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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8201443/
https://www.ncbi.nlm.nih.gov/pubmed/34042448
http://dx.doi.org/10.1021/acs.jmedchem.0c01313

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8201443/
https://www.ncbi.nlm.nih.gov/pubmed/34042448
http://dx.doi.org/10.1021/acs.jmedchem.0c01313

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