BOSTON and SOUTH SAN FRANCISCO, Calif. — October 3, 2025 — Leads & Copy — Frontier Medicines Corporation announced the publication of groundbreaking discoveries in Structure, a Cell Press journal, demonstrating that DCAF2 can be harnessed as a novel E3 ligase for targeted protein degradation (TPD). DCAF2 presents an opportunity to deliver tumor-targeted protein degraders given its frequent overexpression in various types of cancer.
The study leveraged the Frontier™ Platform and advanced cryogenic electron microscopy to present the first reported structures of the DCAF2 complex in both its apo and liganded state. The team discovered DCAF2 can covalently and selectively bind to small molecules and cause the degradation of other proteins, opening up a novel target site for TPD and a new avenue for the development of therapeutic bifunctional degraders and molecular glues that leverage DCAF2.
Weiru Wang, Executive Director of Protein Sciences and Structural Biology and lead study author at Frontier Medicines, said that demonstrating that DCAF2 can be harnessed for TPD is a major step forward for protein degradation, and for Frontier, as it aligns with their mission to unlock new ways to fight cancer and drug the undruggables.
Cory Tromblee, Scient PR, cory@scientpr.com
Source: Frontier Medicines
