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. 1996 Sep;40(9):2226–2228. doi: 10.1128/aac.40.9.2226

Glycylcyclines bind to the high-affinity tetracycline ribosomal binding site and evade Tet(M)- and Tet(O)-mediated ribosomal protection.

J Bergeron 1, M Ammirati 1, D Danley 1, L James 1, M Norcia 1, J Retsema 1, C A Strick 1, W G Su 1, J Sutcliffe 1, L Wondrack 1
PMCID: PMC163507  PMID: 8878615

Abstract

N,N-dimethylglycylamido (DMG) derivatives of 6-demethyl-6-deoxytetracycline and doxycycline bind 5-fold more effectively than tetracycline to the tetracycline high-affinity binding site on the Escherichia coli 70S ribosome, which correlates with a 10-fold increase in potency for inhibition of E. coli cell-free translation. The potencies of DMG-doxycycline and DMG-6-demethyl-6-deoxytetracycline were unaffected by the ribosomal tetracycline resistance factors Tet(M) and Tet(O) in cell-free translation assays and whole-cell bioassays with a conditional Tet(M)-producing E. coli strain.

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Selected References

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