Article
Structure-activity relationships of Bak derived peptides: affinity and specificity modulations by amino acid replacement.
European journal of medicinal chemistry - 1 May 2008
Frey Virginie, Viaud Julien, Subra Guy, Cauquil Nicolas, Guichou Jean-François, Casara Patrick, Grassy Gérard, Chavanieu Alain
Abstract excerpt
To study the structure-activity relationships (SAR) and the binding activity of pro-apoptotic Bak BH3 domain, we synthesised several 16mer peptide analogues corresponding to the region (72)-GQVGRQLAIIGDDINR-(87). Using different amino acids varying in length, steric and electronic properties, we investigated the role and the nature of physicochemical parameters of residues Val74, Leu78, Ile81 and Ile85,...
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