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Current Drug Targets


ISSN (Print): 1389-4501
ISSN (Online): 1873-5592

Discovery of Antibacterials and Other Bioactive Compounds from Microorganisms — Evaluating Methodologies for Discovery and Generation of Non-Ribosomal Peptide Antibiotics

Author(s): K. Witting and R. D. Sussmuth

Volume 12, Issue 11, 2011

Page: [1547 - 1559] Pages: 13

DOI: 10.2174/138945011798109527

Price: $65


After decades of neglect in industrial research the comeback of natural products is due since improved screening approaches are at disposal, yielding a multitude of new compounds from natural sources. Besides traditional compound libraries peptides are characterized by an enormous structural complexity, thus increasing the chance of finding a hit in a screening. Emphasizing antibacterial compounds structural complexity is a prerequisite for their success.

This review focuses on the screening approaches employed for the discovery of mostly antibacterial, non-ribosomal peptides derived from natural sources. Traditional screening methodologies as well as genetic approaches are discussed in this context. Utilizing genetic engineering methods e.g., precursor-directed biosynthesis, mutasynthesis, combinatorial biosynthesis, as well as chemoenzymatics to achieve greater structural diversity is thoroughly discussed and exemplified by recent discoveries.

Keywords: Antibacterials, peptides, screening approaches, genetic engineering, chemical screening, combinatorial biosynthesis, mutasynthesis, precursor-directed biosynthesis, Bioactive Compounds, Microorganisms

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