Targeting DNA damage response components induces enhanced STING-dependent type-I IFN response in ATM deficient cancer cells and drives dendritic cell activation

Autor: Marta Lopez-Pelaez, Lucy Young, Mercedes Vazquez-Chantada, Nadine Nelson, Steve Durant, Robert W. Wilkinson, Edmund Poon, Miguel Gaspar, Viia Valge-Archer, Paul Smith, Simon J. Dovedi

Publikováno v: OncoImmunology, Vol 11, Iss 1 (2022)

The concept of exploiting tumor intrinsic deficiencies in DNA damage repair mechanisms by inhibiting compensatory DNA repair pathways is well established. For example, ATM-deficient cells show increased sensitivity to the ATR inhibitor ceralasertib.

Externí odkaz: https://doaj.org/article/9d2d450388024f9abe63eda60fc9f35d

Impaired Function of Solute Carrier Family 19 Leads to Low Folate Levels and Lipid Droplet Accumulation in Hepatocytes

Autor: Ainara Cano, Mercedes Vazquez-Chantada, Javier Conde-Vancells, Aintzane Gonzalez-Lahera, David Mosen-Ansorena, Francisco J. Blanco, Karine Clément, Judith Aron-Wisnewsky, Albert Tran, Philippe Gual, Carmelo García-Monzón, Joan Caballería, Azucena Castro, María Luz Martínez-Chantar, José M. Mato, Huiping Zhu, Richard H. Finnell, Ana M. Aransay

Publikováno v: Biomedicines, Vol 11, Iss 2, p 337 (2023)

Low serum folate levels are inversely related to metabolic associated fatty liver disease (MAFLD). The role of the folate transporter gene (SLC19A1) was assessed to clarify its involvement in lipid accumulation during the onset of MAFLD in humans and

Externí odkaz: https://doaj.org/article/604e1f5cef3f4e0f877c63c8750f776b

Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8

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(8)

The DNA-PK complex is activated by double-strand DNA breaks and regulates the non-homologous end-joining repair pathway; thus, targeting DNA-PK by inhibiting the DNA-PK catalytic subunit (DNA-PKcs) is potentially a useful therapeutic approach for onc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2661b30d6b91249b7feab29e38d45bb4
https://pubmed.ncbi.nlm.nih.gov/35978693

Bicyclic β‐Sheet Mimetics that Target the Transcriptional Coactivator β‐Catenin and Inhibit Wnt Signaling

Autor: Alan Gerber, Sven Hennig, Rosa Bellavita, Isabel Everard, Thirza van Ramshorst, Elisabetta Chiarparin, Nina Louisa Efrém, Nicholas M Pearce, Paul R. J. Davey, Tom N. Grossmann, Paolo Grieco, Mathias Wendt, Mercedes Vazquez-Chantada

Publikováno v: Angewandte Chemie (International Ed. in English)
Angewandte Chemie-International Edition, 60(25), 13937-13944. Wiley
Wendt, M, Bellavita, R, Gerber, A, Efrém, N L, van Ramshorst, T, Pearce, N M, Davey, P R J, Everard, I, Vazquez-Chantada, M, Chiarparin, E, Grieco, P, Hennig, S & Grossmann, T N 2021, ' Bicyclic β-Sheet Mimetics that Target the Transcriptional Coactivator β-Catenin and Inhibit Wnt Signaling ', Angewandte Chemie-International Edition, vol. 60, no. 25, pp. 13937-13944 . https://doi.org/10.1002/anie.202102082
Angewandte Chemie-International Edition, 60(25), 13937-13944. John Wiley and Sons Ltd

Protein complexes are defined by the three‐dimensional structure of participating binding partners. Knowledge about these structures can facilitate the design of peptidomimetics which have been applied for example, as inhibitors of protein–protei

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6210eeee6d272df71252f5b2989c6227
http://europepmc.org/articles/PMC8252567

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