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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Publié dans:J Med Chem
Auteurs principaux: 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: Artigo
Langue:Inglês
Publié: American Chemical Society 2021
Accès en ligne: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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