1228827-77-7Relevant articles and documents
Serotonin derivatives as a new class of non-ATP-competitive receptor tyrosine kinase inhibitors
Büttner, Anita,Cottin, Thomas,Xu, Jing,Tzagkaroulaki, Lito,Giannis, Athanassios
experimental part, p. 3387 - 3402 (2010/10/03)
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.