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Increasing avß3 selectivity of the anti-angiogenic drug cilengitide by N-methylation

Autor
Mas-Moruno, C.; Beck, J.G.; Doedens, L.; Frank, A.O.; Marinelli, L.; Cosconati, S.; Novellino, E.; Kessler, H.
Tipus d'activitat
Article en revista
Revista
Angewandte chemie. International edition
Data de publicació
2011
Volum
50
Número
40
Pàgina inicial
9496
Pàgina final
9500
DOI
https://doi.org/10.1002/anie.201102971 Obrir en finestra nova
Repositori
http://hdl.handle.net/2117/22785 Obrir en finestra nova
URL
http://onlinelibrary.wiley.com/doi/10.1002/anie.201102971/abstract Obrir en finestra nova
Resum
Thumbnail image of graphical abstract A subtle change: Structural changes upon amide bond methylation improve the selectivity of the anti-angiogenic drug Cilengitide, which after N-methylation at distinct positions discriminates between the closely related pro-angiogenic integrins avß3 and avß5 (see scheme).
Citació
Mas-Moruno, C. [et al.]. Increasing avß3 selectivity of the anti-angiogenic drug cilengitide by N-methylation. "Angewandte chemie. International edition", 2011, vol. 50, núm. 40, p. 9496-9500.
Paraules clau
N-methylation, conformational studies, cyclic peptides, integrin, receptor selectivity
Grup de recerca
CRnE - Centre de Recerca en Ciència i Enginyeria Multiescala de Barcelona

Participants

  • Mas Moruno, Carlos  (autor)
  • Beck, J.G.  (autor)
  • Doedens, L.  (autor)
  • Frank, A.O.  (autor)
  • Marinelli, L.  (autor)
  • Cosconati, S.  (autor)
  • Novellino, E.  (autor)
  • Kessler, Horst  (autor)