Ontology highlight
ABSTRACT:
SUBMITTER: Cini E
PROVIDER: S-EPMC6144071 | biostudies-literature | 2018 Aug
REPOSITORIES: biostudies-literature
Cini Elena E Faltoni Valentina V Petricci Elena E Taddei Maurizio M Salvini Laura L Giannini Giuseppe G Vesci Loredana L Milazzo Ferdinando Maria FM Anastasi Anna Maria AM Battistuzzi Gianfranco G De Santis Rita R
Chemical science 20180703 31
We describe here two novel antibody-drug conjugates loaded with the HDAC inhibitor ST7612AA1 (IC<sub>50</sub> equal to 0.07 μM on NCI-H460 cells), a thiol-based molecule with a moderate toxicity <i>in vivo</i>. Two payloads were prepared using cleavable and non-cleavable linkers. After anchoring to cetuximab through amide bond with lysines, the resulting HDAC inhibitor-antibody conjugates showed ability to recognize EGFR and efficient internalization in tumor cells. Both ADCs induced sensible in ...[more]