Targeting oncoproteins with a positive selection assay for protein degraders

Most intracellular proteins lack hydrophobic pockets suitable for altering their function with drug-like small molecules. Recent studies indicate that some undruggable proteins can be targeted by compounds that can degrade them. For example, thalidomide-like drugs (IMiDs) degrade the critical multip...

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Veröffentlicht in:	Science advances 2021-02, Vol.7 (6)
Hauptverfasser:	Koduri, Vidyasagar, Duplaquet, Leslie, Lampson, Benjamin L, Wang, Adam C, Sabet, Amin H, Ishoey, Mette, Paulk, Joshiawa, Teng, Mingxing, Harris, Isaac S, Endress, Jennifer E, Liu, Xiaoxi, Dasilva, Ethan, Paulo, Joao A, Briggs, Kimberly J, Doench, John G, Ott, Christopher J, Zhang, Tinghu, Donovan, Katherine A, Fischer, Eric S, Gygi, Steven P, Gray, Nathanael S, Bradner, James, Medin, Jeffrey A, Buhrlage, Sara J, Oser, Matthew G, Kaelin, Jr, William G
Format:	Artikel
Sprache:	eng
Schlagworte:	Adaptor Proteins, Signal Transducing - genetics Basic Helix-Loop-Helix Transcription Factors - metabolism Benzylamines Biochemistry CRISPR-Cas Systems Humans Ikaros Transcription Factor - metabolism Oncogene Proteins - chemistry Oncogene Proteins - metabolism Proteolysis - drug effects Quinazolines SciAdv r-articles Thalidomide - analysis Thalidomide - pharmacology Transcription Factors
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