title: Serotonin derivatives as a new class of non-ATP-competitive receptor tyrosine kinase inhibitors.
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.
authors.affiliation: Institut für Organische Chemie, Universität Leipzig, Johannisallee 29, D-04103 Leipzig, Germany.
authors.forename: Anita
authors.initials: A
authors.lastname: Büttner
authors.forename: Thomas
authors.initials: T
authors.lastname: Cottin
authors.forename: Jing
authors.initials: J
authors.lastname: Xu
authors.forename: Lito
authors.initials: L
authors.lastname: Tzagkaroulaki
authors.forename: Athanassios
authors.initials: A
authors.lastname: Giannis
mesh_terms: D000255:Adenosine Triphosphate / Q000737:chemistry / Q000494:pharmacology; D000494:Allosteric Regulation; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000187:drug effects / Q000378:metabolism; D012701:Serotonin / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D047428:Protein Kinase Inhibitors; D012701:Serotonin; D000255:Adenosine Triphosphate; D020794:Receptor Protein-Tyrosine Kinases