Abstract
Theranostic RGD-camptothecin conjugates, possessing a disulfide linker and a fluorescent naphthalimide moiety, were synthesized and biologically evaluated. The conjugates showed nanomolar affinity for the purified αVβ3-integrin receptor. For antiproliferative assays, the U87 human glioblastoma were chosen as αVβ3-expressing cells, whereas a non αVβ3-expressing clone (U87 β3-KO) was generated as negative control. Although the U87 β3-KO cells treated with the conjugates showed a statistically significant reduced fluorescence intensity (in the range 7–12 %) compared to the parental U87, internalization of the conjugates was clearly observed in both cell lines. Stability studies showed premature cleavage of the disulfide linker in the cell media, with consequent release of free camptothecin. Consistent with the results of the internalization and stability studies, the conjugates did not show significant selectivity against the U87 cells compared to the U87 β3-KO clone.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
