4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo

Autor:	Scott K. Thompson, Randall K. Johnson, Thau F. Ho, Keith W. Ward, Lara S. Kallander, Thaddeus A. Tomaszek, Cheryl A. Janson, Kyung O. Johanson, Robert B. Kirkpatrick, Ward W. Smith, Guang Yang, Michael R. Mattern, Gui-Feng Zhang, Christina K. Schulz-Pritchard, Michael J Hansbury, Ryan M Dominic, Wenfang Chen, James D. Winkler, Thomas D. Meek, Daniel F. Veber, David G. Tew, Qing Lu, P.W. Fisher, Glenn A. Hofmann
Rok vydání:	2005
Předmět:	Models Molecular Angiogenesis Methionyl aminopeptidase Biological Availability Angiogenesis Inhibitors Crystallography X-Ray Aminopeptidases Mice Structure-Activity Relationship In vivo Drug Discovery Animals Humans Cells Cultured Cell Proliferation Matrigel Binding Sites biology Molecular Structure Chemistry Endothelial Cells Metalloendopeptidases Cobalt Triazoles Small molecule METAP2 Rats Endothelial stem cell Enzyme Activation Drug Combinations Biochemistry Enzyme inhibitor biology.protein Molecular Medicine Proteoglycans Collagen Endothelium Vascular Laminin
Zdroj:	Journal of medicinal chemistry. 48(18)
ISSN:	0022-2623
Popis:	Inhibitors of human methionine aminopeptidase type 2 (hMetAP2) are of interest as potential treatments for cancer. A new class of small molecule reversible inhibitors of hMetAP2 was discovered and optimized, the 4-aryl-1,2,3-triazoles. Compound 24, a potent inhibitor of cobalt-activated hMetAP2, also inhibits human and mouse endothelial cell growth. Using a mouse matrigel model, this reversible hMetAP2 inhibitor was also shown to inhibit angiogenesis in vivo.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf1be748eb5e7ee3f51352eb14a0c3d0 https://pubmed.ncbi.nlm.nih.gov/16134930 Zobrazit plný text záznamu