Tailored biosensors for drug screening, efficacy assessment, and toxicity evaluation

Y Tao, L Chen, M Pan, F Zhu, D Zhu - ACS sensors, 2021 - ACS Publications
Biosensors have been flourishing in the field of drug discovery with pronounced
developments in the past few years. They facilitate the screening and discovery of innovative …

The E3 ligase adapter cereblon targets the C-terminal cyclic imide degron

S Ichikawa, HA Flaxman, W Xu, N Vallavoju, HC Lloyd… - Nature, 2022 - nature.com
The ubiquitin E3 ligase substrate adapter cereblon (CRBN) is a target of thalidomide and
lenalidomide, therapeutic agents used in the treatment of haematopoietic malignancies …

A cereblon modulator (CC-220) with improved degradation of Ikaros and Aiolos

ME Matyskiela, W Zhang, HW Man… - Journal of medicinal …, 2018 - ACS Publications
The drugs lenalidomide and pomalidomide bind to the protein cereblon, directing the CRL4–
CRBN E3 ligase toward the transcription factors Ikaros and Aiolos to cause their …

[HTML][HTML] Identification and structural basis of C-terminal cyclic imides as natural degrons for cereblon

C Heim, AK Spring, S Kirchgäßner, D Schwarzer… - Biochemical and …, 2022 - Elsevier
Cereblon (CRBN) is a ubiquitously expressed E3 ligase substrate receptor and a key player
in pharmaceutical targeted protein degradation. Despite substantial insight gained into its …

[HTML][HTML] Development of KEAP1-targeting PROTAC and its antioxidant properties: In vitro and in vivo

SY Park, R Gurung, JH Hwang, JH Kang, HJ Jung… - Redox Biology, 2023 - Elsevier
Oxidative stress due to abnormal accumulation of reactive oxygen species (ROS) is an
initiator of a large number of human diseases, and thus, the elimination and prevention of …

A MedChem toolbox for cereblon-directed PROTACs

C Steinebach, I Sosič, S Lindner, A Bricelj, F Kohl… - …, 2019 - pubs.rsc.org
A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of
linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used …

[HTML][HTML] Cereblon neo-substrate binding mimics the recognition of the cyclic imide degron

C Heim, AK Spring, S Kirchgäßner, D Schwarzer… - Biochemical and …, 2023 - Elsevier
In targeted protein degradation, immunomodulatory drugs (IMiDs) or cereblon (CRBN) E3
ligase modulatory drugs (CELMoDs) recruit neo-substrate proteins to the E3 ubiquitin ligase …

Chemical ligand space of cereblon

I Boichenko, K Bär, S Deiss, C Heim, R Albrecht… - ACS …, 2018 - ACS Publications
The protein cereblon serves as a substrate receptor of a ubiquitin ligase complex that can be
tuned toward different target proteins by cereblon-binding agents. This approach to targeted …

De-novo design of cereblon (CRBN) effectors guided by natural hydrolysis products of thalidomide derivatives

C Heim, D Pliatsika, F Mousavizadeh… - Journal of Medicinal …, 2019 - ACS Publications
Targeted protein degradation via cereblon (CRBN), a substrate receptor of an E3 ubiquitin
ligase complex, is an increasingly important strategy in various clinical settings, in which the …

Leveraging ligand affinity and properties: discovery of novel benzamide-type cereblon binders for the design of PROTACs

C Steinebach, A Bricelj, A Murgai, I Sosic… - Journal of medicinal …, 2023 - ACS Publications
Immunomodulatory imide drugs (IMiDs) such as thalidomide, pomalidomide, and
lenalidomide are the most common cereblon (CRBN) recruiters in proteolysis-targeting …