Design, synthesis and evaluation of inhibitors against tumour-associated protease

Proteases are a class of physiologically active proteins which lead different biochemistry reactions and are responsible to many physiology and pathology processes. Protease inhibitors therefore have emerged as potent therapeutic agents for various diseases. Successful examples include Cathepsin inh...

Full description

Bibliographic Details
Main Author: Hu, X.
Published: Queen's University Belfast 2012
Subjects:
Online Access:http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.557630
Description
Summary:Proteases are a class of physiologically active proteins which lead different biochemistry reactions and are responsible to many physiology and pathology processes. Protease inhibitors therefore have emerged as potent therapeutic agents for various diseases. Successful examples include Cathepsin inhibitors and HIV aspartste protease inhibitors, while the matrix metalloproteinase inhibitors are deemed to be failure examples. In this thesis, a series of inhibitors of two distinct proteases seprase and proteasome were designed, synthesized and evaluated through different methods. The assessment of methodologies and clinical applications was also provided in guiding the future works.