A receptor degrader binds to a receptor and induces its breakdown, causing down-regulation of signaling of that receptor. It is distinct from the mechanism of action of receptor antagonists and inverse agonists, which reduce receptor signaling but do not cause receptor breakdown. Examples include selective estrogen receptor degraders and androgen receptor degraders, both developed for hormone-sensitive cancers.[1][2][3]
References
edit- ^ Lai, Ashton C.; Crews, Craig M. (February 2017). "Induced protein degradation: an emerging drug discovery paradigm". Nature Reviews Drug Discovery. 16 (2): 101–114. doi:10.1038/nrd.2016.211. PMC 5684876.
- ^ Tria, George S.; Abrams, Tinya; Baird, Jason; Burks, Heather E.; Firestone, Brant; Gaither, L. Alex; Hamann, Lawrence G.; He, Guo; Kirby, Christina A.; Kim, Sunkyu; Lombardo, Franco; Macchi, Kaitlin J.; McDonnell, Donald P.; Mishina, Yuji; Norris, John D.; Nunez, Jill; Springer, Clayton; Sun, Yingchuan; Thomsen, Noel M.; Wang, Chunrong; Wang, Jianling; Yu, Bing; Tiong-Yip, Choi-Lai; Peukert, Stefan (12 April 2018). "Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer". Journal of Medicinal Chemistry. 61 (7): 2837–2864. doi:10.1021/acs.jmedchem.7b01682.
- ^ Ha, Si; Luo, Guoshun; Xiang, Hua (22 December 2022). "A Comprehensive Overview of Small-Molecule Androgen Receptor Degraders: Recent Progress and Future Perspectives". Journal of Medicinal Chemistry. 65 (24): 16128–16154. doi:10.1021/acs.jmedchem.2c01487.
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