Tetracycline

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Tetracycline (INN) (pronounced /ˌtɛtrəˈsaɪkliːn/) is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and played a historical role in reducing the incidence of mortality because of cholera. It is sold under the brand names Sumycin, Terramycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber form, used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics.

Contents

Mechanism of action

Tetracyclines bind to the 30S subunit of microbial ribosomes. They inhibit protein synthesis by blocking the attachment of charged aminoacyl-tRNA. Thus they prevent introduction of new amino acids to the nascent peptide chain. The action is usually inhibitory and reversible upon withdrawal of the drug. Resistance to the tetracyclines results from changes in permeability of the microbial cell envelope. In susceptible cells, the drug is concentrated from the environment and does not readily leave the cell. In resistant cells, the drug is not actively transported into the cell or leaves it so rapidly that inhibitory concentrations are not maintained. This is often plasmid-controlled. Mammalian cells do not actively concentrate tetracyclines.

History

The tetracyclines are a large family of antibiotics that were discovered as natural products by Benjamin Minge Duggar and first described in 1948.[1] Under Yellapragada Subbarao, Benjamin Duggar made his discovery of the world's first tetracycline antibiotic, Aureomycin, in 1945.

In 1950, Harvard Professor Robert Woodward determined the chemical structure of Terramycin, the brand name for a member of the tetracycline family; the patent [1] protection for its fermentation and production was also first issued in 1950. A research team of seven scientists (Drs. K.J. Brunings, Francis A. Hochstein, C.R. Stephens, L.H. Conover, Abraham Bavley, Richard Pasternack, and Peter P. Regna) at Pfizer [2] [3], in collaboration with Woodward, participated in the two-year research leading to the discovery [4].

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