Cyclative cleavage of an amine-carbamate self-immolative spacer to deliver a hydroxyl cargo was inhibited by the spacer derivatisation with a phosphate monoester handle. This trifunctional spacer was installed in a model anticancer prodrug which showed a fast drug release only when incubated with both a protease and a phosphatase enzymes.
A Trifunctional Self-Immolative Spacer Enables Drug Release with Two Non-Sequential Enzymatic Cleavages / A. Dal Corso, S. Arosio, N. Arrighetti, P. Perego, L. Belvisi, L.L. Pignataro, C.M.A. Gennari. - In: CHEMICAL COMMUNICATIONS. - ISSN 1359-7345. - 57:63(2021 Aug 14), pp. 7778-7781. [10.1039/D1CC02895B]
A Trifunctional Self-Immolative Spacer Enables Drug Release with Two Non-Sequential Enzymatic Cleavages
A. DAL CORSO
Primo
;L. Belvisi;L.L. PignataroPenultimo
;C.M.A. Gennari
Ultimo
2021
Abstract
Cyclative cleavage of an amine-carbamate self-immolative spacer to deliver a hydroxyl cargo was inhibited by the spacer derivatisation with a phosphate monoester handle. This trifunctional spacer was installed in a model anticancer prodrug which showed a fast drug release only when incubated with both a protease and a phosphatase enzymes.
| File | Dimensione | Formato | |
|---|---|---|---|
|
ChemComm_Manuscript_POSTPRINT.pdf
accesso aperto
Tipologia:
Pre-print (manoscritto inviato all'editore)
Dimensione
980.38 kB
Formato
Adobe PDF
|
980.38 kB | Adobe PDF | Visualizza/Apri |
|
d1cc02895b.pdf
accesso riservato
Tipologia:
Post-print, accepted manuscript ecc. (versione accettata dall'editore)
Dimensione
1.52 MB
Formato
Adobe PDF
|
1.52 MB | Adobe PDF | Visualizza/Apri Richiedi una copia |
|
d1cc02895b.pdf
accesso riservato
Tipologia:
Publisher's version/PDF
Dimensione
2.52 MB
Formato
Adobe PDF
|
2.52 MB | Adobe PDF | Visualizza/Apri Richiedi una copia |
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
