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Electronic theses and dissertations repository

 

Tesi etd-02072017-112046


Thesis type
Tesi di laurea magistrale LM5
Author
LICARI, CRISTINA
URN
etd-02072017-112046
Title
Synthesis of benzoylpiperidine-based MAGL inhibitors as prospective anticancer agents
Struttura
FARMACIA
Corso di studi
CHIMICA E TECNOLOGIA FARMACEUTICHE
Commissione
relatore Prof. Minutolo, Filippo
relatore Dott.ssa Granchi, Carlotta
Parole chiave
  • magl
  • reversible inhibitors
Data inizio appello
08/03/2017;
Consultabilità
parziale
Data di rilascio
08/03/2020
Riassunto analitico
Monoacylglycerol lipase (MAGL) is a serine hydrolase enzyme involved in many biological processes, such as the degradation of 2-arachidonoylglycerol (2-AG), one of the most important endocannabinoid neurotransmitters. Moreover, MAGL is upregulated in aggressive human cancer cells and primary tumors, where it has a unique role of providing lipolytic sources of free fatty acids for the synthesis of oncogenic signalling lipids that promote cancer aggressiveness.<br>Considering the numerous functions played by this enzyme, MAGL inhibitors may be useful for the treatment of pain, inflammation and cancer. <br>However, the use of irreversible MAGL inhibitors gives an unwanted chronic inactivation of this enzyme, which causes a functional antagonism of the endocannabinoid system, a mild physical dependence, and an impaired endocannabinoid-dependent synaptic plasticity. For all these reasons, the need to discover selective and reversible inhibitors is urgent. Considering what said above, the aim of this thesis work is the synthesis of reversible MAGL inhibitors. <br><br>
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