Alvos Biológicos
Os alvos enzimáticos em estudo no grupo na área de antiparasitários compreendem:
1. Gliceraldeído 3-fosfato desidrogenase (EC 1.2.1.12) GAPDH
2. Diidrooratado desidrogenase (EC 1.3.99.11) DHODH
3. Cruzaína (EC 3.4.22.51)
Os alvos macromoleculares de interesse na área de antitumorais são envolvidos com:
1. o receptor andrógeno (AR) e sua via de sinalização
2. mTOR e survivina, que estão envolvidas com o mecanismo de controle da morte celular
Uma nova estratégia para o combate ao cancer começa a ser desenhada no NEQUIMED:
“The target is a PTB domain from the protein Shc. There is an NMR structure for the domain. We would like to find an antagonist inhibitor for the site of binding for the phosphorylated receptor. The binding of a tyrosyl phosphopeptide on a receptor tyrosine kinase (RTK) to the PTB domain results in a conformational change which releases the pre-existing interaction of Shc with the MAP kinase, Erk which occurs at a distal site on the domain. The therapeutic benefit of an inhibitor in cancer is to prevent this Shc-RTK interaction occurring. This will effectively leave Erk bound to Shc and prevent it from translocating to the nucleus causing cell proliferation (and hence cancer). Thus the inhibitor cannot mimic the phosphotyrosine interaction of the activated receptor. This is a major challenge, but it could be fun to find a molecule. This would represent a completely novel approach to cancer therapy.”