Abstract 4273: Discovery of first in class, polyphenolic inhibitors of CKAP4 and their antitumor activity in ovarian and endometrial cancer

Authors: Eugenio Gaudio, Viktor Ivasishin, Paulina Biniecka, Christian Kleusch, Cosimo Kropp, Benjamin Zimmer, Kamilla Pawlicka, Helena Almqvist, Alexey Chernobrovkin, Janneke Melis, Guido Zaman, Dan F. Stoicescu

Published: 2025-04-21

DOI: 10.1158/1538-7445.am2025-4273

Source: Full article

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Abstract

While some plant-derived polyphenolic compounds exhibit anticancer activity, their complex mechanism of action is generally hindering the efforts to produce clinically useful derivatives. Here we present several compounds that are, to the best of our knowledge, the first known inhibitors of cytoskeleton associated protein 4 (CKAP4) a transmembrane protein associated with resilient forms of cancer. Since CKAP4 is overexpressed in ovarian cancer the compounds were evaluated in the experimental models below as proof of concept.