Serotonin derivatives as a new class of non-ATP-competitive receptor tyrosine kinase inhibitors
摘要:
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.
[EN] NON-PEPTIDE GLP-1 AGONISTS<br/>[FR] AGONISTES NON PEPTIDIQUES DE GLP-1
申请人:NOVO NORDISK AS
公开号:WO2000042026A1
公开(公告)日:2000-07-20
Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.