XRS Box (106-aa adducts) biological testing results (updating) #37
Description
The following compounds for XRS Box were synthesised and sent to TGSLS for potency evaluation against P. falciparum 3D7. The results have been received as below and will keep updating until I finish all the analogs. The raw data file attached below. (all L-amino acid bought as reagents)
The reason we want to make XRS Box (all 106-aa adducts):
1) If this reaction hijacking mechanism operates with AsnRS, to generate an Asn-derived inhibitor, might OSM-S-106 be a multi-targeting inhibitor, able to form other amino-acid derived inhibitors of other tRNA synthetases in situ? Clearly it would be challenging for the parasite to develop resistance to such a molecule if it simultaneously targets several enzymes.
2) Might other amino acid conjugates of OSM-S-106 be effective drug candidates?
3) Might these molecules inhibit tRNA synthetases in other pathogens? OSM-S-106 and Asn-106 display no cytotoxicity vs HepG2, clearly indicating their potential for use vs pathogens in humans.