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 …
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
The ubiquitin E3 ligase substrate adapter cereblon (CRBN) is a target of thalidomide and
lenalidomide, therapeutic agents used in the treatment of haematopoietic malignancies …
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 …
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 …
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 …
initiator of a large number of human diseases, and thus, the elimination and prevention of …
A MedChem toolbox for cereblon-directed PROTACs
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 …
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 …
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 …
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 …
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
Immunomodulatory imide drugs (IMiDs) such as thalidomide, pomalidomide, and
lenalidomide are the most common cereblon (CRBN) recruiters in proteolysis-targeting …
lenalidomide are the most common cereblon (CRBN) recruiters in proteolysis-targeting …