Pelophen B is a non-taxoid binding microtubule-stabilizing agent with promising preclinical anticancer properties.

ABSTRACT: Taxanes, such as paclitaxel (PTX), stabilize microtubules and are used as a first-line therapy in multiple cancer types. Disruption of microtubule equilibrium, which plays an essential role in mitosis and cell homeostasis, ultimately results in cell death. Even though PTX is a very potent chemotherapy, its use is associated with major side effects and therapy resistance. Pelophen B (PPH), a synthetic analog of peloruside A, stabilizes microtubules through interaction with a non-taxoid binding site of β-tubulin. We evaluated the anticancer effect of PPH in a variety of tumor types by using established cell lines, early-passage cultures and ex vivo tumor-derived cultures that preserve the 3D architecture of the tumor microenvironment. PPH significantly blocks colony formation capacity, reduc

SUBMITTER: Vermeulen S 

PROVIDER: S-EPMC11618378 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature