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. Pignataro
Penultimo
;
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.
Settore CHIM/06 - Chimica Organica
   Tumor-targeting peptidomimetics: synthesis and bio-medical applications
   MINISTERO DELL'ISTRUZIONE E DEL MERITO
   20157WW5EH_001
14-ago-2021
5-lug-2021
https://pubs.rsc.org/en/content/articlelanding/2021/cc/d1cc02895b
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/854634
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