Ramin Dubey

TL;DR: A stabilized alpha-helix designed to target the binding interface between the C-terminal transactivation domain (C-TAD) of hypoxia-inducible factor 1alpha (HIF-1alpha) and cysteine-histidine rich region (CH1) of transcriptional coactivator CBP/p300 is reported.

TL;DR: An unbiased approach directed at identifying novel RPE differentiation-promoting factors using a high-throughput quantitative PCR screen complemented by a novel orthogonal human induced pluripotent stem cell (hiPSC)-based RPE reporter assay is developed.

TL;DR: The results indicate that disrupting this interaction of the p300/CBP coactivator with the transcription factor HIF-1alpha results in rapid downregulation of hypoxia-inducible genes critical for cancer progression.

TL;DR: The designs, synthesis, and in vivo efficacy evaluation of a protein domain mimetic targeting the interaction of the p300/CBP coactivator with the transcription factor hypoxia-inducible factor-1α suggest that rationally designed synthetic mimics of protein subdomains that target the transcription factors–coactivator interfaces represent a unique approach for in vivo modulation of oncogenic signaling and arresting tumor growth.

TL;DR: Results suggest that inhibition of HIF1 transcriptional activity by designed dimeric ETPs could offer an innovative approach to cancer therapy with the potential to overcome hypoxia-induced tumor growth and resistance.