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- W859102647 abstract "Tetracycline appears to bind directly to the S7 protein and to the region of 16S RNA from bases 892 to 1054. The hydroxyl group of tetracycline binds to the A892 base. At physiological pH, the tetracyclines exist as a mixture of two forms: (i) a low-energy, nonionized, lipophilic form and (ii) a high-energy zwitterionic form. Resistance to the action of tetracyclines is due principally to the acquisition of the Tet determinant and not to a chromosomally mediated mutation. The mechanisms of resistance of Neisseria gonorrhoeae are an exception. The tet(A) and tet(R) gene repressor and the TetA export molecule recognize the tetracyclines in the form of the chelation complex. Tet(M) and Tet(O) are 70% homologous in terms of their amino acid sequence, and likewise Otr(A), Tet(B)(P), and Tet(Q) are 45% homologous and form a third group. They appear to prevent the binding of tetracyclines to the ribosomes. The pharmacokinetics of thiacycline were determined versus those of doxycycline by Dingeldein and Ungethum in 17 volunteers. Single doses of 100 and 200 mg of thiacycline and 200 mg of doxycycline were administered orally. The aglycone, dactylocyclinone or Sch-34164, possesses cross-resistance with the tetracyclines and is active against gram-negative bacteria. The MICs of minocycline are lower and dependent on the nature of the tet determinant. Tigecycline exhibits good in vitro activity against Streptococcus mitis, Streptococcus anginosus, Streptococcus sanguinis, Streptococcus bovis, and Streptococcus salivarius, with MICs under 0.25 µg/ml." @default.
- W859102647 created "2016-06-24" @default.
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- W859102647 date "2014-04-30" @default.
- W859102647 modified "2023-09-23" @default.
- W859102647 title "Tetracyclines Under Investigation" @default.
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- W859102647 doi "https://doi.org/10.1128/9781555815929.ch25" @default.
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