Article abstract
Nature Chemical Biology 2, 381 - 389 (2006)
Published online: 11 June 2006 | doi:10.1038/nchembio798
Combinatorial chemistry identifies high-affinity peptidomimetics against 
4
1 integrin for in vivo tumor imaging
Li Peng1, Ruiwu Liu1, Jan Marik1, Xiaobing Wang1, Yoshikazu Takada2 & Kit S Lam1
Abstract
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 
4
1 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 41-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 41 expression and activity during tumor progression, and it shows great potential as an imaging and therapeutic agent for 41-positive tumors.
- Division of Hematology & Oncology, Department of Internal Medicine, UC Davis Cancer Center, University of California, Davis, 4501 X Street, Sacramento, California 95817, USA.
- Department of Dermatology, University of California, Davis, 4501 X Street, Sacramento, California 95817, USA.
Correspondence to: Kit S Lam1 e-mail: Kit.Lam@ucdmc.ucdavis.edu
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