Literature DB >> 26730808

A FRET-Based Assay for the Identification and Characterization of Cereblon Ligands.

Iuliia Boichenko1, Silvia Deiss1, Kerstin Bär1, Marcus D Hartmann1, Birte Hernandez Alvarez1.   

Abstract

Cereblon serves as an ubiquitin ligase substrate receptor that can be tuned toward different target proteins by various cereblon-binding agents. This offers one of the most promising avenues for targeted protein degradation in cancer therapy, but cereblon binding can also mediate teratogenic effects. We present an effective assay that is suited for high-throughput screening of compound libraries for off-target cereblon interactions but also can guide lead optimization and rational design of novel cereblon effector molecules.

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Year:  2016        PMID： 26730808     DOI： 10.1021/acs.jmedchem.5b01735

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  9 in total

1.  A MedChem toolbox for cereblon-directed PROTACs.

Authors:  Christian Steinebach; Izidor Sosič; Stefanie Lindner; Aleša Bricelj; Franziska Kohl; Yuen Lam Dora Ng; Marius Monschke; Karl G Wagner; Jan Krönke; Michael Gütschow
Journal:  Medchemcomm       Date:  2019-05-28       Impact factor: 3.597

2.  Development of BODIPY FL Thalidomide As a High-Affinity Fluorescent Probe for Cereblon in a Time-Resolved Fluorescence Resonance Energy Transfer Assay.

Authors:  Wenwei Lin; Yongtao Li; Jaeki Min; Jiuyu Liu; Lei Yang; Richard E Lee; Taosheng Chen
Journal:  Bioconjug Chem       Date:  2020-10-18       Impact factor: 4.774

3.  On the correlation of cereblon binding, fluorination and antiangiogenic properties of immunomodulatory drugs.

Authors:  Christopher Heim; Samuel Maiwald; Christian Steinebach; Matthew K Collins; Jonathan Strope; Cindy H Chau; William D Figg; Michael Gütschow; Marcus D Hartmann
Journal:  Biochem Biophys Res Commun       Date:  2020-12-10       Impact factor: 3.575

4.  Design, synthesis, and biological evaluation of a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon modulators.

Authors:  Yilin Liu; Yuming Song; Yingju Xu; Meixu Jiang; Haibin Lu
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

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

Authors:  Saki Ichikawa; Hope A Flaxman; Wenqing Xu; Nandini Vallavoju; Hannah C Lloyd; Binyou Wang; Dacheng Shen; Matthew R Pratt; Christina M Woo
Journal:  Nature       Date:  2022-10-19       Impact factor: 69.504

6.  N-Adamantyl Phthalimidine: A New Thalidomide-like Drug That Lacks Cereblon Binding and Mitigates Neuronal and Synaptic Loss, Neuroinflammation, and Behavioral Deficits in Traumatic Brain Injury and LPS Challenge.

Authors:  Shih Chang Hsueh; Weiming Luo; David Tweedie; Dong Seok Kim; Yu Kyung Kim; Inho Hwang; Jung-Eun Gil; Baek-Soo Han; Yung-Hsiao Chiang; Warren Selman; Barry J Hoffer; Nigel H Greig
Journal:  ACS Pharmacol Transl Sci       Date:  2021-03-30

7.  De-Novo Design of Cereblon (CRBN) Effectors Guided by Natural Hydrolysis Products of Thalidomide Derivatives.

Authors:  Christopher Heim; Dimanthi Pliatsika; Farnoush Mousavizadeh; Kerstin Bär; Birte Hernandez Alvarez; Athanassios Giannis; Marcus D Hartmann
Journal:  J Med Chem       Date:  2019-07-12       Impact factor: 7.446

8.  Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.

Authors:  Samuel Maiwald; Christopher Heim; Birte Hernandez Alvarez; Marcus D Hartmann
Journal:  ACS Med Chem Lett       Date:  2020-12-04       Impact factor: 4.345

9.  High-resolution structures of the bound effectors avadomide (CC-122) and iberdomide (CC-220) highlight advantages and limitations of the MsCI4 soaking system.

Authors:  Christopher Heim; Marcus D Hartmann
Journal:  Acta Crystallogr D Struct Biol       Date:  2022-02-18       Impact factor: 7.652
  9 in total

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