Discovery of CRBN as a target of thalidomide: a breakthrough for progress in the development of protein degraders-Reference-Cited by-同舟云学术

Discovery of CRBN as a target of thalidomide: a breakthrough for progress in the development of protein degraders

Published:2022 Issue:15 Volume:51 Page:6234-6250
ISSN:0306-0012
Container-title:Chemical Society Reviews
language:en
Short-container-title:Chem. Soc. Rev.

Author:

Yamamoto Junichi¹^ORCID,Ito Takumi²^ORCID,Yamaguchi Yuki¹,Handa Hiroshi³^ORCID

Affiliation:

1. School of Life Science and Technology, Tokyo Institute of Technology, Yokohama 226-8501, Japan

2. Institute of Medical Science, Tokyo Medical University, Shinjuku, Tokyo 160-8402, Japan

3. Center for Future Medical Research, Tokyo Medical University, Shinjuku, Tokyo 160-8402, Japan

Abstract

Thalidomide and its derivatives are the only protein degraders currently used in clinical practice. This tutorial review provides an overview of the mechanism of action of thalidomide-based degraders and their future perspectives.

Funder

Japan Society for the Promotion of Science

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/CS/D2CS00116K

Reference116 articles.

1. Identification of a Primary Target of Thalidomide Teratogenicity

2. Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

3. The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins

4. Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS

5. A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

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