Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators

Whereas the PROTAC approach to target protein degradation greatly benefits from rational design, the discovery of small-molecule degraders relies mostly on phenotypic screening and retrospective target identification efforts. Here, we describe the design, synthesis, and screening of a large diverse...

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Veröffentlicht in:	Journal of medicinal chemistry Jg. 64; H. 11; S. 7296
Hauptverfasser:	Nishiguchi, Gisele, Keramatnia, Fatemeh, Min, Jaeki, Chang, Yunchao, Jonchere, Barbara, Das, Sourav, Actis, Marisa, Price, Jeanine, Chepyala, Divyabharathi, Young, Brandon, McGowan, Kevin, Slavish, P Jake, Mayasundari, Anand, Jarusiewicz, Jamie A, Yang, Lei, Li, Yong, Fu, Xiang, Garrett, Shalandus H, Papizan, James B, Kodali, Kiran, Peng, Junmin, Pruett Miller, Shondra M, Roussel, Martine F, Mullighan, Charles, Fischer, Marcus, Rankovic, Zoran
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	10.06.2021
ISSN:	1520-4804, 1520-4804
Online-Zugang:	Weitere Angaben
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