Russomanno, Pasquale (2021) Design of Small Molecules with Antitumor Activity through Computational Methodologies. [Tesi di dottorato]

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Item Type: Tesi di dottorato
Resource language: English
Title: Design of Small Molecules with Antitumor Activity through Computational Methodologies
Creators:
CreatorsEmail
Russomanno, Pasqualepasquale.russomanno@unina.it
Date: 2021
Number of Pages: 174
Institution: Università degli Studi di Napoli Federico II
Department: Farmacia
Dottorato: Scienza del farmaco
Ciclo di dottorato: 33
Coordinatore del Corso di dottorato:
nomeemail
D'Auria, Maria Valeriamariavaleria.dauria@unina.it
Tutor:
nomeemail
Marinelli, LucianaUNSPECIFIED
Date: 2021
Number of Pages: 174
Keywords: Cancer, Drug Discovery, NMR
Settori scientifico-disciplinari del MIUR: Area 03 - Scienze chimiche > CHIM/08 - Chimica farmaceutica
Additional information: recapito telefonico +39 3889553041
Date Deposited: 20 Jul 2021 14:37
Last Modified: 07 Jun 2023 11:09
URI: http://www.fedoa.unina.it/id/eprint/14072

Collection description

Today, there are multiple targeted therapies against cancer. The most relevant ones are those aimed at the stop of cancer cells from growing, or at the halting of signals that stimulate blood vessels, or at helping the immune system destroy cancer cells, and many others. The last one, has achieved impressive results to date. Indeed, the immuno- oncology field is entering a new, exciting phase having the potential to change the current cancer treatment either as a standalone therapy or in combination. Recently, many innovative strategies exist to overcome tumor-induced immunosuppression. Currently the main ones are checkpoint blockade inhibitors, adoptive T cell transfers, and vaccination strategies. To date, the immuno-oncology therapeutics on the market are mostly biologic products (e.g. monoclonal antibodies (mAbs), proteins, engineered cells, and oncolytic viruses). However, for example, antibodies have specific drawbacks: high production costs, lack of oral bioavailability, poor tumor penetrating capacity, Fc-related toxicities, and immunogenic properties. In this perspective, small molecules could potentially overcome many of these issues and be complementary to, and potentially synergistic with, biologic therapeutics too. In this context, my PhD work was focused on discovery of small molecules targeting three different proteins: MDM2 (Mouse Double Minute 2) the PD-1/PD-L1 axis (Programmed cell Death protein-1/ Programmed Death-ligand 1), and STING protein (STimulator of INterferon Genes). For all targets, a tandem approach of computational studies/NMR spectroscopy was applied.

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