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Antibody drug conjugates (ADCs) charged with HDAC inhibitor for targeted epigenetic modulation

We describe here two novel antibody-drug conjugates loaded with the HDAC inhibitor ST7612AA1 (IC(50) equal to 0.07 μM on NCI-H460 cells), a thiol-based molecule with a moderate toxicity in vivo. Two payloads were prepared using cleavable and non-cleavable linkers. After anchoring to cetuximab throug...

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Detalles Bibliográficos
Autores principales: Cini, Elena, Faltoni, Valentina, Petricci, Elena, Taddei, Maurizio, Salvini, Laura, Giannini, Giuseppe, Vesci, Loredana, Milazzo, Ferdinando Maria, Anastasi, Anna Maria, Battistuzzi, Gianfranco, De Santis, Rita
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6144071/
https://www.ncbi.nlm.nih.gov/pubmed/30288233
http://dx.doi.org/10.1039/c7sc05266a