Structural and biophysical comparisons of the pomalidomide
Dec 12, 2023 · To expand our understanding of the molecular basis for the interaction of SALL4 with cereblon, we performed biophysical and structural studies demonstrating that SALL4 zinc …
See results only from nature.comDesign of a Cereblon construct for crystallographic and biophysic…
In this work, the authors design and validate a truncated CRBN construct, CRBNmidi, that enables crystallization and biophysical characterization o…
Crbn-based molecular Glues: Breakthroughs and perspectives
Apr 15, 2024 · It has been observed that CRBN can be exploited by small molecules to facilitate the recruitment and ubiquitination of non-natural CRL4 substrates, resulting in the degradation …
Discovery and characterization of a selective IKZF2 glue degrader …
Mar 16, 2023 · The binding of recombinant IKZF2 zinc finger domains to the DDB1:CRBN:DKY709 complex was explored using surface plasmon resonance (SPR) with …
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Representative SPR binding data with 1:1 kinetic ... - ResearchGate
Download scientific diagram | Representative SPR binding data with 1:1 kinetic modelling for the interaction of SALL4 ZF1-2 domains with DDB1:CRBN complexed with pomalidomide (POM) …
Molecular glues (A) Crystal structure of DDB1:CRBN:CC …
In this study, a one-pot synthesis via photoinduced C (sp2)–C (sp3) coupling followed by amide formation to access proteolysis targeting chimeras (PROTACs) was developed.
Small Molecule Induced Protein Complexes: Gluing the …
Thalidomide is an example of a monofunctional molecule that induces complex formation between an E3 ubiquitin ligase (Cereblon, CRBN) and a substrate protein. The net effect is K48 linked poly-ubiquitination which leads to …
Mining the CRBN Target Space Redefines Rules for Molecular Glue …
Apr 1, 2024 · Our combined biochemical/biophysical approach to glue identification using HTRF and SPR demonstrates the successful and scalable use of these methodologies for HTS, with …
Protein–protein interfaces in molecular glue-induced …
The E3 ubiquitin ligase cereblon (CRBN) was identified as the effector protein of thalidomide. 1 Binding of thalidomide to CRBN recruits and degrades neosubstrates, providing an early example of molecular glue-induced targeted …
(A) Structures of CRBN-binding drugs. (B) Diagram of …
Molecular glues can specifically induce aggregation between two or more proteins to modulate biological functions. In recent years, molecular glues have been widely used as protein degraders.
Design of a Cereblon construct for crystallographic and …
Oct 15, 2024 · In this work, the authors design and validate a truncated CRBN construct, CRBNmidi, that enables crystallization and biophysical characterization of CRBN-binding …
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