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Bottromycin is a macrocyclic peptide with antibiotic activity. It was first discovered in 1957 as a natural product isolated from ''Streptomyces bottropensis''. It has been shown to inhibit methicillin-resistant ''Staphylococcus aureus'' (MRSA) and vancomycin-resistant Enterococci (VRE) among other Gram-positive bacteria and mycoplasma. Bottromycin is structurally distinct from both vancomycin, a glycopeptide antibiotic, and methicillin, a beta-lactam antibiotic. Bottromycin binds to the A site of the ribosome and blocks the binding of aminoacyl-''t''RNA, therefore inhibiting bacterial protein synthesis. Although bottromycin exhibits antibacterial activity ''in vitro'', it has not yet been developed as a clinical antibiotic, potentially due to its poor stability in blood plasma.〔 To increase its stability ''in vivo'', some bottromycin derivatives have been explored.〔 The structure of bottromycin contains a macrocyclic amidine as well as a thiazole ring. The absolute stereochemistry at several chiral centers has been determined as of 2009. In 2012, a three-dimensional solution structure of bottromycin was published. The solution structure revealed that several methyl groups are on the same face of the structure. Bottromycin falls within the ribosomally synthesized and post-translationally modified peptide class of natural product.〔 == History == Bottromycin was first isolated from ''Streptomyces bottropensis'' in 1957.〔 It has since been identified in at least two other members of the ''Streptomyces'' genus;〔〔 members of ''Streptomyces'' are known to be prolific producers of secondary metabolites. Bottromycin has a unique structure, consisting of the macrocyclic amidine linkage and four β-methylated amino acids. Bottromycin blocks aminoacyl ''t''RNA binding to the ribosome by binding to the A site of the 50s subunit.〔 Although bottromycin was discovered over 50 years ago, there was a lack of research following initial studies on bottromycin until recent years. The lack of research is potentially a result of bottromycin's low stability in blood plasma.〔 However, the unique structure and mode of action have recently made bottromycin a more target for drug development, especially given the rise of antibiotic resistance. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Bottromycin」の詳細全文を読む スポンサード リンク
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