
Herein, we report the synthesis and biological characterization of the new peptide psiRGDechi as the first step toward novel-targeted theranostics in melanoma. This pseudopeptide is designed from our previously reported RGDechi peptide, known to bind selectively alphavbeta3 integrin, and differs for a modified amide bond at the main protease cleavage site. This chemical modification drastically reduces the enzymatic degradation in serum, compared to its parental peptide, resulting in an overall magnification of the biological activity on a highly expressing alphavbeta3 human metastatic melanoma cell line. Selective inhibition of cell adhesion, wound healing, and invasion are demonstrated; near-infrared fluorescent psiRGDechi derivative is able to detect alphavbeta3 integrin in human melanoma xenografts in a selective fashion. More, molecular docking studies confirm that psiRGDechi recognizes the receptor similarly to RGDechi. All these findings pave the way for the future employment of this novel peptide as promising targeting probe and therapeutic agent in melanoma disease.![Your query: [atitle, adesc, keywords] "Antineoplastic Agents" OR [atitle, adesc, keywords] "Pharmacology" OR [atitle, adesc, keywords] "Cell Adhesion" OR [atitle, adesc, keywords] "Drug Effects" OR [atitle, adesc, keywords] "Integrin Alphavbeta3"](/img/info20.png)
![Your query: [btitle, keywords] "Antineoplastic Agents" [btitle, keywords] "Pharmacology" [btitle, keywords] "Cell Adhesion" [btitle, keywords] "Drug Effects" [btitle, keywords] "Integrin Alphavbeta3"](/img/info20.png)