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Issue 7, 2019
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Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)

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Abstract

A preloaded resin consisting of a thalidomide moiety and an ethylene-oxy linker allows the simple and fast formation of PROTACs. The feasibility of the procedure was illustrated by conjugating different protein kinase inhibitors. The biological functionality of an ibrutinib-like conjugate was then confirmed by a cellular experiment.

Graphical abstract: Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)

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Supplementary files

Article information


Submitted
01 Nov 2018
Accepted
17 Dec 2018
First published
17 Dec 2018

Chem. Commun., 2019,55, 929-932
Article type
Communication

Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)

S. Krajcovicova, R. Jorda, D. Hendrychova, V. Krystof and M. Soural, Chem. Commun., 2019, 55, 929
DOI: 10.1039/C8CC08716D

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