Much Colorectal cancer (Hatakeyama et al., 2011) NGR (asparagines-glycine-arginine)

Much research is going on nanoparticles labeled with peptides as cancer imaging probes for the diagnosis purpose of cancer. On the basis of label sources, they can be classified in two classes, one class of peptides is derived from affinity selections (e.g., phage display) and the other ones come from the adaptation of natural sources. On the basis of their targeting strategy, one type of peptide labels, directly targets to the receptors present on the tumor cells while the other types of labels, target indirectly to tumor-associated systems like nutrisystems or immune systems. Normally, peptide-nanoparticles system for diagnostic purpose can be designed by conjugating a tumor-targeting peptide with the help of a spacer or linker to the imaging moiety. Prepared Pep-NPs probes having high cellular uptake and sufficient retention time in the tumor tissues, along with low penetration into the normal tissues so that the surrounding signal is reduced therefore imaging of tumor tissues will show high contrast. Table 1 describes various peptides used for the tumor targeting with their molecular targets.

Table 1. Peptides used as tumor targeting molecules

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Peptide

Targets

Sequence

Location

RGD

?v?3

RGD

Endothelial cells during tumor
angiogenesis and metastasis

Matrix metalloproteinases

MMP-2
MMP-9

CTTHWGFTLC

Breast carcionoma (Koivunen et al., 1999)

IF7

Anxal

IFLLWQR

Melanoma Colorectal cancer (Hatakeyama et al., 2011)

NGR (asparagines-glycine-arginine)

CD13

CNGRCVSGCAGRC

Endothelial cells of various types of tumors (Corti et al., 2008; Arap et al., 1998)

Neuropeptide-Y

NPY receptor

36-amino acid-long peptide

Breast carcinomas, adrenal
gland (Korner and Reubi, 2007), lymph node

Glucagon-like peptide-1

GLP-1 receptor

HAEGTFTSDVSSYLEGQAAKE-
FIAWLVKGRG

Brain, central nervous system,
Intestine

Bombesin

GRP receptor

p-EERLGNQWAVGHLM-NH2

Multi-tumor

Somatostatin

G-protein-coupled somatostatin 
Receptors

Analog commonly used

Digestive system; Brain

Transferrin

Transferrin receptor

760-amino acid-long peptide

Multi-tumors (Kim et al., 2012)

Cholecystokinin

CCK receptor

DY(SO3H)MGWMDF-NH2
(CCK-8)

Medullary thyroid cancer

Vasoactive intestinal peptide

VIP receptor

28-amino acid-long peptide

Multi-tumors

Gastrin releasing Peptide

GRP receptor

Generated by processing of a 125- amino acid prohormone

Multi-cancer (Patel et al., 2006)

Neurotensin

NT receptor

p-ELYGNKPRRPYIL

Multi-tumors

TCP-1

Colorectal cancer

CTPSPFSHC

Colon and gastric cancers (Svensen et al., 2012)

PEGA

Membrane bound proline-specific
aminopeptidase P

CPGPEGAGC

Breast tumor (Svensen et al., 2012)

DV1-DV3

Chemokine receptor 4

DV1
(LGASWHRPDKCCLGYQKRPLP);
its shorter analog,  DV3
cyclo-(LGASWHRPDK)

Multi-tumors (Svensen et al., 2012)

Fms-like Tyrosine kinase-1

VEGF1-receptor

WFLLTM

Multi-tumor (Fairbrother et al., 1998)

CBO-P11

VEGF2 receptor

Cyclo-
(DFPQIMRIKPHQGQHIGE)55

Tumor angiogenesis (Zilberberg et al., 2003)

Anti-HER2 antibody (AHNP)

Human Epidermal Growth Factor Receptor 2

FCDGFYACYKDV

Breast cancer, ovarian cancer,
Gastric cancer (Tai et al., 2010)