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Antitumor activity of opiorphin, sialorphin and their conjugates with a peptide klaklakklaklak
- Source :
- Journal of Peptide Science. 22:723-730
- Publication Year :
- 2016
- Publisher :
- Wiley, 2016.
-
Abstract
- This is the study on the effect of opiorphin, sialorphin and their analogs on antitumor activity. We demonstrated that conjugation of opiorphin and sialorphin with a proapoptotic, antimicrobial peptide klak (klaklakklaklak) led to compounds (opio-klak and sialo-klak) that were cytotoxic against cancer cells (LN18, PC3, A549, HCT116 and B10-F16) in the MTT test. The conjugated analogs were designed to increase the effectiveness of the peptide. The opio-klak derivative was the most effective in the in vitro assays and led to a decrease in viability of cancer cells over time as compared with that of untreated controls. In contrast, treatment with either the untargeted klak peptide or opiorphin as a negative control led to a negligible loss in viability. Antitumor effect of the opio-klak was also observed in vivo in murine melanoma tumor-bearing mice. Cessation of peptide administration resulted in tumor regrowth. Our results are seemingly valuable for the development of opiorphin analogs with potential clinical applications. Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd.
- Subjects :
- 0301 basic medicine
Peptide
Pharmacology
Biochemistry
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Structural Biology
In vivo
Drug Discovery
medicine
Peptide synthesis
Cytotoxic T cell
Molecular Biology
chemistry.chemical_classification
Melanoma
Organic Chemistry
Opiorphin
In vitro toxicology
General Medicine
medicine.disease
030104 developmental biology
chemistry
030220 oncology & carcinogenesis
Cancer cell
Molecular Medicine
medicine.drug
Subjects
Details
- ISSN :
- 10752617
- Volume :
- 22
- Database :
- OpenAIRE
- Journal :
- Journal of Peptide Science
- Accession number :
- edsair.doi...........31df7d80d97ee79eb720966c5fa73774