Combinatorial chemistry identifies high-affinity peptidomimetics against α4β1 integrin for in vivo tumor imaging

Li Peng, Ruiwu Liu, Jan Marik, Xiaobing Wang, Yoshikazu Takada, Kit S. Lam

研究成果: 雜誌貢獻文章同行評審

210 引文 斯高帕斯(Scopus)


Small peptide-based agents have attracted wide interest as cancer-targeting agents for diagnostic imaging and targeted therapy. There is a need to develop new high-affinity and high-specificity peptidomimetic or small-molecule ligands against cancer cell surface receptors. Here we report on the identification of a high-affinity peptidomimetic ligand (LLP2A; IC50 = 2 pM) against α4β1 integrin using both diverse and highly focused one-bead-one-compound combinatorial peptidomimetic libraries in conjunction with high-stringency screening. We further demonstrate that LLP2A can be used to image α4β1-expressing lymphomas with high sensitivity and specificity when conjugated to a near infrared fluorescent dye in a mouse xenograft model. Thus, LLP2A provides an important tool for noninvasive monitoring of α4β1 expression and activity during tumor progression, and it shows great potential as an imaging and therapeutic agent for α4β1- positive tumors.

頁(從 - 到)381-389
期刊Nature Chemical Biology
出版狀態已發佈 - 七月 2006

ASJC Scopus subject areas

  • 細胞生物學
  • 分子生物學


深入研究「Combinatorial chemistry identifies high-affinity peptidomimetics against α<sub>4</sub>β<sub>1</sub> integrin for in vivo tumor imaging」主題。共同形成了獨特的指紋。