-10 (2020)
Adihou, H, Gopalakrishnan, R, Förster, T, Guéret, S M, Gasper, R, Geschwindner, S, Carrillo García, C, Karatas, H, Pobbati, A V, Vazquez-Chantada, M, Davey, P, Wassvik, C M, Pang, J K S, Soh, B S, Hong, W, Chiarparin, E, Schade, D, Plowright, A T, Valeur, E, Lemurell, M, Grossmann, T N & Waldmann, H 2020, ' A protein tertiary structure mimetic modulator of the Hippo signalling pathway ', Nature Communications, vol. 11, no. 1, 5425 . https://doi.org/10.1038/s41467-020-19224-8
Nature Communications, 11(1):5425. Nature Publishing Group
Nature Communications

Transcription factors are key protein effectors in the regulation of gene transcription, and in many cases their activity is regulated via a complex network of protein–protein interactions (PPI). The chemical modulation of transcription factor acti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4a62c13a75607c3b0b4ec116b5e51b4
http://link.springer.com/article/10.1038/s41467-020-19224-8

Lipidated Stapled Peptides Targeting the Acyl Binding Protein UNC119

Autor: Tom N. Grossmann, Philipp M. Cromm, Walter Hofer, Elisabeth Hennes, Philipp Küchler, Elisabetta Chiarparin, Herbert Waldmann, Shobhna Kapoor, David Longmire, Paul R. J. Davey, Hélène Adihou, Mercedes Vazquez-Chantada

Publikováno v: ChemBioChem, 20(24), 2987-2990. Wiley-VCH Verlag
Cromm, P M, Adihou, H, Kapoor, S, Vazquez-Chantada, M, Davey, P, Longmire, D, Hennes, E, Hofer, W, Küchler, P, Chiarparin, E, Waldmann, H & Grossmann, T N 2019, ' Lipidated Stapled Peptides Targeting the Acyl Binding Protein UNC119 ', ChemBioChem, vol. 20, no. 24, pp. 2987-2990 . https://doi.org/10.1002/cbic.201900615
Chembiochem

The acyl‐binding UNC119 proteins mediate the activation and transport of various N‐myristoylated proteins. In particular, UNC119a plays a crucial role in the completion of cytokinesis. Herein, we report the use of a lipidated peptide originating

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91a44fabdad54efc230d88f99c2ae89c
https://research.vu.nl/en/publications/72bfb642-0cf7-4fb0-8818-6aab2bf16fa9