Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation

Aberrant expression of proteins often underlies many diseases, including cancer. A recently developed approach in drug development is small molecule-mediated, selective degradation of dysregulated proteins. We have devised a protein-knockdown system that utilizes chimeric molecules termed specific a...

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Veröffentlicht in:	The Journal of biological chemistry 2018-05, Vol.293 (18), p.6776-6790
Hauptverfasser:	Ohoka, Nobumichi, Morita, Yoko, Nagai, Katsunori, Shimokawa, Kenichiro, Ujikawa, Osamu, Fujimori, Ikuo, Ito, Masahiro, Hayase, Youji, Okuhira, Keiichiro, Shibata, Norihito, Hattori, Takayuki, Sameshima, Tomoya, Sano, Osamu, Koyama, Ryokichi, Imaeda, Yasuhiro, Nara, Hiroshi, Cho, Nobuo, Naito, Mikihiko
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - pharmacology Down-Regulation ERalpha estrogen receptor Estrogen Receptor alpha - metabolism Humans Ligands MCF-7 Cells Mice proteasome Protein Binding protein knockdown Protein Synthesis and Degradation Proteolysis SNIPER Thiazoles - pharmacology tumor therapy ubiquitin Ubiquitination X-linked inhibitor of apoptosis protein (XIAP) X-Linked Inhibitor of Apoptosis Protein - metabolism Xenograft Model Antitumor Assays
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