Static and dynamic crystallographic investigations for developing new inhibitors for the epigenetic therapy of cancers.
Project funded in the framework of the collaboration between CNR and the National Research Fundation of Korea (NRF)
Funding for the Institute of Crystallography: 20000,00 €
SHORT DESCRIPTION AND USEFUL INFO:
The development of epigenetic therapies is the latest frontier in the fight against cancer. Although the role of histone post-translational modifications (PTM) is still not fully understood, it is today unanimously acquired that the enzymes that catalyze the addition or removal of PTMs are novel candidate therapeutic targets in cancer.
The project aims at elucidating the crystal structures of transcriptional co-regulators Histone lysine methyltransferases complexed with candidate inhibitors and to develop lead compounds by a structure-based drug design based on static and dynamic investigations.
The project will allow discovering new inhibitors for histone modifications like lysine methylation, which can affect transcriptional events. These results will open new routes for collaborating with pharmaceutical companies interested into targeting epigenetic regulators for cancer therapy, and will allow preparing competitive proposals for forthcoming calls.
Link korean partner: http://webbuild.knu.ac.kr/~diluccio/structuralbiology/Welcome.html
Italian Coordinator : ROCCO CALIANDRO
National Research Council of Italy (CNR)
Institute of Crystallography (IC)
Via G, Amendola 122/o
70126 Bari (BA), Italy
Tel.: +39 0805929150; Fax: +39 0805929170