Structure of the human Cereblon–DDB1–lenalidomide complex reveals basis for responsiveness to thalidomide analogs
By P. Chamberlain, A. Lopez-Girona, Karen Miller, G. Carmel, B. Pagarigan, B. Chie-Leon, E. Rychak, L. Corral, Yan J Ren, Maria Wang and 10 more. 2014
464 citations recorded by the source corpus.
Subfields: Hematology, Molecular Biology
How researchers see this paper
The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.
In Hematology
In Molecular Biology
- George M. Burslem
- C. Crews
- Steven A. Carr
- Benjamin L. Ebert
- Andrei N. Lupas
- N. Vargesson
- M. Coles
- Marcus D. Hartmann
Citations in the corpus
- Structural Dynamics of the Cereblon Ligand Binding Domain (2015, background): “This structure [8] is bound to lenalidomide and is in a virtually identical conformation to the structures of chicken cereblon in complex with thalidomide, lenalidomide or pomalidomide [9].”
- Plasticity in binding confers selectivity in ligand induced protein degradation (2018, unknown): “IMiDs bind CRBN, the substrate receptor of the CUL4-RBX1-DDB1-CRBN (CRL4 CRBN ) E3 ubiquitin ligase 18–20 , and act by redirecting the activity of the CRL4 CRBN ligase to ubiquitinate these neo-substrates 17 .”
- Lessons in PROTAC design from selective degradation with a promiscuous warhead (2017, background): “The immunomodulatory imide drug thalidomide and its analogs have been shown to bind to CRBN and induce degradation of several neosubstrate proteins (Chamberlain et al., 2014; Krönke et al., 2014; Lu et al., 2014).”
- Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS (2015, background): “To investigate how the substitution of isoleucine for valine in mouse Crbn confers lenalidomide-responsiveness, we superimposed the structures for the mouse and human IMiD-binding regions bound to lenalidomide as solved in Chamberlain et al. (2014)25.”
- Thalidomide‐induced teratogenesis: History and mechanisms (2015, background): “…bind each other, that the S-enantiomer of thalidomide (and also for both its related analogs, pomalidomide, and lenalidomide) can bind Cereblon, and also demonstrated how thalidomide can target myeloma cells and target them through binding Cereblon (Chamberlain et al., 2014; Fischer et al., 2014).”