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Updated: Jun 8, 2026

Co-immunoprecipitation Assay Using Endogenous Nuclear Proteins from Cells Cultured Under Hypoxic Conditions
Published on: August 2, 2018
Inhibition of hypoxia-inducible transcription factor complex with designed epipolythiodiketopiperazine
Swati Kushal1, Hui Wang, Csaba F László
1Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, 1985 Zonal Ave., Los Angeles, CA 90033, USA.
Abstract:
Designed small molecule inhibitors of hypoxia-inducible gene expression have potential to become new research tools for molecular biology, genetics and serve as leads to new therapeutics. We report design, synthesis evaluation of biological activity, and a preliminary mechanistic study of epipolythiodiketopiperazine (ETP) transcriptional antagonist that targets the interaction between the C-terminal transactivation domain (C-TAD) of hypoxia-inducible factor 1α (HIF-1α) and cysteine-histidine rich region (CH1) of transcriptional coactivator p300/CBP. Our results indicate that in cultured cells synthetic ETP 3 disrupts the structure and function of this complex in a dose-dependent manner, resulting in rapid downregulation of hypoxia-inducible gene expression.
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