Serotonin derivatives as a new class of non-ATP-competitive receptor tyrosine kinase inhibitors |
| |
Authors: | Anita Büttner Thomas Cottin Jing Xu Lito Tzagkaroulaki Athanassios Giannis |
| |
Institution: | Institut für Organische Chemie, Universität Leipzig, Johannisallee 29, D-04103 Leipzig, Germany |
| |
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. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|