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. Author manuscript; available in PMC: 2010 Feb 10.
Published in final edited form as: Expert Opin Drug Discov. 2007 Apr 1;2(4):525. doi: 10.1517/17460441.2.4.525

Table 1. Summary of targeting peptides either isolated by in vivo biopanning or evaluated in vivo.

Target Selection method(s) Peptide characteristics Reference
Cancer-related
Breast cancer M13 Phage display; mouse xenograft p160 (VPWMEPAYQRFL) targeted and internalized into MDA-MB-435 cells, IC50 = 0.6 μM, Kd = 0.86 μM [78,79]
Gastric cancer metastases M13 Phage display; mouse xenograft SWKLPPS-coated liposomes targeted peritoneal metastases of AZ-P7a cells and enhanced adriamycin anti-cancer activity [80]
Hepatocellular carcinoma M13 Phage display; mouse xenograft EGFR-selected GE11 (YHWYGYTPQNVI, Kd = 22 nM) and GE11-polyethylenimine vectors targeted SMMC-7721 cells [81]
M13 Phage display; mouse model SMMC-7721-selected KSLSRHDHIHHH suppressed tumor migration and when conjugated to TSST-1 superantigen, inhibited mouse H22 tumor growth [82]
M13 Phage display; mouse xenograft TACHQHVRMVRP targeted BEL-7402 tumors [83]
Leukemia One-bead-one compound; mouse xenograft Jurkat cell-selected LLP2A peptide targeted Molt-4 tumors; α4β1-integrin receptor ligand, IC50 = 2 pM [84,85]
Medullary thyroid carcinoma M13 Phage-display; mouse xenograft HTFEPGV phage targeted human MTC-derived TT cells and directed adenoviral binding and internalization [86]
M13 Phage-display; mouse in vivo biopanning; transgenic mouse model SRESPHP phage specifically targeted and internalized into MTC cells [87]
Melanoma M13 Phage display; mouse in vivo and in vitro biopanning; mouse model TRTKLPRLHLQS phage targeted B16 tumors and enhanced host immune response resulting in tumor necrosis and increased survival [88]
Pancreatic cancer fUSE 5 Phage display; mouse xenograft Penetratin sequence-conjugated G7-18NATE peptide decreased cell migration and metastasis; non-phosphorylated inhibitor targeted Grb7 SH2 domain [89,90]
M13 Phage display; mouse xenograft SHGFSRHSMTLI targeted irradiated Capan-2 tumors [91]
Prostate carcinoma fUSE 5 Phage display; mouse xenograft IAGLATPGWSHWLAL phage targeted PC-3 cells [92]
Bacterial display, FliTrx; mouse xenograft MM-2 (CPGDRGQRRLFSKIEGPC) targeted PC-3 cells [93]
M13 Phage display; mouse xenograft and rat model DUP-1 (FRPNRAQDYNTN) targeted DU-145 cells, IC50 = 180 nM [94]
Tumor vasculature fUSE 5 Phage-display, mouse models NGR-conjugated IFN-γ and NGR-conjugated TNF-α enhanced antitumor activity in T lymphoma (RMA), WEHI-164 fibrosarcoma, TS/A adenocarcinoma [97,99-101]
Non-cancer-related
Pancreas fUSE 5 Phage display; mouse in vivo biopanning CRVASVLPC phage targeted prolactin receptor in pancreas vasculature and islets [102]
fUSE 5 Phage display; mouse in vivo biopanning CVSNPRWKC and CHVLWSTRC, ephrin A-type ligand homologs, homed to pancreatic islets [103]
fd-tet Phage display RIP1 phage clone (LSGTPERSGQAVKVKLKAIP) targeted rat β-cells in islets [104]
Endothelium M13 Phage display; rat in vivo biopanning VNTANST and QPEHSST targeted adeno-associated virus to lung and brain endothelium, respectively [105]
T7 Phage display; ex vivo and in vivo mouse biopanning CRPPR peptide, and CKRAVR, CRSTRANPC, CPKTRRVPC phage targeted cardiac endothelium [106]
M13 Phage display; mouse inflammatory and atherosclerotic model CVHSPNKKC-coated superparamagnetic fluorescent nanoparticle targeted VCAM-1-expressing endothelium and atherosclerotic lesions [107]
M13 Phage display; mouse atherosclerotic model VHPKQHR-coated superparamagnetic fluorescent nanoparticle targeted VCAM-1-expressing endothelium and atherosclerotic lesions [108]
Fibrinogen/fibronectin T7 Phage-display; mouse zenograft and model CGLIIQKNEC,CNAGESSKNC targeted clotted plasma proteins and tumor tissue [109]

MTC: Medullary thyroid carcinoma; TT: Medullary thyroid carcinoma cells.