%0 Journal Article
%T Novel Linear Peptides with High Affinity to ¦Áv¦Â3 Integrin for Precise Tumor Identification
%A Congying Zhang
%A Guanhua Ai
%A Menglu Zhao
%A Min Zhang
%A Siwen Li
%A Weidong Gao
%A Xue Dong
%A Yi Ma
%A Yueqing Gu
%A Yuxi Liu
%A Zhaohui Wang
%A Zhihao Han
%J Theranostics
%D 2017
%I Ivyspring International Publisher
%R 10.7150/thno.18401
%X Development of alternative linear peptides for targeting ¦Áv¦Â3 integrin has attracted much attention, as the traditional peptide ligand, cyclic RGD, is limited by inferior water-solubility and complex synthesis. Using pharmacophore-based virtual screening and high-throughput molecular docking, we identified two novel linear small peptides RWr and RWrNM with high affinity and specificity to ¦Áv¦Â3 integrin. The competitive binding with cyclic RGD (c(RGDyK)) and cellular uptake related to the integrin expression levels verified their affinity to ¦Áv¦Â3 integrin. The intermolecular interaction measurement and dynamics simulation demonstrated the high binding affinity and stability, especially for RWrNM. In vivo peptide-guided tumor imaging and targeted therapy further confirmed their specificity. Results indicated that the newly identified small linear peptide RWrNM, with high affinity and specificity to ¦Áv¦Â3 integrin, better water-solubility, and simplified synthetic process, could overcome limitations of the current cyclic RGD peptides, paving the way for diverse use in diagnosis and therapy.
%K ¦Áv¦Â3 integrin
%K linear peptide
%K binding affinity.
%U http://www.thno.org/v07p1511.htm