Interaction of tyrosyl aryl dipeptides with S. aureus tyrosyl tRNA synthetase: inhibition and crystal structure of a complex. |
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| Authors: | R L Jarvest J M Berge C S Houge-Frydrych C Janson L M Mensah P J O'Hanlon A Pope A Saldanha X Qiu |
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| Affiliation: | SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK. Richard_L_Jarvest@sbphrd.com |
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| Abstract: | Tyrosyl aryl dipeptide inhibitors of S. aureus tyrosyl tRNA synthetase have been identified with IC50 values down to 0.5 microM. A crystal structure of the enzyme complexed to one of the inhibitors shows occupancy of the tyrosyl binding pocket coupled with inhibitor interactions to key catalytic residues. |
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