Molecular mechanisms of cereblon-based drugs

T Asatsuma-Okumura, T Ito, H Handa - Pharmacology & therapeutics, 2019 - Elsevier
Thalidomide, well known for its potent teratogenicity, has been re-evaluated as a clinically
effective drug for the treatment of multiple myeloma. Although the direct target of thalidomide …

[HTML][HTML] Molecular mechanisms of the teratogenic effects of thalidomide

T Asatsuma-Okumura, T Ito, H Handa - Pharmaceuticals, 2020 - mdpi.com
Thalidomide was sold worldwide as a sedative over 60 years ago, but it was quickly
withdrawn from the market due to its teratogenic effects. Thalidomide was later found to have …

Molecular mechanisms of thalidomide and its derivatives

T Ito, H Handa - Proceedings of the Japan Academy, Series B, 2020 - jstage.jst.go.jp
Thalidomide, originally developed as a sedative drug, causes multiple defects due to severe
teratogenicity, but it has been re-purposed for treating multiple myeloma, and derivatives …

[PDF][PDF] Exploiting ubiquitin ligase cereblon as a target for small-molecule compounds in medicine and chemical biology

T Ito, Y Yamaguchi, H Handa - Cell Chemical Biology, 2021 - cell.com
Cereblon (CRBN), originally identified as a gene associated with intellectual disability, was
identified as primary target of thalidomide. Accumulating evidence has shown that CRBN is …

The molecular mechanism of thalidomide analogs in hematologic malignancies

S Lindner, J Krönke - Journal of molecular medicine, 2016 - Springer
Thalidomide was sold in the 1950s as a sedative and was also used by pregnant women to
treat morning sickness. It became notorious for causing severe birth defects and was …

Influence of linker attachment points on the stability and neosubstrate degradation of cereblon ligands

A Bricelj, YL Dora Ng, D Ferber, R Kuchta… - ACS Medicinal …, 2021 - ACS Publications
Proteolysis targeting chimeras (PROTACs) hijacking the cereblon (CRBN) E3 ubiquitin
ligase have emerged as a novel paradigm in drug development. Herein we found that linker …

[HTML][HTML] Cereblon and its downstream substrates as molecular targets of immunomodulatory drugs

T Ito, H Handa - International journal of hematology, 2016 - Springer
Thalidomide was first developed as a sedative around 60 years ago, but exhibited
teratogenicity, leading to serious defects such as limb deformities. Nevertheless, thalidomide …

[HTML][HTML] What is the functional role of the thalidomide binding protein cereblon?

X Chang, AK Stewart - International journal of biochemistry and …, 2011 - ncbi.nlm.nih.gov
It has been found that nonsense mutation R419X of cereblon (CRBN) is associated with
autosomal recessive non-syndromic mental retardation. Further experiments showed that …

Ligands for cereblon: 2017–2021 patent overview

A Kazantsev, M Krasavin - Expert Opinion on Therapeutic Patents, 2022 - Taylor & Francis
Introduction Cereblon (CRBN), the substrate receptor of the CRL4CRBN E3 ubiquitin ligase
has been extensively studied due to its involvement in many biological processes. It has …

Selective degradation-inducing probes for studying cereblon (CRBN) biology

CE Powell, G Du, JW Bushman, Z He, T Zhang… - RSC Medicinal …, 2021 - pubs.rsc.org
Targeted protein degradation represents a rapidly growing area in drug discovery and
development. Moreover, small molecules that induce the targeted degradation of a given …