Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators
Gisele Nishiguchi, Fatemeh Keramatnia, Jaeki Min, Yunchao Chang, Barbara Jonchère, Sourav Das, Marisa Actis, Jeanine E. Price, Divyabharathi Chepyala, Brandon Young, Kevin McGowan, P.J. Slavish, Anand Mayasundari, Jamie Jarusiewicz, Lei Yang, Yong Li, Xiang Fu, Shalandus H. Garrett, James B. Papizan, Kiran Kodali, Junmin Peng, Shondra Miller, Martine F. Roussel, Charles G. Mullighan, Marcus Fischer, Zoran Ranković
Abstract
, and it supports the utility of a diverse library of CRBN binders in the pursuit of targeting undruggable oncoproteins.
Topics & Concepts
CereblonChemistryDrug discoverySmall moleculePhenotypic screeningChemical libraryComputational biologyBioavailabilityIn vivoPharmacologyBiochemistryPhenotypeBiologyGeneticsUbiquitin ligaseGeneUbiquitinProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysMultiple Myeloma Research and Treatments