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Current Topics in Medicinal Chemistry
ISSN (Print): 1568-0266
ISSN (Online): 1873-5294
VOLUME: 3
ISSUE: 9
DOI: 10.2174/1568026033452131      Price:  $58









Aminoglycoside and its Derivatives as Ligands to Target the Ribosome

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Author(s): Jeffrey B.-H. Tok and Lanrong Bi
Pages 1001-1019 (19)
Abstract:
Protein synthesis is a central function in cellular physiology, and this important process is the target of many naturally occurring antibiotics and toxins. One such antibiotic is the aminoglycoside, which has been widely utilized in the clinical in the last fifty years due to their low cost and reliable activities. However the usage and applications of aminoglycosides have been severely limited due to their numerous side effects and resistance mechanism acquired by bacteria. Advances in understanding their mechanism of action have led to attempts in developing novel aminoglycoside-derivatives that would potentially eliminate harmful side effects and be resistant to aminoglycoside-modifying enzymes. This account provides a brief introduction to the various classes of antibiotics that target the ribosome, and also provide highlights in recent advancement of the synthesis of aminoglycoside analogs.
Keywords:
aminoglycoside, antibiotics, translation, ribosome, drug-resistance enzymes, aminoglycoside analogs, nmr, xray crystallography
Affiliation:
York College and Graduate Center, The City University of New York, Department ofChemistry&Natural Sciences, 94-20 Guy R. Brewer Blvd., Jamaica, NY11451, USA