Highlights from the data presented today include:
- Tumor cell lines representing different tumor types are consistently more sensitive to BET protein degradation than BET protein inhibition
- BET PROTACs cause robust BRD4 degradation and more prolonged suppression of oncogene c-Myc in vitro and have greater efficacy in vivo compared to BET inhibitors
- Intermittent dosing in vivo of BET PROTACs causes tumor regression or stasis in diffuse large B-cell lymphoma, prostate cancer and ovarian cancer xenograft models
This presentation was part of Plenary Session 1, "Degradation Based Therapeutics," which was co-chaired by Dr. Craig M. Crews, Lewis B. Cullman Professor of Molecular, Cellular and Developmental Biology at Yale University, and Arvinas Founder and Chief Scientific Advisor.
Dr. Coleman's presentation is available on the Arvinas website under Publications at www.arvinas.com.
Arvinas is a pharmaceutical company focused on developing new small molecules ‒ known as PROTACs (PROteolysis TArgeting Chimeras) ‒ aimed at degrading disease-causing cellular proteins. Based on groundbreaking research conducted at Yale University by Founder and Chief Scientific Advisor, Dr. Craig Crews, the company is translating innovative protein degradation approaches into novel drugs for the treatment of cancer and other diseases. The company's new PROTAC-based drug paradigm induces protein degradation, rather than protein inhibition, and offers the advantage of potentially targeting "undruggable" as well as "druggable" elements of the proteome. This greatly expands the ability to create drugs for many new, previously unapproachable targets. For more information, visit www.arvinas.com.
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