Tumor targeting Peptides
Peptide showed good research value and application prospect in tumor immunotherapy because of its mature and stable synthesis process and good tumor penetration and biological compatibility.The number of peptide drugs entering clinical trials has been increasing in recent years,it plays an increasingly important role in tumor drug therapy.
Tumor targeting peptides can recognize tumor tissues and tumor associated micro environment, including tumor metastasis. These tumor-targeting peptides have a strong affinity for specific receptors/markers present in tumors and in tumor blood vessels .Thus, they can be used to deliver drugs selectively in tumors.They are also commonly known as tumor homing peptide because they travel through the bloodstream to the tumor site/vasculature.
RGD peptide is a kind of short peptide containing Arginine - Glycine - Aspartate (Arg - Gly - Asp).Tumor cells or neovascularization can specifically express certain integrins, such as αvβ3, which can bind RGD peptide with certain affinity and become a new target for tumor treatment.
Bankpeptide has rich experience in the synthesis of RDG peptides and can provide a variety of RGD peptides, RGD cyclic peptides.
Peptide Type Name Sequence Target Tumor N-terminus Modification Reference
Line   RGDF Sarcoma Protected with (Boc)2O Du H et al. Mol Pharm. 2011 Aug 1;8(4):1224-32.
Line   RGDPAYQRFL Breast cancer N/A Ahmed S et al. Anal Chem. 2010 Sep 15;82(18):7533-41.
Line   Ac-CRGDC GGKWCFR VCYRGICY RRCR Prostate cancer, Melanoma Acetylation Du H et al. Mol Pharm. 2011 Aug 1;8(4):1224-32.
Line   CRGDK-Amidation Breast cancer Amidation Kumar A et al.Biomaterials 2012 Feb;33(4):1180-9.
Cyclic   c(RGDfK)  Human glioblastoma and prostate cancer N/A Ito T et al. Bioorg Med Chem Lett 2011 Jun 15;21(12):3515-8.
Cyclic   c(RGDyC)   N/A  
Line   FITC-GGCRGDMFGC Metastiasis in tumor FITC labeling Borgne-Sanchez A et al. Cell Death Differ. 2007 Mar;14(3):422-35
NGR peptide is a kind of short peptide containing Asparagine - Arginine - Glycine (Asn - Gly - Arg) which can be specifically connect to the  cells expressing aminopeptidase CD13.
CD13 is a transmembrane metalloproteinases ,which is one of the important regulatory factor angiogenesis production has not been activated on normal vascular endothelial cells, and highly expressed in the endothelial cells in tumor angiogenesis, thus NGR modified liposomes by endothelial cells and tumor angiogenesis of specificity ligand CD13 combining liposome targeting tumor area to achieve targeted therapeutic purposes.
Peptide Type Name Sequence Target Tumor N-terminus Modification Reference
Line   CPNGRC Angiogenic tumors N/A Plesniak LA et al. Chem Biol Drug Des. 2010 Jun;75(6):551-62.
Line   WXEPAYNGRFL Breast cancer N/A Ahmed S et al. Anal Chem. 2010 Sep 15;82(18):7533-41.
Line   RGEPAYNGRFL Breast cancer N/A Ahmed S et al. Anal Chem. 2010 Sep 15;82(18):7533-41.
Cell-penetrating peptide is a kind of small molecules short peptide with transmembrane transport capacity. Their sequence length is generally no more than 30 amino acids and they are rich in basic amino acids in the sequence.
Human immunodeficiency virus type 1 activation of transcription factor TAT (Hiv-1 TAT) is the first cell penetrating peptide, which penetrates peptides into cells through a non-toxic and efficient way.
An important feature of cell penetrating peptides (CPPs) is that it can carry a variety of bioactive substances of different sizes and properties into cells, including small molecular compounds, dyes, peptides, peptide nucleo acid (PNA), proteins, plasmid DNA siRNA, 200nm liposomes, phage particles and superparamagnetic particles and so on . This property makes it possible to be a good vector for targeted drugs.
As a carrier, CPPs has the advantages of low toxicity and no cell type restrictions. Although CPPs can transport different types of substances into cells, its practical application focuses on the cell transport of oligonucleotides (ONs) and their analogues.
Name Sequence Target Tumor Effect Reference
MPG Ac-GALFLGFLGAA GSTMGAWSQPKKK RKV-Cys HeLa,Cos-7c Cellular uptake of single- and double-stranded ONs  
HS68, NIH-3T3 50 nmol/l siRNA→85% and 78% luciferase downregulation Simeoni et al.
HS68 100 nmol/l siRNA→60% GAPDH downregulation Simeoni et al.
MPGΔNLS Ac-GALFLGFLGAA GSTMGAWSQPKKK RKV-Cys HeLa, Cos-7 50 nmol/l siRNA→95% and 90% luciferase downregulation Simeoni et al.
Stearyl-R8 St-RRRRRRRR-NH2 EGFP-expressing hippocampal neurons 16 nmol/l siRNA→>50% reduction in EGFP activity Tönges et al.
EB1 LIKLWSHLIHIWFQN RRLKWKKK-Amide HeLa, HepG2 Luciferase downregulation Lundberg et al.
Tat-DRBD GRKKRRQRRRPQ-DRBD H1299, HUVEC, Jurkat T,hESC >90% reduction in GAPDH mRNA level Eguchi et al.
PF6 St-AGYLLGK[kk2sa4 qn4]INLKALAALAK KIL-NH2 Hepatoma, MEF, HUVEC, mESC Significant downregulation of HPRT1 El-Andaloussiet al.

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