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Digital archive of theses discussed at the University of Pisa

 

Thesis etd-09202013-121915


Thesis type
Tesi di laurea specialistica LC5
URN
etd-09202013-121915
Thesis title
Design, Synthesis, X-ray analysis and preliminary Biological evaluation of Powerful Dual inhibitors for MMP homodimerization.
Department
FARMACIA
Course of study
CHIMICA E TECNOLOGIA FARMACEUTICHE
Supervisors
.
relatore Prof. Rossello, Armando
relatore Dott.ssa Nuti, Elisa
relatore Dott. Stura, Enrico A.
Keywords
  • homodimerization
  • inhibitors
  • MMPs
Graduation session start date
09/10/2013
Availability
Full
Abstract (Inglese)
Abstract (Italiano)
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.
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