Table 1 Peptide structure–activity relationships (SAR) identify key requirements for biological activity and facilitate peptide optimization

From: Structure-based discovery of hydrocarbon-stapled paxillin peptides that block FAK scaffolding in cancer

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  1. Bolded amino acids indicate olefinic amino acids. Bolded peptide IDs indicate order of mention in the manuscript. UA codes refer to internal identification number utilized in compound database. Grayscale shaded amino acids indicate following properties: polar uncharged (light gray), negatively charged (gray), positively charged (dark gray). The reported KD values are the mean ± SD of 5 biological replicates (n = 5) for UA-1907; mean ± SD of 4 biological replicates (n = 4) for UA-1967, UA-1914, UA-1919, UA-2015, UA-2017, UA-1905, UA-1910, UA-1913, UA-2007, UA-1912, UA-2013, and UA-2014; mean ± SD of 3 biological replicates (n = 3) for UA-1921, UA-1920, UA-2011, UA-2009, and UA-1933; and mean ± SD of 2 biological replicates (n = 2) for UA-2010. All Ki values reported are the mean ± SD of 3 biological replicates (n = 3). All source data for derived KD and Ki values are provided as Source Data file.
  2. R8 (R)-2-(7-octenyl)alanine (unstapled), S5 (S)-2-(4-pentenyl)alanine, Aib 2-aminoisobutyric acid.
  3. *indicates unstapled peptide where ring-closing metathesis was not performed.
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