Francesco NICOTRA

1
Francesco NICOTRA

•  Macchine Molecolari per il Trasporto e il
  Rilascio Selettivo di Farmaci

 DIPARTIMENTO DI BIOTECNOLOGIE E BIOSCIENZE
2
Molecular Machinary for Drug Transport and Release
Iminosugars, RAS inhibitors Tyrosine kinase
inhibitors
Folic acid RGD, . Estrogens
Drug
ligand
Linker
internalisation
-S-S- or acid labile or glucuronic acid or
photolabile
Endocytosis Permeabilization after
cleavage Selective tansport mechanisms
3
Protein (cell)-ligand binding studies by NMR
LP 201 1 mM 50 µM
5RAS-GDP STD-1D on-resonance freq. 401.44 Hz
5RAS-GDP 1H
Peri F., Airoldi C., Colombo S, Mari S,
Jiménez-Barbero J., Martegani E., Nicotra F.
Chem. Eur. J., 2006, 3707