- March 23, 2023
Proteolysis targeting chimeras (PROTACs)
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules with three chemical elements: a ligand binding to a target protein of interest, a ligand binding to and recruiting E3 ubiquitin ligase complex, and a linker for conjugating these two ligands together. PROTAC is a chemical knockdown strategy that degrades the target protein through the ubiquitin-proteasome system. Unlike traditional inhibitors’ competitive- and occupancy-driven process, PROTACs are catalytic in their mode of action, which can promote target protein degradation at low exposures.
PROTAC androgen receptor (AR) degraders
In vivo efficacy evaluation of ARD-2585
Plasma stability studies of ARD-2585
Summary
References:
[1] Weiguo Xiang, et al. Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer. J Med Chem. 2021 Sep 23;64(18):13487-13509. doi: 10.1021/acs.jmedchem.1c00900.
[2] Xiaojuan Jia, et al. Targeting androgen receptor degradation with PROTACs from bench to bedside. Biomed Pharmacother. 2023 Feb;158:114112. DOI: 10.1016/j.biopha.2022.114112
[3] Thi-Thao-Linh Nguyen, et al. Development of an LC-MS/MS Method for ARV-110, a PROTAC Molecule, and Applications to Pharmacokinetic Studies. Molecules. 2022 Mar 18;27(6):1977. doi: 10.3390/molecules27061977.
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