Probes for Neurological Diseases
The research group is involved in the design and syntesis of chemical probes for enzymes involved in the excitatory pathways in the CNS.
Our current interests are focused on enzymes belonging to the kynurenine pathway of tryptophan metabolism, and in particular on 3HAO, the enzyme synthesizing the neurotoxic
quinolinic acid, and on serine racemase, the enzyme synthesing D-serine, the endogenous co-agonist of the NMDA receptors.
For further information feel free to contact Gabriele Costantino
Recent publications:
- Vallerini, G.P., Amori, L., Beato, C., Tararina, M., Wang, X.-D., Schwarcz, R., Costantino, G. 2-Aminonicotinic acid 1-oxides are chemically stable inhibitors of quinolinic acid synthesis in the mammalian brain: A step toward new antiexcitotoxic agents (2013) Journal of Medicinal Chemistry, 56 (23), pp. 9482-9495. DOI: 10.1021/jm401249c
- Bruno, A., Amori, L., Costantino, G. Addressing the conformational flexibility of serine racemase by combining targeted molecular dynamics, conformational sampling and docking studies (2011) Molecular Informatics, 30 (4), pp. 317-328. DOI: 10.1002/minf.201000162
- New promises for manipulation of kynurenine pathway in cancer and neurological diseases. Costantino G. Expert Opin Ther Targets 2009 Feb;13(2), 247-58
DOI: 10.1517/14728220802665734
