PDE4 bifunctional degrader

PDE4 bifunctional degraders are novel targeted protein degradation agents designed to selectively degrade the phosphodiesterase 4 (PDE4) enzyme, particularly the PDE4D isoform. These degraders use a bifunctional mechanism that links a PDE4 inhibitor warhead to an E3 ligase recruiter, promoting ubiquitination and proteasomal degradation of PDE4. This approach aims to achieve superior potency in reducing inflammatory cytokines such as TNF-α, IFN-γ, and IL-1β compared to traditional PDE4 inhibitors and JAK inhibitors. The design potentially avoids gastrointestinal side effects commonly associated with oral PDE4 inhibitors. These degraders are being developed primarily for autoimmune and inflammatory diseases.

Other names

PDE4D bifunctional degraderPDE-4D bifunctional degraderPDE 4D bifunctional degrader