Site-directed ligand discovery

D. A. Erlanson , A. C. Braisted , D. R. Raphael , M. Randal , R. M. Stroud , E. M. Gordon , J. A. Wells

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DOI 10.1073/pnas.97.17.9367

Journal Proceedings of the National Academy of Sciences
Location p 9367-9372, Volume 97, Issue 17, 2000
Publication Type journal-article

Tags escherichia coli, protein engineering, ligands, thymidylate synthase, enzyme, binding sites, drug design, molecular weight, infectious disease, thermodynamics, protein conformation, multidisciplinary
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31 Jan 2021

Ken Hallenbeck

(1)

Important contribution to fragment hit-finding technologies

Logic / Design

Reproducibility

Impact

Transparency

Clarity

Versatility

Innovation

This paper by Erlanson and colleagues describes the disulfide tethering technique, which has proven to be a reproducible and versatile method for finding fragment hits. The main advance is the covalent targeting of the fragment library to a specific site on a protein surface....

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Site-directed ligand discovery

D. A. Erlanson , A. C. Braisted , D. R. Raphael , M. Randal , R. M. Stroud , E. M. Gordon , J. A. Wells

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Important contribution to fragment hit-finding technologies

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