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
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
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,CPP
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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