A potent seryl tRNA synthetase inhibitor SB-217452 isolated from a Streptomyces species.

A L Stefanska, M Fulston, C S Houge-Frydrych, J J Jones, S R Warr

SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.

The Journal of antibiotics 2000 Dec

filter terms:

A potent inhibitor of seryl tRNA synthetase, designated SB-217452 has been isolated from Streptomyces sp. ATCC 700974. The fermentation, isolation, structure elucidation and some properties are described. SB-217452 showed inhibitory activity against both Staphylococcus aureus and rat seryl tRNA synthetases, with similar IC50 values of approximately 8 nM. The inhibitor is the serine linked nucleoside moiety of the antibiotic albomycin delta2. In contrast to albomycin delta2, SB-217452 showed only very weak antibacterial activity against a limited range of microorganisms. The compound has not been previously reported as a naturally occurring metabolite. In addition to SB-217452, albomycin delta2 Fe3+ complex and the novel Al3+ complex were isolated from the fermentation. These complexes had no seryl tRNA synthetase inhibitory activity.

Citation

A L Stefanska, M Fulston, C S Houge-Frydrych, J J Jones, S R Warr. A potent seryl tRNA synthetase inhibitor SB-217452 isolated from a Streptomyces species. The Journal of antibiotics. 2000 Dec;53(12):1346-53