Tesi etd-09202013-121915 |
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Tipo di tesi
Tesi di laurea specialistica LC5
Autore
ANTONI, CLAUDIA
URN
etd-09202013-121915
Titolo
Design, Synthesis, X-ray analysis and preliminary Biological evaluation of Powerful Dual inhibitors for MMP homodimerization.
Dipartimento
FARMACIA
Corso di studi
CHIMICA E TECNOLOGIA FARMACEUTICHE
Relatori
relatore Prof. Rossello, Armando
relatore Dott.ssa Nuti, Elisa
relatore Dott. Stura, Enrico A.
relatore Dott.ssa Nuti, Elisa
relatore Dott. Stura, Enrico A.
Parole chiave
- homodimerization
- inhibitors
- MMPs
Data inizio appello
09/10/2013
Consultabilità
Completa
Riassunto
AIMS OF THE THESIS
This work aims to investigate the role of the linker when used to join two different or identical chemical entities in a biological context. The chemical structure of the linker has been given little importance and the possible interaction that it makes with proteins overlooked. The difficulty in going beyond the consideration of length and branch point is given by the difficulty in obtaining structural information. In this work we have been able to overcome these difficulties and by employing crystallization and X-ray structure determination to understand how linker length and branch point influences the inhibition of MMPs, our model enzyme system. The results presented here can be used to pursue a more detailed structure-guided spacer design.
This work aims to investigate the role of the linker when used to join two different or identical chemical entities in a biological context. The chemical structure of the linker has been given little importance and the possible interaction that it makes with proteins overlooked. The difficulty in going beyond the consideration of length and branch point is given by the difficulty in obtaining structural information. In this work we have been able to overcome these difficulties and by employing crystallization and X-ray structure determination to understand how linker length and branch point influences the inhibition of MMPs, our model enzyme system. The results presented here can be used to pursue a more detailed structure-guided spacer design.
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