Serotonin derivatives as a new class of non-ATP-competitive receptor tyrosine kinase inhibitors
Buettner, A; Cottin, T; Xu, J; Tzagkaroulaki, L; Giannis, A
| HERO ID | 1594177 |
|---|---|
| In Press | No |
| Year | 2010 |
| Title | Serotonin derivatives as a new class of non-ATP-competitive receptor tyrosine kinase inhibitors |
| Authors | Buettner, A; Cottin, T; Xu, J; Tzagkaroulaki, L; Giannis, A |
| Journal | Bioorganic & Medicinal Chemistry |
| Volume | 18 |
| Issue | 10 |
| Page Numbers | 3387-3402 |
| Abstract | The discovery of new templates and their subsequent elaboration to clinically useful receptor tyrosine kinase (RTK) inhibitors continues to be an important issue. RTKs are a class of enzymes responsible for the activation of different cellular signal transduction cascades. The majority of the known small molecules RTK inhibitors are ATP- competitive and they are multiple targeted inhibitors. We describe here serotonin derivatives as a new class of multiple targeted RTK inhibitors. In contrast to most other RTK inhibitors they act via a non-ATP-competitive (allosteric) mechanism. Furthermore, they are able to inhibit the proliferation of HUVE cells, fibroblasts and two cancer cell lines. (C) 2010 Elsevier Ltd. All rights reserved. |
| Doi | 10.1016/j.bmc.2010.04.001 |
| Pmid | 20456957 |
| Wosid | WOS:000277545900004 |
| Is Certified Translation | No |
| Dupe Override | No |
| Comments | Source: Web of Science WOS:000277545900004Scopus URL: https://www.scopus.com/inward/record.uri?eid=2-s2.0-77953126861&doi=10.1016%2fj.bmc.2010.04.001&partnerID=40&md5=45f781c1ad2a68dd21de0c70a146b631 |
| Is Public | Yes |
| Language Text | English |
| Keyword | Receptor tyrosine kinases; Serotonin; Carbazole; Inhibitor |