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RCSB PDB - 9DQD: cryo-EM structure of human Cereblon DDB1 in complex . . . We developed conditions for the direct cross-coupling of unprotected glutarimides with amines, streamlining the synthesis of alternative CRBN binders This manuscript describes the rapid synthesis of 30 CRBN binders, their characterization as potential degraders and a cryo-EM structure of the CRBN DDB1 with a representative compound ( 6 )
EMDB lt; EMD-40261 - EMBL-EBI Oral estrogen receptor PROTAC vepdegestrant (ARV-471) is highly efficacious as monotherapy and in combination with CDK4 6 or PI3K mTOR pathway inhibitors in preclinical ER+ breast cancer models
Kymera ENA 2024 Preclinical Poster CDK2 TPD_October 2024 CDK2 degradation results in reduced RB phosphorylation and proliferative capacity in both CCNE1amp cancer cells and breast cancer cells that have adapted to Palbociclib via upregulation of CCNE1 and reduction of RB expression, identifying biomarker-driven activity
Structure of the human DDB1– Cereblon – thalidomide complex CRBN, originally identified as a cerebral protein associated with mild mental retardation, is a highly conserved protein that forms a CRL4-type E3 ubiquitin ligase complex with Cul4A and damaged DNA binding protein 1 (DDB1), and plays a key role in limb outgrowth and expression of fibroblast growth factor Fgf8 in zebrafish and chicks
CRBN - DDB1 Interaction Summary | BioGRID Structure of the human Cereblon-DDB1-lenalidomide complex reveals basis for responsiveness to thalidomide analogs The Cul4-Rbx1-DDB1-Cereblon E3 ubiquitin ligase complex is the target of thalidomide, lenalidomide and pomalidomide, therapeutically important drugs for multiple myeloma and other B-cell malignancies
RCSB PDB - 8D81: Cereblon~DDB1 bound to Pomalidomide We performed cryo-electron microscopy analyses of the DNA damage-binding protein 1 (DDB1)-CRBN apo complex and compared these structures with DDB1-CRBN in the presence of CELMoD compounds alone and complexed with neosubstrates
Recombinant Human DDB1 CRBN Complex Protein, CF - R D Systems Binding of CRBN to Cullin-4 is mediated in part by DNA damage-binding protein 1 (DDB1), a component of multiple DCX class ligases In addition to its role in limb development, DDB1 is also involved in various DNA damage response mechanisms This product consists of an untagged complex of DDB1 and CRBN