PROTAC (PROTAC)

Proteolysis-Targeting Chimera: a heterobifunctional small molecule consisting of a target protein ligand connected via a linker to an E3 ubiquitin ligase recruiter. Induces proximity-driven ubiquitination and subsequent proteasomal degradation of the target protein rather than merely inhibiting its function. Operates catalytically, with one PROTAC molecule capable of degrading multiple target protein copies.

ตัวอย่าง

• ARV-110 (bavdegalutamide) targeting androgen receptor in prostate cancer
• ARV-471 (vepdegestrant) targeting estrogen receptor in breast cancer
• MZ1 degrader targeting BRD4 bromodomain