Design, Synthesis, and Pharmacological Evaluation of Metabolically Stable Apelin Receptor Antagonists with Improved In Vivo Exposure and Efficacy in Ovarian Cancer

Youngjae You · 2026-01-29

TL;DR

A focused medicinal chemistry effort was undertaken to design and synthesize a second-generation series of APJ antagonists with improved metabolic stability while retaining APJ antagonist activity, which significantly increased median survival and reduced metastatic tumor burden and ascites formation in an orthotopic ovarian cancer xenograft mouse model.

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Funding
Targeting ovarian cancer spheroid formation and metabolic adaptation by APJ inhibitionSite Specific Drug Delivery with Light-responsive Conjugates for Photo-biomodulation

Division of Cancer Prevention, National Cancer Institute

R01CA258546

National Institute of General Medical Sciences

R01GM113940