Conjugates for Angiogenesis Targeted Imaging

Compound

Nuclear imaging C(RGDfY) Gluco-RGD Galacto-RGD c(RGDf(N-Me)V)

DOTA-c(RGDyK)

HYNIC-RGD4C FB-c(RGDyK)2 DOTA-c(RGDyK)2

HYNIC-E-c(RGDfK)2

DOTA-E- c(RGDfK)2

DOTA-E{E- c(RGDfK)2}2 FB-PEG-c(RGDyK) DOTA-PEG-c(RGDyK) DOTA-PEG-E-c(RGDyK)2

HPMA copolymer-RGD4C

HPMA copolymer-RGDfK CGS27023A SAV03M D-Tyr-HWGF DOTA-HWGF

Magnetic resonance imaging Anti-aVb3 antibody (LM609)-

liposome Anti-aVb3 antibody (DM101)-

nanoparticle aVb3 peptidomimetic antagonist-

nanoparticle Optical imaging Cy5.5-c(RGDyK) Cy5.5- E- c(RGDyK)2 Cy5.5-E{E- c(RGDfK)2}2 Cy5.5-GPLGVRGK-PEG-PLL NIRQ820-GVPLSLTMGC-Cy5.5

Label

Cu-64

Tc-99m

F-18

Cu-64

Tc-99m

In-111

Tc-99m

In-111

F-18

F-18

I-125

Cu-64

Gadolinium Gadolinium Gadolinium

integrin integrin integrin integrin aVß3 integrin aVß3 aVß3 aVß3

integrin integrin integrin integrin aVß3 i aVß3 integrin integrin integrin integrin integrin aVß3 integrin aVß3 integrin

aVß3 integrin aVß3 integrin aVß3 integrin

Cy5.5(NIR dye)

Cy5.5

Cy5.5

Cy5.5

Cy5.5

Tumor Model Reference

Murine osteosarcoma 117

M21 human melanoma 120

M21 human melanoma 121

DLD-1 human colon 199

adenocarcinoma

MDA-MB-435 human 118

mammary carcinoma

Human renal adenocarcinoma 200

U87MG human glioblastoma 136

MDA-MB-435 human 135

mammary carcinoma

OVCAR-3 human ovarian 107

carcinoma

OVCAR-3 human ovarian 107

carcinoma

U87MG human glioblastoma 137

U87MG human glioblastoma 140

U87MG human glioblastoma 141

Human female lung 201

adenocarcinoma

DU145 & PC-3 human prostate 23, 178

carcinoma

Murine lewis lung carcinoma 181

Murine ehrlich breast tumor 85, 87

Murine ehrlich breast tumor 87

Murine lewis lung carcinoma 83

MDA-MB-435 human 90, 91 mammary carcinoma

Rabbit V2 carcinoma 126

Rabbit corneal micropocket 127 model

Rabbit V2 carcinoma 110

Cy5.5(NIR dye)

Cy5.5

Cy5.5

Cy5.5

aVß3 integrin

U87MG human glioblastoma

111

aVß3 integrin

U87MG human glioblastoma

129

aVß3 integrin

U87MG human glioblastoma

129

MMP-2

HT1080 human fibrosarcoma

94

MMP-7

HT1080 human fibrosarcoma

97

containing an Asn-Gly-Arg (NGR) motif.54 NGR peptides have been used to deliver chemothera-peutic agents64 and pro-apoptotic peptides65 to tumor cells. In a murine breast carcinoma xenograft model, a NGR-doxorubicin conjugate significantly decreased metastasis to lymph nodes and substantially increased survival compared to free doxorubicin. In addition, the conjugates were less toxic to the liver and heart as compared to the free drug.64

Aminopeptidase A (APA) is a homodimeric membrane, spanning cell surface protein that is upregulated in the pericytes of tumor blood vessels.66 Phage display studies have identified an APA binding peptide (CPRECESIC) that inhibits enzymatic activity of APA, suppresses both migration and proliferation of endothelial cells, and inhibits tumor growth.67

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