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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Yayımlandı:J Med Chem
Asıl Yazarlar: 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
Materyal Türü: Artigo
Dil:Inglês
Baskı/Yayın Bilgisi: American Chemical Society 2021
Online Erişim: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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