Journal Article

DKFZ-2017-05079

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development.

Lohbeck, J. (First author)DKFZ* ; Miller, A. (Last author)DKFZ*

2016
Elsevier Science Amsterdam [u.a.]

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Please use a persistent id in citations: doi:10.1016/j.bmcl.2016.09.048

Abstract: The use of small molecules to regulate cellular levels of specific proteins is poised to become a powerful technique in the coming years. Critical to the success of any project utilizing such an approach will be the ability to synthesize libraries of candidate small molecules for testing in cellular systems. Herein, we describe a practical synthesis of a phthalimide-based scaffold, which can be easily diversified to make Cereblon-targeting PROTACs. We demonstrate the effectiveness of this approach by synthesizing a PROTAC toolbox of four amines which can be coupled to inhibitors in a straightforward manner.

Keyword(s): Ligands ; Phthalimides ; phthalimide ; CRBN protein, human ; Peptide Hydrolases

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Contributing Institute(s):

1. Wirkstoffforschung (G404)

Research Program(s):

1. 317 - Translational cancer research (POF3-317) (POF3-317)

Appears in the scientific report 2016

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Database coverage:
; BIOSIS Previews ; Current Contents - Life Sciences ; Ebsco Academic Search ; IF < 5 ; JCR ; NCBI Molecular Biology Database ; Nationallizenz ; SCOPUS ; Science Citation Index ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection

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