Chemical screening methods to identify ligands that promote protein stability, protein crystallization, and structure determination

By M. Vedadi, F. Niesen, A. Allali-Hassani, O. Fedorov, P. Finerty, G. Wasney, Ron Yeung, C. Arrowsmith, Linda J. Ball, H. Berglund and 6 more. Proceedings of the National Academy of Sciences of the United States of America, 2006

605 citations recorded by the source corpus.

Subfields: Materials Chemistry, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/44fd285b428da5ebe3b8a0ca714f5bb2a0f6a41c

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In Materials Chemistry

1. B. V. Potter
2. S. J. Mills
3. C. Silvander
4. P. Nordlund
5. L. Trésaugues
6. G. Cozier

In Molecular Biology

1. Ye Fang
2. B. Kuster
3. Marcus Bantscheff
4. Mikhail M. Savitski
5. Alexey I. Nesvizhskii

Citations in the corpus

• The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability (2007, background): “It has been shown that the stabilizing effect of compounds upon binding is proportional to the concentration and affinity of the ligand”
• Ligand–receptor interaction platforms and their applications for drug discovery (2012, background): “For most proteins, Tagg and Tm values are reasonably close [113].”
• Crystal Structures of Type-II Inositol Polyphosphate 5-Phosphatase INPP5B with Synthetic Inositol Polyphosphate Surrogates Reveal New Mechanistic Insights for the Inositol 5-Phosphatase Family (2016, positive): “One such method developed by the Structural Genomics Consortium (SGC) [15] uses light scattering-based approaches to measure the variation of the thermal stability of proteins (thermal-shift) when screened against a library of compounds.”
• Protein stability by number: high-throughput and statistical approaches to one of protein science’s most difficult problems (2011, neutral): “Most laboratory implementations of DSF, which is used extensively to optimize buffer conditions for crystallography [38,39], use real-time PCR machines that typically lack filter sets in the blue.”
• High-throughput production of human proteins for crystallization: The SGC experience (2010, background): “In some cases it has been possible to identify stabilizing conditions by systematic screens using fluorescence or static light scattering (Vedadi et al., 2006).”
• Tracking cancer drugs in living cells by thermal profiling of the proteome (2014, background): “For many proteins, a good correlation between the thermofluor unfolding assay and heat-induced precipitation in solution, or in cells by CETSA, has been demonstrated (11, 17), suggesting that properly shaped curves represent real unfolding events.”
• Meclofenamic acid selectively inhibits FTO demethylation of m6A over ALKBH5 (2014, background): “Although no linear correlation of the degree of temperature shift upon ligand binding with binding affinity could be established (54,55), this high degree of Tm shift of FTO by MA, at least in this one instance, suggests direct binding of the MA inhibitor to the target FTO.”