Télévie: Design and enzymatic evaluation of new inhibitors of the serin metabolic pathway as potential anticancer agents : structural and functional approach of PHDGH and PSAT1.

Project: Research

Description

This project aims to understand the role of the serine pathway in tumor progression and in particular to develop pharmacological tools to evaluate the extent of tumor addiction to this metabolic path and their therapeutic potential by exploring potential side effects on healthy tissues.
To this end, novel innovative pharmacological inhibitors of PHGDH and PSAT1, the two main enzymes of the serine pathway, will be designed and chemically synthesized. These compounds will help deciphering the exact roles of these enzymes in cancer progression and will provide insights on their physiological roles.
This project will benefit from a collaboration between UNamur (Prof J.Wouters, structural study through protein crystallography and modelling ) and UCL (Prof R.Frédérick ( LDRI ) medicinal chemistry and chemical synthesis & Prof O.Feron ( IREC ) tumor hypoxia and metabolism). Together, this combined complementary expertise will allow
i) the design and synthesis of novel anticancer agents using a structure- guided drug design strategy and
ii) the biological evaluation on the tumor metabolism of the inhibitors via cellular testing.
StatusFinished
Effective start/end date1/10/1530/09/17