Beckers, Thomas and Mahboobi, Siavosh and Sellmer, Andreas and Winkler, Matthias and Eichhorn, Emerich and Pongratz, Herwig and Maier, Thomas and Ciossek, Thomas and Baer, Thomas and Kelter, Gerhard and Fiebig, Heinz-Herbert and Schmidt, Mathias (2012) Chimerically designed HDAC- and tyrosine kinase inhibitors. A series of erlotinib hybrids as dual-selective inhibitors of EGFR, HER2 and histone deacetylases. MEDCHEMCOMM, 3 (7). pp. 829-835. ISSN 2040-2503,
Full text not available from this repository. (Request a copy)Abstract
The regulation of chromatin structure and, therefore, transcriptional activity of histone proteins by reversible lysine acetylation is an important posttranslational modification. Inhibitors of histone deacetylase (HDAC) are considered as promising new anti-neoplastic drugs. The hydroxamic acid SAHA e. g. is currently used in the treatment of advanced primary cutaneous T-cell lymphoma. The EGFR protein tyrosine kinase inhibitor erlotinib is a prominent drug in cancer chemotherapy and currently approved for treatment of non-small cell lung cancer. In this report, we present a novel strategy for cancer drug development by a combination of EGFR/HER2 kinase and HDAC inhibitory activity in one molecule. By combining two distinct pharmacological properties in one molecule, we expect a broader activity spectrum and less likelihood of drug resistance in cancer patients. The combination led to substances with both HDAC inhibitory properties and EGFR as well as HER2 kinase inhibitory activities.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | CELL LUNG-CANCER; PHASE-II TRIAL; POTENT INHIBITORS; DERIVATIVES; MUTATIONS; GEFITINIB; LAPATINIB; ACIDS; ASSAY; |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 11 May 2020 07:31 |
| Last Modified: | 11 May 2020 07:31 |
| URI: | https://pred.uni-regensburg.de/id/eprint/18525 |
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