ArticleBiochemical and biophysical research communications2021
On the correlation of cereblon binding, fluorination and antiangiogenic properties of immunomodulatory drugs.
Article in Biochemical and biophysical research communications, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 17 citations in OpenAlex.
- Fluorinated Aminopiperidones as Non-Glutarimide Thalidomide Analogs: Stereodivergent Synthesis and Validation.ChemMedChem · 2026Article
- Monoterpenoid fluorophthalimide IMiDs that lack human cereblon binding: synthesis and anti-proliferative, anti-angiogenic and anti-inflammatory activities.Biochemical and biophysical research communications · 2025Article
- Revisiting the antiangiogenic mechanisms of fluorinated thalidomide derivatives.Bioorganic & medicinal chemistry letters · 2024Article
- Preclinical Evaluation of a Novel Series of Polyfluorinated Thalidomide Analogs in Drug-Resistant Multiple Myeloma.Biomolecules · 2024Article
- Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs.Journal of medicinal chemistry · 2023Article
- Thalidomide upper limb embryopathy - pathogenesis, past and present management and future considerations.The Journal of hand surgery, European volume · 2023Review
- A New Generation of IMiDs as Treatments for Neuroinflammatory and Neurodegenerative Disorders.Biomolecules · 2023Review
- Accessing three-branched high-affinity cereblon ligands for molecular glue and protein degrader design.RSC chemical biology · 2023Article
- Replacing the phthalimide core in thalidomide with benzotriazole.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- High-resolution structures of the bound effectors avadomide (CC-122) and iberdomide (CC-220) highlight advantages and limitations of the MsCI4 soaking system.Acta crystallographica. Section D, Structural biology · 2022Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
Abstract
Cereblon (CRBN), the substrate receptor of an E3 ubiquitin ligase complex, is a target of thalidomide and thalidomide-derived immunomodulatory drugs (IMiDs). The binding of these IMiDs to CRBN alters the substrate specificity of the ligase, thereby mediating multiple effects that are exploited in cancer therapy. However, to date, it is not clear which other possible targets might be involved in the efficacy of IMiDs. One especially prominent effect of a number of thalidomide analogs is their ability to inhibit angiogenesis, which is typically enhanced in fluorinated analogs. So far, the involvement of CRBN in antiangiogenic effects is under debate. Here, starting from a systematic set of thalidomide analogs and employing a quantitative in vitro CRBN-binding assay, we study the correlation of fluorination, CRBN binding and antiangiogenic effects. We clearly identify fluorination to correlate both with CRBN binding affinity and with antiangiogenic effects, but do not find a correlation between the latter two phenomena, indicating that the main target for the antiangiogenic effects of thalidomide analogs still remains to be identified.
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