Chapter title |
Generation and Assessment of Fusions Between HDACi and TKi
|
---|---|
Chapter number | 31 |
Book title |
HDAC/HAT Function Assessment and Inhibitor Development
|
Published in |
Methods in molecular biology, January 2017
|
DOI | 10.1007/978-1-4939-6527-4_31 |
Pubmed ID | |
Book ISBNs |
978-1-4939-6525-0, 978-1-4939-6527-4
|
Authors |
Siavosh Mahboobi, Bernadette Pilsl, Andreas Sellmer |
Abstract |
Chimeric compounds combine the structural features of inhibitors of histone deacetylases (HDACi) and tyrosine kinase inhibitors (TKi), and therefore unite the effects of a dual-targeting strategy in one compound. Here, we describe the generation of such hybrid molecules. Small molecules, known as TKi, are combined with a Zn(2+) chelating motive, preferentially a hydroxamic acid, in addition. The resulting small molecules also can inhibit histone deacetylases, which are dependent on the catalytically active Zn(2+). Moreover, we summarize how the growth-inhibitory effects of these combined compounds can be determined with a simple proliferation assay with a leukemic cell line. |
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