ESR12

Design and synthesis of selective MMP-9 inhibitors and synthesis of modulators for ADAMTS4

 

 

 

Background:

Recent studies have unveiled the strong role of matrix metalloproteinase-9 (MMP-9) in epileptogenesis in a variety of animal models, showing an up-regulation of the protease in epileptogenic lesions. It is known that MMP-9 is involved in synaptic plasticity, learning and memory. Despite the robust evidences of the role of MMP-9 in the development and/or maintenance of epilepsy and their potential use as a therapeutic target, currently there are no selective MMP-9 inhibitors/ modulators for this metalloproteinase, which has impaired their use as clinical target. Non-selective inhibitors have been recognized to have strong side effects and toxicity thus limiting their therapeutic use. In this project, we aim: (1) to design and synthesise a selective peptide MMP-9 inhibitor. (2) To demonstrate the selectivity and potency of the designed MMP-9 inhibitors over other MMP family members. (3) To improve and refine the potency and ADME properties of the most promising MMP-9 inhibitor candidate. (4) To validate the role of MMP-9 in epileptogenesis and epilepsy.

 

 

Supervisors:  Professor Ernest Giralt (or someone with similar expertise), University of Barcelona, and Dr. Roger Prades, Dr. Teresa Tarragó (or someone with similar expertise), iproteos.

 

 

To apply : 

http://www.iproteos.com/phd-fellowship-at-iproteos-barcelona/

 

Person to contact for further details: Dr. Teresa Tarragó