Targeted Degradation of Transcription Coactivator SRC‐1 through the N‐Degron Pathway

Aberrantly elevated steroid receptor coactivator‐1 (SRC‐1) expression and activity are strongly correlated with cancer progression and metastasis. Here we report, for the first time, the development of a proteolysis targeting chimera (PROTAC) that is composed of a selective SRC‐1 binder linked to a...

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Veröffentlicht in:	Angewandte Chemie International Edition 2020-09, Vol.59 (40), p.17548-17555
Hauptverfasser:	Lee, Yeongju, Heo, Jiwon, Jeong, Hoibin, Hong, Kyung Tae, Kwon, Do Hoon, Shin, Min Hyeon, Oh, Misook, Sable, Ganesh A., Ahn, G‐One, Lee, Jun‐Seok, Song, Hyun Kyu, Lim, Hyun‐Suk
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Animals Antigens, CD - metabolism Antineoplastic Agents - metabolism Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Biocatalysis Cadherins - metabolism Cancer cancer metastasis Cell Line, Tumor Cell migration Cell Movement - drug effects Degradation Down-Regulation - drug effects Humans Macrophage Colony-Stimulating Factor - metabolism Metastases Mice, Inbred BALB C Neoplasm Invasiveness - prevention & control Neoplasms - drug therapy Nuclear Receptor Coactivator 1 - antagonists & inhibitors Nuclear Receptor Coactivator 1 - metabolism Peptides - metabolism Peptides - pharmacology Peptides - therapeutic use Protein Binding Proteins Proteolysis proteolysis-targeting chimers (PROTACs) Signal Transduction - drug effects Src protein SRC-1 transcriptional co-activator stapled peptide Steroids the N-degron pathway Transcription Ubiquitin-Protein Ligases - metabolism Up-Regulation - drug effects
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