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

[Image: see text] 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 o...

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Publicado no:J Med Chem
Main Authors: 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
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2021
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC8201443/
https://ncbi.nlm.nih.gov/pubmed/34042448
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c01313
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