PROTAC (PROTAC)
PROTACProteolysis-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.
Ví dụ
- ARV-110 (bavdegalutamide) targeting androgen receptor in prostate cancer
- ARV-471 (vepdegestrant) targeting estrogen receptor in breast cancer
- MZ1 degrader targeting BRD4 bromodomain
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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 …