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Cilengitide: the first anti-angiogenic small molecule drug candidate. Design, synthesis and clinical evaluation

Autor
Mas-Moruno, C.; Rechenmacher, F.; Kessler, H.
Tipus d'activitat
Article en revista
Revista
Anti-cancer agents in medicinal chemistry
Data de publicació
2010
Volum
10
Número
10
Pàgina inicial
753
Pàgina final
768
DOI
https://doi.org/10.2174/187152010794728639 Obrir en finestra nova
URL
http://www.eurekaselect.com/57631/article Obrir en finestra nova
Resum
Cilengitide, a cyclic RGD pentapeptide, is currently in clinical phase III for treatment of glioblastomas and in phase II for several other tumors. This drug is the first anti-angiogenic small molecule targeting the integrins avß3, avß5 and a5ß1. It was developed by us in the early 90s by a novel procedure, the spatial screening. This strategy resulted in c(RGDfV), the first superactive avß3 inhibitor (100 to 1000 times increased activity over the linear reference peptides), which in additio...
Grup de recerca
CRnE - Centre de Recerca en Ciència i Enginyeria Multiescala de Barcelona

Participants