The Antibody-Drug Conjugates (ADCs) is one of the novel therapeutic strategies with a great potential in many medicinal treatments. ADCs are composed of a monoclonal antibody (mAb) connected to a drug (payload) through a properly designed linker. The mAb is responsible for the selective transport of the drug into target cells expressing the specific antigen; in this way, the off-target toxicity of the drug can be avoided. The linker plays an important role due to its dual features: stability in blood and ability to release the payload into the target cells thanks to its degradation. In this thesis, several different aspects of the ADC development are explored. Different ADCs charged with SMO inhibitors as payload are investigated for the treatment of melanoma, and novel multifunctional linkers with trigger groups are designed for the drug release in different environments in a very elegant and controlled way. Besides the work on bioconjugates aforementioned, micellar catalysis is also investigated to perform catalytic transformations in water media avoiding the use of organic solvents. Micellar catalysis is applied in the presence of a proper rhodium salt to develop a suitable hydroformylation process with very good results.

Migliorini, F. (2022). New biocojugates for targeted anticancer therapy [10.25434/migliorini-francesca_phd2022].

New biocojugates for targeted anticancer therapy

Migliorini, Francesca
2022-01-01

Abstract

The Antibody-Drug Conjugates (ADCs) is one of the novel therapeutic strategies with a great potential in many medicinal treatments. ADCs are composed of a monoclonal antibody (mAb) connected to a drug (payload) through a properly designed linker. The mAb is responsible for the selective transport of the drug into target cells expressing the specific antigen; in this way, the off-target toxicity of the drug can be avoided. The linker plays an important role due to its dual features: stability in blood and ability to release the payload into the target cells thanks to its degradation. In this thesis, several different aspects of the ADC development are explored. Different ADCs charged with SMO inhibitors as payload are investigated for the treatment of melanoma, and novel multifunctional linkers with trigger groups are designed for the drug release in different environments in a very elegant and controlled way. Besides the work on bioconjugates aforementioned, micellar catalysis is also investigated to perform catalytic transformations in water media avoiding the use of organic solvents. Micellar catalysis is applied in the presence of a proper rhodium salt to develop a suitable hydroformylation process with very good results.
2022
Migliorini, F. (2022). New biocojugates for targeted anticancer therapy [10.25434/migliorini-francesca_phd2022].
Migliorini, Francesca
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/1196224