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Updated: Jun 21, 2026

Combining X-Ray Crystallography with Small Angle X-Ray Scattering to Model Unstructured Regions of Nsa1 from S. Cerevisiae
Published on: January 10, 2018
The use of ribosomal crystal structures in antibiotic drug design
1Rib-X Pharmaceuticals Inc, Department of Structure-Based Drug Design, 300 George Street, New Haven, CT 06511, USA. bwimberly@rib-x.com
Abstract:
The ribosome is one of the richest validated targets for antibacterial drug discovery. In combination with advances in computational and biological methods, the determination of ribosomal structures with bound substrates and inhibitors has launched a new era in the structure-based drug design (SBDD) of novel antibacterials. This review discusses the oxazolidone class of compounds, which has been the focus of most of the ribosome-targeted SBDD disclosed in the last 3 years; such SBDD has led to significant improvements in the potency and spectrum of activity of these compounds. Recent SBDD results for the aminoglycosides are also summarized, and ribosome-targeted compounds in clinical trials are reviewed. The encouraging results described support the future use of ribosomal SBDD in the development of antibiotic compounds.
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