Xiaoke Guo

Discovery of Tricyclic Oxazinoquinolinone-Based BCL6 PROTAC Degraders with Potent Activity Against Diffuse Large B-Cell Lymphoma

Abstract B-cell lymphoma 6 (BCL6) is a key transcriptional repressor involved in the pathogenesis of diffuse large B-cell lymphoma (DLBCL). In this study, scaffold hopping of BI-3802 led to compound 1, a new tricyclic BCL6-targeting ligand. Further optimization of linker architec...

Harnessing the E3 Ligase KLHL12 for Tumor‐Selective Protein Degradation

ABSTRACT Proteolysis‐targeting chimeras (PROTACs) are currently constrained by a reliance on ubiquitously expressed E3 ligases, which compromises tumor selectivity and raises toxicity risks. Here, we identified KLHL12 as a potentially tumor‐selective E3 ligase and reported the de...