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Pharmacophoric modifications lead to superpotent avß3 integrin ligands with suppressed a5ß1 activity

Autor
Neubauer, S.; Rechenmacher, F.; Brimioulle, R.; Di Leva, F.S.; Bochen, A.; Sobahi, T.; Schottelius, M.; Novellino, E.; Mas-Moruno, C.; Marinelli , L.; Kessler, H.
Tipus d'activitat
Article en revista
Revista
Journal of medicinal chemistry
Data de publicació
2014-04-24
Volum
57
Número
8
Pàgina inicial
3410
Pàgina final
3417
DOI
https://doi.org/10.1021/jm500092w Obrir en finestra nova
Repositori
http://hdl.handle.net/2117/23048 Obrir en finestra nova
URL
http://pubs.acs.org/doi/abs/10.1021/jm500092w Obrir en finestra nova
Resum
The selective targeting of the avß3 integrin subtype without affecting the structurally closely related receptor a5ß1 is crucial for understanding the details of their biological and pathological functions and thus of great relevance for diagnostic and therapeutic approaches in cancer treatment. Here, we present the synthesis of highly active RGD peptidomimetics for the avß3 integrin with remarkable selectivity against a5ß1. Incorporation of a methoxypyridine building block into a ligand sca...
Citació
Neubauer, S. [et al.]. Pharmacophoric modifications lead to superpotent avß3 integrin ligands with suppressed a5ß1 activity. "Journal of medicinal chemistry", 24 Abril 2014, vol. 57, núm. 8, p. 3410-3417.
Grup de recerca
BBT - Biomaterials, Biomecànica i Enginyeria de Teixits
CRnE - Centre de Recerca en Ciència i Enginyeria Multiescala de Barcelona

Participants

  • Neubauer, Stefanie  (autor)
  • Rechenmacher, Florian  (autor)
  • Brimioulle, Richard  (autor)
  • Di Leva, Francisco Saverio  (autor)
  • Bochen, Alexander  (autor)
  • Sobahi, Tariq R.  (autor)
  • Schottelius, Margret  (autor)
  • Novellino, Ettore  (autor)
  • Mas Moruno, Carlos  (autor)
  • Marinelli, Luciana  (autor)
  • Kessler, Horst  (autor)