Abstract
Target identification through chemical biology has been considered one of the most efficient approaches for drug discovery. Thienopyrimidine derivatives were designed to discover potent IκB kinase β (IKKβ) inhibitors based on a known IKKβ inhibitor library. Most of the thienopyrimidine derivatives inhibited nitric oxide and tumor necrosis factor alpha, which are downstream of the NF-κB signaling pathway, but not IKKβ. To identify the appropriate targets of thienopyrimidine analogues, chemical biology approaches, including text mining and a subsequent kinase panel assay from the kinome profiling were used. Based on the results, Fms-like tyrosine kinase 3 was found to be the target for thienopyrimidine derivatives, and was confirmed to be a potent inhibitor for acute myeloid leukemia.
Original language | English |
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Article number | 634 |
Pages (from-to) | 1575-1581 |
Number of pages | 7 |
Journal | Archives of pharmacal research |
Volume | 38 |
Issue number | 9 |
DOIs | |
Publication status | Published - 2015 Sept 1 |
Bibliographical note
Publisher Copyright:© 2015 The Pharmaceutical Society of Korea.
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery
- Organic Chemistry