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SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL RGD ANALOGUES.

Authors :
Balacheva, Anelia
Lambev, Momchil
Detcheva, Roumyana
Bruckdorfer, Thomas
Pajpanova, Tamara
Source :
Journal of Chemical Technology & Metallurgy; 2020, Vol. 55 Issue 4, p698-701, 4p
Publication Year :
2020

Abstract

Peptides have been developed during the last decade as an alternative for delivery and targeting of drugs, and for the visualization of tumors. In contrast to the antibodies, the peptides are smaller and can be delivered to the cytoplasm by various mechanisms. RGD peptides have been developed as potent integrin ligands and antagonists that inhibit the adhesion and formation of tumor metastases or directly induce apoptosis by activating caspases. A series of short RGD mimetics and their conjugates are synthesized and their cytotoxic activity against four cancer cell lines is examined. RGD peptides modified by shorter homologues of with arginine (α-amino-4-guanidinobutyric acid (Agb) and α-amino-3-guanidino-propionic acid (Agp)) show an increase of the cytotoxic effect compared to that of the parent RGD peptide. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
13147471
Volume :
55
Issue :
4
Database :
Complementary Index
Journal :
Journal of Chemical Technology & Metallurgy
Publication Type :
Academic Journal
Accession number :
143642593