This PhD project is focused on the improvable potency of small molecules to restore and reactivate the physiological functions of specific cellular signaling pathways involved in the development of serious and degenerative diseases, such as skin cancer, leukemia, neurodegenerative diseases. Hence, here is reported the synthesis and the biological evaluation of the Hedgehog pathway's agonists and antagonists, as well as the MRN Complex inhibitors. Moreover, we worked in the field of the bioconjugation with the synthesis of the so called molecular linkers, which have been then used to conjugate some known cytotoxic agents. The resulting payloads have been sent to prepare new Antibody Drug Conjugates (ADC) using specific monoclonal antibodies (mAbs)

Synthesis of small molecules active on tumor relevant cellular signaling pathways

GABRIELLI, ANNALISA;TADDEI, MAURIZIO
2017

Abstract

This PhD project is focused on the improvable potency of small molecules to restore and reactivate the physiological functions of specific cellular signaling pathways involved in the development of serious and degenerative diseases, such as skin cancer, leukemia, neurodegenerative diseases. Hence, here is reported the synthesis and the biological evaluation of the Hedgehog pathway's agonists and antagonists, as well as the MRN Complex inhibitors. Moreover, we worked in the field of the bioconjugation with the synthesis of the so called molecular linkers, which have been then used to conjugate some known cytotoxic agents. The resulting payloads have been sent to prepare new Antibody Drug Conjugates (ADC) using specific monoclonal antibodies (mAbs)
2017
Inglese
Target therapy, small molecules, Hedgehog, GSA-10, MRT-92, MRN complex, Mre11, Mirina, PFM39, Bioconjugation, linkers, payloads, ADC, Kadcyla, Adcetris
TADDEI, MAURIZIO
Università degli Studi di Siena
105
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.14242/304751
Il codice NBN di questa tesi è URN:NBN:IT:UNISI-304751