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. Author manuscript; available in PMC: 2014 Jul 1.
Published in final edited form as: J Pharm Sci. 2013 Nov 25;103(1):29–52. doi: 10.1002/jps.23773

Table 7.

Select Tumor Antigens and Their Targeting Ligands

Disease Molecular Target Targeting Ligand Lipid Used In Vitro Test In Vivo Test
Breast cancer HER-2 SP90 SP90–PEG–DSPE +
Estrogen receptor Estrogen ES–PEG–DSPE + +
HER-2 mAb fragments mAb–PEG–DSPE + +
Surface nucleosomes mAb 2C5 mAb–PEG3400–DSPE + +
Ovarian cancer Gelactinase Gelactinase peptides CTT2–PEG3400–DSPE +
SSTR2 Octreotide OCT–PEG–DSPE + +
Alpha(v) beta(3) integrin RGD peptides RGD–PEG2000–DSPE + +
Lymphoma CD22 HB22.7 (mAb) mAb–DSPE–mPEG +
BAFF receptor mBAFF mBAFF–PEG–DSPE + +
CD19 Anti-CD19-IgG2a aCD19–DSPE–mPEG + +
Lung cancer NSCLC cell line SP5-2 SP5–PEG–DSPE +
LHRH receptor Analog of LHRH peptide LHRH–PEG–DSPE +
Murine tumor Transferrin receptor Transferrin Transferrin–DSPE–PEG + +
FA receptors Folic acid FA–PEG–DSPE +
Alpha(v) beta(3) integrin RGD tripeptides RGD–PEG–DSPE +
Prostate cancer Sigma receptor Anisamide AA–PEG3400–DSPE + +
EGFR Anti-EGFR scFv C10 scFv–PEG–DSPE +

+ stands for p < 0.05 or significant.

– stands for p > 0.05, insignificant or unspecified.

2C5, a monoclonal antibody that is a nucleosome-specific nonpathogenic antinuclear antibody; AA, anisamide; aCD19, antibody bound to CD19; CD19, cluster of differentiation 19; CD22, cluster of differentiation-22; CD19, cluster of differentiation-19; DSPE, distearoylphosphatidylcholine; EGFR, epidermal growth factor receptor; FA, folic acid; HER-2, human epidermal growth factor receptor 2; IgG2a, subclass of IgG; LHRH, luteinizing hormone-releasing hormone; mAB, monoclonal antibody; mBAFF, mutant soluble B-cell activating factor; NSCLC, nonsmall cell–lung carcinoma; PEG, polyethylene glycol; RGD, arginine–glycine–aspartate; anti-EGFR scFv C10, a novel anti-EGFR single-chain variable antibody fragment (scFv) generated from screening a phage antibody library; SSTR2, somatostatin receptor 2; SP90, a synthetic targeting peptide with a sequence of SMDPFLFQLLQ; and SP5-2, a synthetic peptide with a sequence TDSILRSYDWTY.