AI Article Synopsis
- - The high incidence of HER2-positive breast cancer poses a serious concern due to its elevated mortality rates, making early detection crucial for effective treatment and improved patient outcomes.
- - This study explores the development of DOTA-A9 peptide and its pegylated version, which were radiolabeled using a specific isotope to enhance tumor targeting and reduce non-target tissue uptake.
- - The new radiopeptides showed strong binding to breast cancer cells and effective clearance from normal organs, with enhanced tumor visibility in imaging studies, highlighting their potential as promising tools for targeting HER2-positive tumors in future clinical applications.
Article Abstract
Highest global cancer incidence of female breast cancer is a matter of great concern. HER2-positive breast cancers have high mortality rate hence detection at an early stage is vital for successful treatment, improved cancer care and survival rate. Radiolabeled peptides have emerged as new alternatives to radiolabeled antibodies to overcome the limitations of slow clearance and uptake in non-target tissues. Herein, DOTA-A9 peptide and its pegylated variant were constructed on solid phase and radiolabeled with [Lu]LuCl. [Lu]DOTA-A9 and [Lu]DOTA-PEG-A9 displayed high binding affinity (K = 48.4 ± 1.4 and 55.7 ± 12.3 nM respectively) in human breast carcinoma SKBR3 cells. Two radiopeptides exhibited renal excretion and rapid clearance from normal organs. Uptake in SKBR3 tumor and tumor-to-background ratios were significantly higher (p < 0.05) for [Lu]DOTA-PEG-A9 at the three time points investigated. Xenografts could be clearly visualized by [Lu]DOTA-PEG-A9 in SPECT images at 3, 24 and 48 h p.i. indicating the potential for further exploration as HER2-targeting probe. The encouraging in vivo profile of PEG construct, [Lu]DOTA-PEG-A9 incentivizes future studies for clinical applications.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9489682 | PMC |
| http://dx.doi.org/10.1038/s41598-022-19201-9 | DOI Listing |
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