Eurostars project, SARTRIC, 8139, SARomics Biostructures

Purpose and goal

Antimicrobial resistance is a major global public health threat and societal burden with a high unmet medical need. SARTRIC addresses this growing problem with the development of small-molecule inhibitors that switch-off resistance gene expression and thus restore antibiotic activity. Characterization of existing hits and identification of new using computational chemistry methods and fragments-based drug design has been performed. These hits are now being developed into lead molecules that should be qualified to continue preclinical development.

Results and expected effects

SARTRIC has resulted in I) hits currently developed into lead molecules with the goal to undergo continued pre-clinical development II) identification of further hit molecules by fragment-based drug design and III) the implementation of a highly efficient platform for crystallization and structure-based drug design which permits routine handling of large quantities of samples that will come handy when MAX IV opens. If the molecules are working as they should hope exists that antibiotic resistance could be restored for common antibiotics.

Approach and implementation

The parties in SARTRIC have combined their complementary technology modules, knowledge and resources for the effective enforcement of the development process from early hit molecules to lead molecules that are eligible for continued pre-clinic development. The process has involved the determination of 3D target structures, a platform for massive data collection, fragment-based screening and SBDD for the improvement of existing hit molecules and for the identification of fragments that currently are developed into more mature compounds belonging to new structural families.