Third generation quinoline-3-carboxamide transcriptional disrupter of HDAC4, HIF-1α, and MEF-2 signaling for metastatic castration-resistant prostate cancer.

John T IsaacsSusan L DalrympleLizamma AntonyDavid Marc RosenIlsa M ColemanPeter S NelsonMaya KostovaIain A MurrayGary H PerdewSamuel R DenmeadeEmmanuel S AkinboyeW Nathaniel Brennen

Published in: The Prostate (2023)

This increased therapeuticindex nominates ESATA-20 as a lead candidate forclinical development as an orally active third generation quinoline-3-carboxamide analog thatretains its on-target ability to disrupt HDAC4/HIF-1α/MEF-2-dependent adaptive survival signaling in the compromisedtumor microenvironment found in mCRPC.

Keyphrases

molecular docking
histone deacetylase
squamous cell carcinoma
stem cells
endothelial cells
transcription factor